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

2274 3173 None 38 Human Functional pAC50 = 5 5.0 -724 36
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 5.0 -724 36
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 5.0 -724 36
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 5.0 -724 36
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 5.0 -724 36
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 5.0 -724 36
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2600 3779 None 53 Human Functional pAC50 = 5 5.0 -389 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3779 None 53 Human Functional pAC50 = 5 5.0 -389 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3779 None 53 Human Functional pAC50 = 5 5.0 -389 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3779 None 53 Human Functional pAC50 = 5 5.0 -389 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3779 None 53 Human Functional pAC50 = 5 5.0 -389 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2520 206466 None 47 Human Functional pAC50 = 5 5.0 -26 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 5.0 -26 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 5.0 -26 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
72093 35070 None 5 Human Functional pAC50 = 5.0 5.0 -10 28
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.0 5.0 -10 28
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.0 5.0 -10 28
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
4031 99367 None 27 Human Functional pAC50 = 5.0 5.0 -18 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.0 5.0 -18 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
1234 189330 None 32 Human Functional pAC50 = 5.0 5.0 -41 10
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.0 5.0 -41 10
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.0 5.0 -41 10
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
4452 2762 None 13 Human Functional pAC50 = 7.0 7.0 -162 21
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.0 7.0 -162 21
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.0 7.0 -162 21
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
1593 2340 None 41 Human Functional pAC50 = 6.0 6.0 -23 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
30668 2340 None 41 Human Functional pAC50 = 6.0 6.0 -23 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
30668.0 2340 None 41 Human Functional pAC50 = 6.0 6.0 -23 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
9868 2340 None 41 Human Functional pAC50 = 6.0 6.0 -23 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
CHEMBL17860 2340 None 41 Human Functional pAC50 = 6.0 6.0 -23 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
DB04948 2340 None 41 Human Functional pAC50 = 6.0 6.0 -23 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
55645 84404 None 3 Human Functional pAC50 = 6.0 6.0 -389 11
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.0 6.0 -389 11
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.0 6.0 -389 11
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2477 745 None 38 Human Functional pAC50 = 6.9 6.9 -2 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.9 6.9 -2 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.9 6.9 -2 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.9 6.9 -2 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.9 6.9 -2 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.9 6.9 -2 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2372 106524 None 30 Human Functional pAC50 = 5.9 5.9 -51 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 345 10 2 5 2.6 COc1ccc(CCNCC(O)COc2cccc(C)c2)cc1OC 10.1038/s41467-023-40064-9
CHEMBL314010 106524 None 30 Human Functional pAC50 = 5.9 5.9 -51 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 345 10 2 5 2.6 COc1ccc(CCNCC(O)COc2cccc(C)c2)cc1OC 10.1038/s41467-023-40064-9
4418 34231 None 58 Human Functional pAC50 = 5.9 5.9 -1 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -1 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -1 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -1 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2448 99377 None 50 Human Functional pAC50 = 5.9 5.9 -54 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -54 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -54 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -54 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
47936 193531 None 56 Human Functional pAC50 = 5.9 5.9 -25 6
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -25 6
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2869 4152 None 54 Human Functional pAC50 = 4.9 4.9 -4265 5
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -4265 5
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -4265 5
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -4265 5
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -4265 5
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -4265 5
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
68617 207985 None 33 Human Functional pAC50 = 4.9 4.9 -34 30
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.9 4.9 -34 30
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.9 4.9 -34 30
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
4567 9950 None 29 Human Functional pAC50 = 4.9 4.9 -114 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL114655 9950 None 29 Human Functional pAC50 = 4.9 4.9 -114 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
2543 3707 None 46 Human Functional pAC50 = 4.9 4.9 -204 14
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.9 4.9 -204 14
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.9 4.9 -204 14
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.9 4.9 -204 14
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.9 4.9 -204 14
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.9 4.9 -204 14
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
34633 5466 None 43 Human Functional pAC50 = 4.9 4.9 1 2
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 427 5 1 6 4.1 CCOC(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCOCC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1075 5466 None 43 Human Functional pAC50 = 4.9 4.9 1 2
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 427 5 1 6 4.1 CCOC(=O)Nc1ccc2c(c1)N(C(=O)CCN1CCOCC1)c1ccccc1S2 10.1038/s41467-023-40064-9
2162 41527 None 58 Human Functional pAC50 = 4.9 4.9 -15 22
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -15 22
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2165 206241 None 47 Human Functional pAC50 = 4.9 4.9 -8 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
3647519 206241 None 47 Human Functional pAC50 = 4.9 4.9 -8 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
CHEMBL682 206241 None 47 Human Functional pAC50 = 4.9 4.9 -8 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 355 6 2 4 5.2 CCN(CC)Cc1cc(Nc2ccnc3cc(Cl)ccc23)ccc1O 10.1038/s41467-023-40064-9
3689 102826 None 36 Human Functional pAC50 = 5.9 5.9 -186 16
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.9 5.9 -186 16
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.9 5.9 -186 16
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
135398737 958 None 57 Human Functional pAC50 = 5.9 5.9 -295 43
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -295 43
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -295 43
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -295 43
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -295 43
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -295 43
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
1212 1662 None 37 Human Functional pAC50 = 5.9 5.9 -1071 35
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -1071 35
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -1071 35
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -1071 35
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -1071 35
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -1071 35
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
103 4153 None 44 Human Functional pAC50 = 5.9 5.9 -154 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -154 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -154 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -154 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.9 5.9 -154 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
150 2509 None 14 Human Functional pAC50 = 7.8 7.8 -5 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.8 7.8 -5 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.8 7.8 -5 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.8 7.8 -5 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.8 7.8 -5 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.8 7.8 -5 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
10531 1420 None 13 Human Functional pAC50 = 6.9 6.9 -48 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.9 6.9 -48 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.9 6.9 -48 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.9 6.9 -48 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.9 6.9 -48 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.9 6.9 -48 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
212 3806 None 35 Human Functional pAC50 = 5.9 5.9 -309 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -309 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -309 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -309 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -309 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -309 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
71481097 120574 None 38 Human Functional pAC50 = 4.9 4.9 1 2
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 2 7 3.4 O=C(/C=C\n1cnc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)n1)NNc1cnccn1 10.1038/s41467-023-40064-9
CHEMBL3545185 120574 None 38 Human Functional pAC50 = 4.9 4.9 1 2
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 443 5 2 7 3.4 O=C(/C=C\n1cnc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)n1)NNc1cnccn1 10.1038/s41467-023-40064-9
187 255 None 24 Human Functional pAC50 = 6.8 6.8 -3 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
187.0 255 None 24 Human Functional pAC50 = 6.8 6.8 -3 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
294 255 None 24 Human Functional pAC50 = 6.8 6.8 -3 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
65 255 None 24 Human Functional pAC50 = 6.8 6.8 -3 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
8593 255 None 24 Human Functional pAC50 = 6.8 6.8 -3 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
CHEMBL667 255 None 24 Human Functional pAC50 = 6.8 6.8 -3 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
DB03128 255 None 24 Human Functional pAC50 = 6.8 6.8 -3 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 146 3 0 2 0.3 CC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
4640 78295 None 23 Human Functional pAC50 = 6.8 6.8 -1 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.8 6.8 -1 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
213 3853 None 34 Human Functional pAC50 = 5.8 5.8 -33 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.8 5.8 -33 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.8 5.8 -33 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.8 5.8 -33 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.8 5.8 -33 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.8 5.8 -33 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
4066 207084 None 54 Human Functional pAC50 = 4.8 4.8 -954 16
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -954 16
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -954 16
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -954 16
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
1193 1656 None 64 Human Functional pAC50 = 4.8 4.8 -194 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
2447 1656 None 64 Human Functional pAC50 = 4.8 4.8 -194 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3371 1656 None 64 Human Functional pAC50 = 4.8 4.8 -194 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL23588 1656 None 64 Human Functional pAC50 = 4.8 4.8 -194 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB02266 1656 None 64 Human Functional pAC50 = 4.8 4.8 -194 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 281 3 2 2 4.1 OC(=O)c1ccccc1Nc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
135398737 958 None 57 Human Functional pAC50 = 4.8 4.8 -295 43
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -295 43
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -295 43
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -295 43
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -295 43
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -295 43
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2389 3331 None 72 Human Functional pAC50 = 5.8 5.8 -812 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.8 5.8 -812 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.8 5.8 -812 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.8 5.8 -812 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.8 5.8 -812 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.8 5.8 -812 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2470 3653 None 40 Human Functional pAC50 = 7.8 7.8 -3388 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.8 7.8 -3388 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.8 7.8 -3388 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.8 7.8 -3388 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.8 7.8 -3388 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2169 44861 None 29 Human Functional pAC50 = 6.8 6.8 -1 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.8 6.8 -1 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
118422671 2757 None 41 Human Functional pAC50 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.8 5.8 -158 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
119570 3159 None 58 Human Functional pAC50 = 4.8 4.8 -10000 11
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -10000 11
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -10000 11
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -10000 11
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -10000 11
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -10000 11
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2335 11852 None 18 Human Functional pAC50 = 4.8 4.8 -117 34
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -117 34
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -117 34
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -117 34
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
21722 17999 None 26 Human Functional pAC50 = 4.8 4.8 -27 21
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -27 21
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
16231 209968 None 39 Human Functional pAC50 = 4.8 4.8 -4 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N 10.1038/s41467-023-40064-9
CHEMBL945 209968 None 39 Human Functional pAC50 = 4.8 4.8 -4 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N 10.1038/s41467-023-40064-9
37 778 None 41 Human Functional pAC50 = 6.8 6.8 -9 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.8 6.8 -9 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.8 6.8 -9 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.8 6.8 -9 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.8 6.8 -9 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.8 6.8 -9 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
16363 596 None 33 Human Functional pAC50 = 6.8 6.8 -31 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.8 6.8 -31 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.8 6.8 -31 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.8 6.8 -31 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.8 6.8 -31 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.8 6.8 -31 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
3658 4107 None 38 Human Functional pAC50 = 7.8 7.8 -5 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.8 7.8 -5 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.8 7.8 -5 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.8 7.8 -5 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.8 7.8 -5 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.8 7.8 -5 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
31101 729 None 28 Human Functional pAC50 = 6.8 6.8 -53 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
31101.0 729 None 28 Human Functional pAC50 = 6.8 6.8 -53 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 729 None 28 Human Functional pAC50 = 6.8 6.8 -53 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 729 None 28 Human Functional pAC50 = 6.8 6.8 -53 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 729 None 28 Human Functional pAC50 = 6.8 6.8 -53 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 729 None 28 Human Functional pAC50 = 6.8 6.8 -53 29
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
4046 2483 None 21 Human Functional pAC50 = 4.8 4.8 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2600 3779 None 53 Human Functional pAC50 = 4.8 4.8 -389 32
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3779 None 53 Human Functional pAC50 = 4.8 4.8 -389 32
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3779 None 53 Human Functional pAC50 = 4.8 4.8 -389 32
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3779 None 53 Human Functional pAC50 = 4.8 4.8 -389 32
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3779 None 53 Human Functional pAC50 = 4.8 4.8 -389 32
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
43815 187026 None 38 Human Functional pAC50 = 4.8 4.8 -169 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -169 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -169 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2136 3095 None 24 Human Functional pAC50 = 4.8 4.8 -338 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.8 4.8 -338 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.8 4.8 -338 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.8 4.8 -338 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.8 4.8 -338 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.8 4.8 -338 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
6018 11069 None 60 Human Functional pAC50 = 4.8 4.8 -2 4
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 317 4 0 4 3.2 COc1cc2c(cc1OC)C1CC(=O)C(CC(C)C)CN1CC2 10.1038/s41467-023-40064-9
CHEMBL117785 11069 None 60 Human Functional pAC50 = 4.8 4.8 -2 4
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 317 4 0 4 3.2 COc1cc2c(cc1OC)C1CC(=O)C(CC(C)C)CN1CC2 10.1038/s41467-023-40064-9
4011 82440 None 34 Human Functional pAC50 = 4.8 4.8 -2137 26
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -2137 26
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
4993 122423 None 61 Human Functional pAC50 = 4.8 4.8 -4 5
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.8 4.8 -4 5
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
26248 161633 None 72 Human Functional pAC50 = 4.8 4.8 -1 11
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
3157 1470 None 44 Human Functional pAC50 = 4.8 4.8 -17378 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.8 4.8 -17378 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.8 4.8 -17378 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.8 4.8 -17378 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.8 4.8 -17378 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.8 4.8 -17378 21
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2601 3780 None 25 Human Functional pAC50 = 6.8 6.8 -57 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.8 6.8 -57 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.8 6.8 -57 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.8 6.8 -57 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.8 6.8 -57 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
26987 949 None 27 Human Functional pAC50 = 4.7 4.7 -7079 34
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -7079 34
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -7079 34
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -7079 34
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -7079 34
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -7079 34
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
107641 61163 None 56 Human Functional pAC50 = 5.7 5.7 2 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 4 1 2 3.4 CCC(C(=O)O)c1ccc(N2Cc3ccccc3C2=O)cc1 10.1038/s41467-023-40064-9
CHEMBL1765292 61163 None 56 Human Functional pAC50 = 5.7 5.7 2 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 295 4 1 2 3.4 CCC(C(=O)O)c1ccc(N2Cc3ccccc3C2=O)cc1 10.1038/s41467-023-40064-9
129211 3749 None 48 Human Functional pAC50 = 7.7 7.7 -43 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
129211.0 3749 None 48 Human Functional pAC50 = 7.7 7.7 -43 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
2562 3749 None 48 Human Functional pAC50 = 7.7 7.7 -43 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
488 3749 None 48 Human Functional pAC50 = 7.7 7.7 -43 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
CHEMBL836 3749 None 48 Human Functional pAC50 = 7.7 7.7 -43 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
DB00706 3749 None 48 Human Functional pAC50 = 7.7 7.7 -43 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
134 2514 None 19 Human Functional pAC50 = 6.7 6.7 -97 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.7 6.7 -97 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.7 6.7 -97 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.7 6.7 -97 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.7 6.7 -97 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.7 6.7 -97 18
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
1890 2759 None 31 Human Functional pAC50 = 5.7 5.7 -5 28
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.7 5.7 -5 28
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.7 5.7 -5 28
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.7 5.7 -5 28
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.7 5.7 -5 28
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2202 3132 None 63 Human Functional pAC50 = 4.7 4.7 -338 10
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4850 3132 None 63 Human Functional pAC50 = 4.7 4.7 -338 10
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4850.0 3132 None 63 Human Functional pAC50 = 4.7 4.7 -338 10
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
49 3132 None 63 Human Functional pAC50 = 4.7 4.7 -338 10
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
CHEMBL1371770 3132 None 63 Human Functional pAC50 = 4.7 4.7 -338 10
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
DB12478 3132 None 63 Human Functional pAC50 = 4.7 4.7 -338 10
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
2162 41527 None 58 Human Functional pAC50 = 4.7 4.7 -15 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -15 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
1549120 198942 None 55 Human Functional pAC50 = 4.7 4.7 -13 19
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56337 198942 None 55 Human Functional pAC50 = 4.7 4.7 -13 19
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
3149 12618 None 11 Human Functional pAC50 = 4.7 4.7 -60 26
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.7 4.7 -60 26
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
1210 918 None 42 Human Functional pAC50 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2290 22
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
610479 15507 None 60 Human Functional pAC50 = 4.7 4.7 -2 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.7 4.7 -2 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
53276 95087 None 38 Human Functional pAC50 = 4.7 4.7 -1 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 304 5 3 5 3.0 CCOC(=O)Nc1ccc(NCc2ccc(F)cc2)nc1N 10.1038/s41467-023-40064-9
CHEMBL255044 95087 None 38 Human Functional pAC50 = 4.7 4.7 -1 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 304 5 3 5 3.0 CCOC(=O)Nc1ccc(NCc2ccc(F)cc2)nc1N 10.1038/s41467-023-40064-9
37264 189531 None 18 Human Functional pAC50 = 4.7 4.7 -14 3
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 435 6 2 10 1.3 COc1cc2c(N)nc(N3CCN(C(=O)OCC(C)(C)O)CC3)nc2c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL513301 189531 None 18 Human Functional pAC50 = 4.7 4.7 -14 3
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 435 6 2 10 1.3 COc1cc2c(N)nc(N3CCN(C(=O)OCC(C)(C)O)CC3)nc2c(OC)c1OC 10.1038/s41467-023-40064-9
1043 1582 None 6 Human Functional pAC50 = 6.7 6.7 -1096 22
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.7 6.7 -1096 22
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.7 6.7 -1096 22
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.7 6.7 -1096 22
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.7 6.7 -1096 22
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.7 6.7 -1096 22
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
124087 1389 None 72 Human Functional pAC50 = 4.6 4.6 -363 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.6 4.6 -363 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.6 4.6 -363 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.6 4.6 -363 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.6 4.6 -363 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.6 4.6 -363 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
154257 178724 None 43 Human Functional pAC50 = 4.6 4.6 -107 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.6 4.6 -107 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
5077 3578 None 61 Human Functional pAC50 = 4.6 4.6 -912 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.6 4.6 -912 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.6 4.6 -912 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.6 4.6 -912 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.6 4.6 -912 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.6 4.6 -912 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2880 98061 None 34 Human Functional pAC50 = 4.6 4.6 -23 9
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 5 0 3 4.6 C=C(c1ccccc1OCc1cccc(Cl)c1)n1ccnc1 10.1038/s41467-023-40064-9
CHEMBL27289 98061 None 34 Human Functional pAC50 = 4.6 4.6 -23 9
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 310 5 0 3 4.6 C=C(c1ccccc1OCc1cccc(Cl)c1)n1ccnc1 10.1038/s41467-023-40064-9
102 4127 None 36 Human Functional pAC50 = 6.6 6.6 -23 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 4127 None 36 Human Functional pAC50 = 6.6 6.6 -23 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 4127 None 36 Human Functional pAC50 = 6.6 6.6 -23 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969.0 4127 None 36 Human Functional pAC50 = 6.6 6.6 -23 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 4127 None 36 Human Functional pAC50 = 6.6 6.6 -23 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 4127 None 36 Human Functional pAC50 = 6.6 6.6 -23 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2105 3054 None 28 Human Functional pAC50 = 6.6 6.6 -23 25
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.6 6.6 -23 25
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.6 6.6 -23 25
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.6 6.6 -23 25
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.6 6.6 -23 25
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
636403 188375 None 19 Human Functional pAC50 = 5.6 5.6 3 7
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.6 5.6 3 7
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
123606 352 None 46 Human Functional pAC50 = 4.6 4.6 -2089 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.6 4.6 -2089 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.6 4.6 -2089 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.6 4.6 -2089 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.6 4.6 -2089 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.6 4.6 -2089 6
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
392622 56328 None 57 Human Functional pAC50 = 4.6 4.6 -21 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 56328 None 57 Human Functional pAC50 = 4.6 4.6 -21 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
1981 67484 None 62 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 6 1 6 3.5 COc1ccc2c(c1)c(CC(=O)OCC(=O)O)c(C)n2C(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL189171 67484 None 62 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 6 1 6 3.5 COc1ccc2c(c1)c(CC(=O)OCC(=O)O)c(C)n2C(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
25382 9159 None 27 Human Functional pAC50 = 4.6 4.6 -707 21
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 4.6 4.6 -707 21
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
5288783 14438 None 36 Human Functional pAC50 = 4.6 4.6 -2 3
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 5 3 3 5.1 C=C1/C(=C\C=C2/CCC[C@]3(C)[C@@H]([C@H](C)/C=C/[C@@H](O)C4CC4)CC[C@@H]23)C[C@@H](O)C[C@@H]1O 10.1038/s41467-023-40064-9
CHEMBL1200666 14438 None 36 Human Functional pAC50 = 4.6 4.6 -2 3
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 5 3 3 5.1 C=C1/C(=C\C=C2/CCC[C@]3(C)[C@@H]([C@H](C)/C=C/[C@@H](O)C4CC4)CC[C@@H]23)C[C@@H](O)C[C@@H]1O 10.1038/s41467-023-40064-9
157355 57525 None 40 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 344 8 9 11 -5.8 OC[C@@H](O)[C@@H](O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO 10.1038/s41467-023-40064-9
CHEMBL1661 57525 None 40 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 344 8 9 11 -5.8 OC[C@@H](O)[C@@H](O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO 10.1038/s41467-023-40064-9
2515 78279 None 44 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 283 7 3 7 0.8 CCOC(=O)NNc1ccc(N(CC)CC(C)O)nn1 10.1038/s41467-023-40064-9
CHEMBL2106561 78279 None 44 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 283 7 3 7 0.8 CCOC(=O)NNc1ccc(N(CC)CC(C)O)nn1 10.1038/s41467-023-40064-9
168871 89164 None 10 Human Functional pAC50 = 6.6 6.6 -20 13
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 6.6 6.6 -20 13
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
209 3057 None 57 Human Functional pAC50 = 5.6 5.6 -1174 25
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.6 5.6 -1174 25
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.6 5.6 -1174 25
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.6 5.6 -1174 25
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.6 5.6 -1174 25
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.6 5.6 -1174 25
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
4940 14476 None 26 Human Functional pAC50 = 5.6 5.6 -91 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.6 5.6 -91 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
44112 121354 None 36 Human Functional pAC50 = 7.6 7.6 -3 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.6 7.6 -3 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
1816 2540 None 64 Human Functional pAC50 = 4.5 4.5 -4466 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -4466 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -4466 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -4466 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -4466 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -4466 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
11504295 2923 None 40 Human Functional pAC50 = 4.5 4.5 -218776 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -218776 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -218776 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -218776 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -218776 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -218776 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2467 67446 None 31 Human Functional pAC50 = 4.5 4.5 -6 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 8 0 5 2.8 COc1cc(OC)c(C(=O)CCCN2CCCC2)c(OC)c1 10.1038/s41467-023-40064-9
CHEMBL188921 67446 None 31 Human Functional pAC50 = 4.5 4.5 -6 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 307 8 0 5 2.8 COc1cc(OC)c(C(=O)CCCN2CCCC2)c(OC)c1 10.1038/s41467-023-40064-9
2247 505 None 55 Human Functional pAC50 = 5.5 5.5 -53 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.5 5.5 -53 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.5 5.5 -53 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.5 5.5 -53 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.5 5.5 -53 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
12582 950 None 27 Human Functional pAC50 = 5.5 5.5 -234 7
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1038/s41467-023-40064-9
2783 950 None 27 Human Functional pAC50 = 5.5 5.5 -234 7
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1038/s41467-023-40064-9
2783.0 950 None 27 Human Functional pAC50 = 5.5 5.5 -234 7
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1038/s41467-023-40064-9
CHEMBL49080 950 None 27 Human Functional pAC50 = 5.5 5.5 -234 7
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1038/s41467-023-40064-9
DB01407 950 None 27 Human Functional pAC50 = 5.5 5.5 -234 7
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1038/s41467-023-40064-9
31101 729 None 28 Human Functional pAC50 = 5.5 5.5 -53 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -53 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -53 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -53 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -53 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -53 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2337 3256 None 51 Human Functional pAC50 = 5.5 5.5 -10 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -10 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -10 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -10 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -10 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -10 29
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2393 3334 None 46 Human Functional pAC50 = 5.5 5.5 -75 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -75 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -75 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -75 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -75 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -75 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
5090 15568 None 65 Human Functional pAC50 = 4.5 4.5 -1 3
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 10.1038/s41467-023-40064-9
CHEMBL122 15568 None 65 Human Functional pAC50 = 4.5 4.5 -1 3
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 10.1038/s41467-023-40064-9
3158 56283 None 21 Human Functional pAC50 = 4.5 4.5 -3890 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -3890 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -3890 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.5 4.5 -3890 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2220 3134 None 58 Human Functional pAC50 = 5.5 5.5 -398 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -398 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -398 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -398 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -398 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.5 5.5 -398 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
9687 185441 None 21 Human Functional pAC50 = 4.4 4.4 -229 4
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 7 2 11 1.7 CCCC(=O)Nc1ncnc2c1ncn2[C@@H]1O[C@@H]2COP(=O)(O)O[C@H]2[C@H]1OC(=O)CCC 10.1038/s41467-023-40064-9
CHEMBL1522836 185441 None 21 Human Functional pAC50 = 4.4 4.4 -229 4
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 7 2 11 1.7 CCCC(=O)Nc1ncnc2c1ncn2[C@@H]1O[C@@H]2COP(=O)(O)O[C@H]2[C@H]1OC(=O)CCC 10.1038/s41467-023-40064-9
CHEMBL485980 185441 None 21 Human Functional pAC50 = 4.4 4.4 -229 4
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 469 7 2 11 1.7 CCCC(=O)Nc1ncnc2c1ncn2[C@@H]1O[C@@H]2COP(=O)(O)O[C@H]2[C@H]1OC(=O)CCC 10.1038/s41467-023-40064-9
47979 78239 None 45 Human Functional pAC50 = 5.4 5.4 -1202 9
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.4 5.4 -1202 9
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2543 3707 None 46 Human Functional pAC50 = 4.4 4.4 -204 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.4 4.4 -204 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.4 4.4 -204 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.4 4.4 -204 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.4 4.4 -204 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 4.4 4.4 -204 14
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
3899 210233 None 68 Human Functional pAC50 = 4.4 4.4 -478 7
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 270 2 1 3 3.3 Cc1oncc1C(=O)Nc1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
CHEMBL960 210233 None 68 Human Functional pAC50 = 4.4 4.4 -478 7
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 270 2 1 3 3.3 Cc1oncc1C(=O)Nc1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
2585 803 None 59 Human Functional pAC50 = 7.4 7.4 -36 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.4 7.4 -36 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.4 7.4 -36 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.4 7.4 -36 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.4 7.4 -36 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 7.4 7.4 -36 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
242 470 None 70 Human Functional pAC50 = 5.4 5.4 -31 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -31 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -31 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -31 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -31 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -31 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
33624 3821 None 21 Human Functional pAC50 = 5.4 5.4 -8317 6
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1038/s41467-023-40064-9
33624.0 3821 None 21 Human Functional pAC50 = 5.4 5.4 -8317 6
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1038/s41467-023-40064-9
4061 3821 None 21 Human Functional pAC50 = 5.4 5.4 -8317 6
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1038/s41467-023-40064-9
565 3821 None 21 Human Functional pAC50 = 5.4 5.4 -8317 6
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL499 3821 None 21 Human Functional pAC50 = 5.4 5.4 -8317 6
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1038/s41467-023-40064-9
DB00373 3821 None 21 Human Functional pAC50 = 5.4 5.4 -8317 6
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 316 6 2 8 0.5 O[C@H](COc1nsnc1N1CCOCC1)CNC(C)(C)C 10.1038/s41467-023-40064-9
19675 51685 None 37 Human Functional pAC50 = 7.4 7.4 -3 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.4 7.4 -3 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2318 154946 None 18 Human Functional pAC50 = 5.4 5.4 -6 15
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -6 15
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
100 3805 None 44 Human Functional pAC50 = 6.4 6.4 -162 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.4 6.4 -162 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.4 6.4 -162 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.4 6.4 -162 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.4 6.4 -162 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
135 2532 None 33 Human Functional pAC50 = 5.4 5.4 -354 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -354 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -354 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -354 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -354 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.4 5.4 -354 33
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
11658860 2344 None 24 Human Functional pAC50 = 5.4 5.4 -380 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.4 5.4 -380 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.4 5.4 -380 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.4 5.4 -380 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.4 5.4 -380 11
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2726 919 None 48 Human Functional pAC50 = 5.4 5.4 -2089 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2726.0 919 None 48 Human Functional pAC50 = 5.4 5.4 -2089 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 None 48 Human Functional pAC50 = 5.4 5.4 -2089 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 None 48 Human Functional pAC50 = 5.4 5.4 -2089 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 None 48 Human Functional pAC50 = 5.4 5.4 -2089 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 None 48 Human Functional pAC50 = 5.4 5.4 -2089 42
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
137 370 None 37 Human Functional pAC50 = 5.3 5.3 -162 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
2119 370 None 37 Human Functional pAC50 = 5.3 5.3 -162 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
563 370 None 37 Human Functional pAC50 = 5.3 5.3 -162 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
66368 370 None 37 Human Functional pAC50 = 5.3 5.3 -162 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
CHEMBL266195 370 None 37 Human Functional pAC50 = 5.3 5.3 -162 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
DB00866 370 None 37 Human Functional pAC50 = 5.3 5.3 -162 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
118985385 1701 None 63 Human Functional pAC50 = 4.3 4.3 -7 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 330 5 3 5 1.9 OC(=O)c1cc(c(cc1NCc1ccco1)Cl)S(=O)(=O)N 10.1038/s41467-023-40064-9
1258 1701 None 63 Human Functional pAC50 = 4.3 4.3 -7 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 330 5 3 5 1.9 OC(=O)c1cc(c(cc1NCc1ccco1)Cl)S(=O)(=O)N 10.1038/s41467-023-40064-9
3440 1701 None 63 Human Functional pAC50 = 4.3 4.3 -7 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 330 5 3 5 1.9 OC(=O)c1cc(c(cc1NCc1ccco1)Cl)S(=O)(=O)N 10.1038/s41467-023-40064-9
4839 1701 None 63 Human Functional pAC50 = 4.3 4.3 -7 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 330 5 3 5 1.9 OC(=O)c1cc(c(cc1NCc1ccco1)Cl)S(=O)(=O)N 10.1038/s41467-023-40064-9
CHEMBL35 1701 None 63 Human Functional pAC50 = 4.3 4.3 -7 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 330 5 3 5 1.9 OC(=O)c1cc(c(cc1NCc1ccco1)Cl)S(=O)(=O)N 10.1038/s41467-023-40064-9
DB00695 1701 None 63 Human Functional pAC50 = 4.3 4.3 -7 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 330 5 3 5 1.9 OC(=O)c1cc(c(cc1NCc1ccco1)Cl)S(=O)(=O)N 10.1038/s41467-023-40064-9
2435 722 None 63 Human Functional pAC50 = 5.3 5.3 -1659 10
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
2435.0 722 None 63 Human Functional pAC50 = 5.3 5.3 -1659 10
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
395 722 None 63 Human Functional pAC50 = 5.3 5.3 -1659 10
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
520 722 None 63 Human Functional pAC50 = 5.3 5.3 -1659 10
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
5386 722 None 63 Human Functional pAC50 = 5.3 5.3 -1659 10
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL844 722 None 63 Human Functional pAC50 = 5.3 5.3 -1659 10
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
DB00484 722 None 63 Human Functional pAC50 = 5.3 5.3 -1659 10
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
135398744 68684 None 51 Human Functional pAC50 = 4.3 4.3 -151 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 474 7 1 8 1.6 CCCc1nn(C)c2c(=O)[nH]c(-c3cc(S(=O)(=O)N4CCN(C)CC4)ccc3OCC)nc12 10.1038/s41467-023-40064-9
CHEMBL192 68684 None 51 Human Functional pAC50 = 4.3 4.3 -151 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 474 7 1 8 1.6 CCCc1nn(C)c2c(=O)[nH]c(-c3cc(S(=O)(=O)N4CCN(C)CC4)ccc3OCC)nc12 10.1038/s41467-023-40064-9
2540 4402 None 68 Human Functional pAC50 = 5.3 5.3 -741 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 -741 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
228 445 None 20 Human Functional pAC50 = 5.3 5.3 -1412 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
33 445 None 20 Human Functional pAC50 = 5.3 5.3 -1412 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005 445 None 20 Human Functional pAC50 = 5.3 5.3 -1412 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005.0 445 None 20 Human Functional pAC50 = 5.3 5.3 -1412 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
CHEMBL53 445 None 20 Human Functional pAC50 = 5.3 5.3 -1412 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
DB00714 445 None 20 Human Functional pAC50 = 5.3 5.3 -1412 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
1343 1889 None 43 Human Functional pAC50 = 5.3 5.3 -616 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.3 5.3 -616 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.3 5.3 -616 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.3 5.3 -616 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.3 5.3 -616 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.3 5.3 -616 12
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2419 3463 None 53 Human Functional pAC50 = 5.3 5.3 -9549 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
5152 3463 None 53 Human Functional pAC50 = 5.3 5.3 -9549 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
5152.0 3463 None 53 Human Functional pAC50 = 5.3 5.3 -9549 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
559 3463 None 53 Human Functional pAC50 = 5.3 5.3 -9549 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL1263 3463 None 53 Human Functional pAC50 = 5.3 5.3 -9549 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
DB00938 3463 None 53 Human Functional pAC50 = 5.3 5.3 -9549 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
3294 2006 None 61 Human Functional pAC50 = 7.3 7.3 -81 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.3 7.3 -81 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.3 7.3 -81 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.3 7.3 -81 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.3 7.3 -81 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 7.3 7.3 -81 23
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
82153 43915 None 34 Human Functional pAC50 = 6.3 6.3 -11 3
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 434 2 2 6 2.3 CC1(C)O[C@@H]2C[C@H]3[C@@H]4C[C@H](F)C5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@]2(C(=O)CO)O1 10.1038/s41467-023-40064-9
CHEMBL1512 43915 None 34 Human Functional pAC50 = 6.3 6.3 -11 3
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 434 2 2 6 2.3 CC1(C)O[C@@H]2C[C@H]3[C@@H]4C[C@H](F)C5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@]2(C(=O)CO)O1 10.1038/s41467-023-40064-9
4659569 22338 None 65 Human Functional pAC50 = 5.3 5.3 -4 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 273 3 2 5 2.5 Cc1ccc(C(=O)c2cc(O)c(O)c([N+](=O)[O-])c2)cc1 10.1038/s41467-023-40064-9
CHEMBL1324 22338 None 65 Human Functional pAC50 = 5.3 5.3 -4 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 273 3 2 5 2.5 Cc1ccc(C(=O)c2cc(O)c(O)c([N+](=O)[O-])c2)cc1 10.1038/s41467-023-40064-9
5991 206377 None 46 Human Functional pAC50 = 5.2 5.2 2 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL691 206377 None 46 Human Functional pAC50 = 5.2 5.2 2 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 296 0 2 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCc4cc(O)ccc4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
45138674 16653 None 45 Human Functional pAC50 = 5.2 5.2 -3 6
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.2 5.2 -3 6
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2551 794 None 13 Human Functional pAC50 = 5.2 5.2 -56 13
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
2551.0 794 None 13 Human Functional pAC50 = 5.2 5.2 -56 13
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
298 794 None 13 Human Functional pAC50 = 5.2 5.2 -56 13
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
488 794 None 13 Human Functional pAC50 = 5.2 5.2 -56 13
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
CHEMBL965 794 None 13 Human Functional pAC50 = 5.2 5.2 -56 13
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
DB00411 794 None 13 Human Functional pAC50 = 5.2 5.2 -56 13
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 147 3 1 2 -0.2 NC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
180 401 None 38 Human Functional pAC50 = 5.2 5.2 -4265 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.2 5.2 -4265 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.2 5.2 -4265 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.2 5.2 -4265 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.2 5.2 -4265 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.2 5.2 -4265 38
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
71731823 111768 None 45 Human Functional pAC50 = 5.2 5.2 -5 3
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 0 1 7 2.8 C[C@H]1Oc2cc(cnc2N)-c2c(nn(C)c2C#N)CN(C)C(=O)c2ccc(F)cc21 10.1038/s41467-023-40064-9
CHEMBL3286830 111768 None 45 Human Functional pAC50 = 5.2 5.2 -5 3
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 406 0 1 7 2.8 C[C@H]1Oc2cc(cnc2N)-c2c(nn(C)c2C#N)CN(C)C(=O)c2ccc(F)cc21 10.1038/s41467-023-40064-9
213046 2385 None 44 Human Functional pAC50 = 7.2 7.2 -2 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
213046.0 2385 None 44 Human Functional pAC50 = 7.2 7.2 -2 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 2385 None 44 Human Functional pAC50 = 7.2 7.2 -2 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 2385 None 44 Human Functional pAC50 = 7.2 7.2 -2 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 2385 None 44 Human Functional pAC50 = 7.2 7.2 -2 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 2385 None 44 Human Functional pAC50 = 7.2 7.2 -2 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
5311507 194927 None 32 Human Functional pAC50 = 5.2 5.2 -562 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.2 5.2 -562 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.2 5.2 -562 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.2 5.2 -562 12
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
12574 2605 None 60 Human Functional pAC50 = 5.2 5.2 -104 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
4810 2605 None 60 Human Functional pAC50 = 5.2 5.2 -104 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
4810.0 2605 None 60 Human Functional pAC50 = 5.2 5.2 -104 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
CHEMBL19236 2605 None 60 Human Functional pAC50 = 5.2 5.2 -104 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
DB09242 2605 None 60 Human Functional pAC50 = 5.2 5.2 -104 8
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
2407 3372 None 50 Human Functional pAC50 = 6.2 6.2 -204 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.2 6.2 -204 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.2 6.2 -204 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.2 6.2 -204 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.2 6.2 -204 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.2 6.2 -204 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2470 3653 None 40 Human Functional pAC50 = 5.2 5.2 -3388 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.2 5.2 -3388 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.2 5.2 -3388 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.2 5.2 -3388 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.2 5.2 -3388 23
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
5591 157623 None 57 Human Functional pAC50 = 5.2 5.2 -8 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.2 5.2 -8 17
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
17676 7074 None 25 Human Functional pAC50 = 8.2 8.2 -1 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 8.2 8.2 -1 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 8.2 8.2 -1 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 8.2 8.2 -1 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 8.2 8.2 -1 13
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
214 3860 None 43 Human Functional pAC50 = 5.2 5.2 -776 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3860 None 43 Human Functional pAC50 = 5.2 5.2 -776 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3860 None 43 Human Functional pAC50 = 5.2 5.2 -776 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566.0 3860 None 43 Human Functional pAC50 = 5.2 5.2 -776 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3860 None 43 Human Functional pAC50 = 5.2 5.2 -776 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3860 None 43 Human Functional pAC50 = 5.2 5.2 -776 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3860 None 43 Human Functional pAC50 = 5.2 5.2 -776 28
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
71496458 115628 None 61 Human Functional pAC50 = 6.2 6.2 -1 16
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 499 10 2 8 4.5 C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)C 10.1038/s41467-023-40064-9
CHEMBL3353410 115628 None 61 Human Functional pAC50 = 6.2 6.2 -1 16
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
5803 162321 None 58 Human Functional pAC50 = 5.2 5.2 -1 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 622 4 2 3 4.6 O=C(O)Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1 10.1038/s41467-023-40064-9
CHEMBL41632 162321 None 58 Human Functional pAC50 = 5.2 5.2 -1 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
3151 1462 None 65 Human Functional pAC50 = 5.1 5.1 -2691 24
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3151.0 1462 None 65 Human Functional pAC50 = 5.1 5.1 -2691 24
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
945 1462 None 65 Human Functional pAC50 = 5.1 5.1 -2691 24
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
965 1462 None 65 Human Functional pAC50 = 5.1 5.1 -2691 24
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL219916 1462 None 65 Human Functional pAC50 = 5.1 5.1 -2691 24
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01184 1462 None 65 Human Functional pAC50 = 5.1 5.1 -2691 24
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2142 3096 None 36 Human Functional pAC50 = 5.1 5.1 -891 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -891 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -891 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -891 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -891 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -891 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -891 18
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
1971 2866 None 32 Human Functional pAC50 = 5.1 5.1 -10964 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -10964 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -10964 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -10964 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -10964 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -10964 32
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
8730 198347 None 44 Human Functional pAC50 = 5.1 5.1 -1 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 777 5 3 4 4.6 N[C@H](Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
90657408 198347 None 44 Human Functional pAC50 = 5.1 5.1 -1 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 777 5 3 4 4.6 N[C@H](Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL559 198347 None 44 Human Functional pAC50 = 5.1 5.1 -1 5
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 777 5 3 4 4.6 N[C@H](Cc1cc(I)c(Oc2cc(I)c(O)c(I)c2)c(I)c1)C(=O)O 10.1038/s41467-023-40064-9
2713 207729 None 57 Human Functional pAC50 = 5.1 5.1 -16 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -16 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -16 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -16 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -16 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -16 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 5.1 5.1 -16 27
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
135409453 3773 None 26 Human Functional pAC50 = 6.1 6.1 -61 35
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3773 None 26 Human Functional pAC50 = 6.1 6.1 -61 35
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3773 None 26 Human Functional pAC50 = 6.1 6.1 -61 35
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
2583 208352 None 32 Human Functional pAC50 = 5.1 5.1 -8709 4
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 292 5 3 4 1.7 CC(C)(C)NCC(O)COc1cccc2c1CCC(=O)N2 10.1038/s41467-023-40064-9
2583.0 208352 None 32 Human Functional pAC50 = 5.1 5.1 -8709 4
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 292 5 3 4 1.7 CC(C)(C)NCC(O)COc1cccc2c1CCC(=O)N2 10.1038/s41467-023-40064-9
CHEMBL839 208352 None 32 Human Functional pAC50 = 5.1 5.1 -8709 4
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 292 5 3 4 1.7 CC(C)(C)NCC(O)COc1cccc2c1CCC(=O)N2 10.1038/s41467-023-40064-9
DB00521 208352 None 32 Human Functional pAC50 = 5.1 5.1 -8709 4
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 292 5 3 4 1.7 CC(C)(C)NCC(O)COc1cccc2c1CCC(=O)N2 10.1038/s41467-023-40064-9
202 1508 None 46 Human Functional pAC50 = 5.1 5.1 -6 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.1 5.1 -6 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.1 5.1 -6 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.1 5.1 -6 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.1 5.1 -6 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
124 2981 None 32 Human Functional pAC50 = 8.0 8.0 -12 24
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 8.0 8.0 -12 24
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 8.0 8.0 -12 24
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 8.0 8.0 -12 24
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 8.0 8.0 -12 24
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 8.0 8.0 -12 24
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
3036780 107587 None 16 Human Functional pAC50 = 8.0 8.0 -48 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
3036780.0 107587 None 16 Human Functional pAC50 = 8.0 8.0 -48 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
46780481 107587 None 16 Human Functional pAC50 = 8.0 8.0 -48 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 107587 None 16 Human Functional pAC50 = 8.0 8.0 -48 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970.0 107587 None 16 Human Functional pAC50 = 8.0 8.0 -48 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 107587 None 16 Human Functional pAC50 = 8.0 8.0 -48 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 107587 None 16 Human Functional pAC50 = 8.0 8.0 -48 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL504548 107587 None 16 Human Functional pAC50 = 8.0 8.0 -48 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
DB06216 107587 None 16 Human Functional pAC50 = 8.0 8.0 -48 15
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
4746 207349 None 24 Human Functional pAC50 = 5.0 5.0 -8 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.0 5.0 -8 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 = 5.0 5.0 -8 19
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
71927 78434 None 13 Human Functional pAC50 = 5.0 5.0 2 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 202 2 1 3 0.9 COc1cc(N)cn[n+]1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL2106667 78434 None 13 Human Functional pAC50 = 5.0 5.0 2 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 202 2 1 3 0.9 COc1cc(N)cn[n+]1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL2110922 78434 None 13 Human Functional pAC50 = 5.0 5.0 2 2
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 202 2 1 3 0.9 COc1cc(N)cn[n+]1-c1ccccc1 10.1038/s41467-023-40064-9
4046 2483 None 21 Human Functional pAC50 = 5.0 5.0 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2176 3127 None 40 Human Functional pAC50 = 7.0 7.0 -33 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1038/s41467-023-40064-9
4828 3127 None 40 Human Functional pAC50 = 7.0 7.0 -33 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1038/s41467-023-40064-9
4828.0 3127 None 40 Human Functional pAC50 = 7.0 7.0 -33 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1038/s41467-023-40064-9
91 3127 None 40 Human Functional pAC50 = 7.0 7.0 -33 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL500 3127 None 40 Human Functional pAC50 = 7.0 7.0 -33 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1038/s41467-023-40064-9
DB00960 3127 None 40 Human Functional pAC50 = 7.0 7.0 -33 8
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1038/s41467-023-40064-9
2303 3187 None 44 Human Functional pAC50 = 6.0 6.0 -346 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
4946 3187 None 44 Human Functional pAC50 = 6.0 6.0 -346 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
564 3187 None 44 Human Functional pAC50 = 6.0 6.0 -346 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
63 3187 None 44 Human Functional pAC50 = 6.0 6.0 -346 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
91536 3187 None 44 Human Functional pAC50 = 6.0 6.0 -346 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL27 3187 None 44 Human Functional pAC50 = 6.0 6.0 -346 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL452861 3187 None 44 Human Functional pAC50 = 6.0 6.0 -346 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
DB00571 3187 None 44 Human Functional pAC50 = 6.0 6.0 -346 20
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1038/s41467-023-40064-9
4046 2483 None 21 Human Functional pAC50 = 5.0 5.0 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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 -20 17
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
2865 4143 None 47 Human Functional pAC50 = 6.0 6.0 -8 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 4143 None 47 Human Functional pAC50 = 6.0 6.0 -8 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 4143 None 47 Human Functional pAC50 = 6.0 6.0 -8 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854.0 4143 None 47 Human Functional pAC50 = 6.0 6.0 -8 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 4143 None 47 Human Functional pAC50 = 6.0 6.0 -8 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate reader
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 4143 None 47 Human Functional pAC50 = 6.0 6.0 -8 20
Agonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAgonist activity at human HTR1A 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
1353 1911 None 63 Human Functional pAC50 = 6.0 6.0 -457 39
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.0 6.0 -457 39
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.0 6.0 -457 39
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.0 6.0 -457 39
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.0 6.0 -457 39
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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 = 6.0 6.0 -457 39
Antagonist activity at human HTR1A in an in vitro cell-based assay measured by fluorescent imaging plate readerAntagonist activity at human HTR1A 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
10324985 76809 None 6 Human Functional pEC50 = 11 11.0 - 1
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulationAgonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76809 None 6 Human Functional pEC50 = 11 11.0 - 1
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulationAgonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76809 None 6 Human Functional pEC50 = 11 11.0 - 1
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulationAgonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
132257058 181015 None 0 Human Functional pEC50 = 10.9 10.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 449 7 2 4 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3c2CCN3)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4757755 181015 None 0 Human Functional pEC50 = 10.9 10.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 449 7 2 4 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3c2CCN3)CC1 10.1021/acs.jmedchem.0c00814
132247312 180761 None 0 Human Functional pEC50 = 10.9 10.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4755058 180761 None 0 Human Functional pEC50 = 10.9 10.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
24804775 19350 None 0 Human Functional pEC50 = 10.5 10.5 31 2
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 412 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290716 19350 None 0 Human Functional pEC50 = 10.5 10.5 31 2
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 412 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
10324985 76809 None 6 Human Functional pEC50 = 10.3 10.3 - 1
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76809 None 6 Human Functional pEC50 = 10.3 10.3 - 1
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76809 None 6 Human Functional pEC50 = 10.3 10.3 - 1
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
132247307 180516 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 481 8 2 4 4.6 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4752177 180516 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 481 8 2 4 4.6 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
89638711 114346 None 6 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
ChEMBL 344 6 0 8 -0.1 Cn1c(=O)cnn(CCCCN2CCN(c3ccccn3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
CHEMBL3330612 114346 None 6 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
ChEMBL 344 6 0 8 -0.1 Cn1c(=O)cnn(CCCCN2CCN(c3ccccn3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
132247301 180875 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4756233 180875 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1 10.1021/acs.jmedchem.0c00814
156010510 177209 None 0 Human Functional pEC50 = 10 10.0 70 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 426 6 0 8 2.8 O=c1n(CCCCN2CCN(c3cccc4scnc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
CHEMBL4633397 177209 None 0 Human Functional pEC50 = 10 10.0 70 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 426 6 0 8 2.8 O=c1n(CCCCN2CCN(c3cccc4scnc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
156020913 178141 None 0 Human Functional pEC50 = 10 10.0 263 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 425 6 0 7 3.5 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccc(F)cn12 10.1016/j.bmcl.2020.127027
CHEMBL4647011 178141 None 0 Human Functional pEC50 = 10 10.0 263 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 425 6 0 7 3.5 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccc(F)cn12 10.1016/j.bmcl.2020.127027
156021409 178216 None 0 Human Functional pEC50 = 10 10.0 4073 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 475 6 0 7 4.6 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Cl)cc(Cl)cn12 10.1016/j.bmcl.2020.127027
CHEMBL4648027 178216 None 0 Human Functional pEC50 = 10 10.0 4073 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 475 6 0 7 4.6 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Cl)cc(Cl)cn12 10.1016/j.bmcl.2020.127027
21830793 91869 None 12 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmcl.2014.07.048
CHEMBL2413154 91869 None 12 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmcl.2014.07.048
21830793 91869 None 12 Human Functional pEC50 = 10 10.0 - 1
Partial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS bindingPartial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS binding
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91869 None 12 Human Functional pEC50 = 10 10.0 - 1
Partial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS bindingPartial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS binding
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
132256760 183350 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 437 8 2 4 4.1 CNc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4796345 183350 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 437 8 2 4 4.1 CNc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
4223 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
6918314 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
6918314.0 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
7427 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
CHEMBL439849 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
DB06684 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2018.04.037
4223 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
6918314 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
6918314.0 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
7427 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
CHEMBL439849 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
DB06684 3992 None 57 Human Functional pEC50 = 9.9 9.9 7 17
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.bmc.2019.01.025
18922713 98551 None 0 Human Functional pEC50 = 9.9 9.9 - 1
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 10.1021/jm000339w
CHEMBL276031 98551 None 0 Human Functional pEC50 = 9.9 9.9 - 1
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 10.1021/jm000339w
132256714 180490 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4751777 180490 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
71294258 114350 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
ChEMBL 362 6 0 8 0.1 Cn1c(=O)cnn(CCCCN2CCN(c3cccc(F)n3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
CHEMBL3330616 114350 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
ChEMBL 362 6 0 8 0.1 Cn1c(=O)cnn(CCCCN2CCN(c3cccc(F)n3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
1809 134 None 25 Human Functional pEC50 = 9.6 9.6 12 8
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2023.115285
4 134 None 25 Human Functional pEC50 = 9.6 9.6 12 8
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2023.115285
CHEMBL18840 134 None 25 Human Functional pEC50 = 9.6 9.6 12 8
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2023.115285
1809 134 None 25 Human Functional pEC50 = 9.6 9.6 12 8
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2023.115285
4 134 None 25 Human Functional pEC50 = 9.6 9.6 12 8
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2023.115285
CHEMBL18840 134 None 25 Human Functional pEC50 = 9.6 9.6 12 8
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1016/j.ejmech.2023.115285
11948707 166262 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cellsAgonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
CHEMBL426317 166262 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cellsAgonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
89638708 114337 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
ChEMBL 343 6 0 7 0.5 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
CHEMBL3330603 114337 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
ChEMBL 343 6 0 7 0.5 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3)CC2)c1=O 10.1016/j.bmcl.2014.07.048
132256714 180490 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4751777 180490 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 438 8 1 4 4.1 COc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
132256724 180853 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4756041 180853 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.0c00814
11382841 18428 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 360 9 2 3 4.1 COc1ccc(F)cc1OCCNCCCc1c[nH]c2ccc(F)cc12 10.1021/jm0304010
CHEMBL127171 18428 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 360 9 2 3 4.1 COc1ccc(F)cc1OCCNCCCc1c[nH]c2ccc(F)cc12 10.1021/jm0304010
145961968 161606 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 531 6 2 4 6.1 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(Br)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
CHEMBL4128200 161606 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 531 6 2 4 6.1 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(Br)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
145960843 161500 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4126644 161500 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
5 139 None 45 Human Functional pEC50 = 9.3 9.3 -33 26
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
5202 139 None 45 Human Functional pEC50 = 9.3 9.3 -33 26
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
CHEMBL39 139 None 45 Human Functional pEC50 = 9.3 9.3 -33 26
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
DB08839 139 None 45 Human Functional pEC50 = 9.3 9.3 -33 26
Agonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S bindingAgonistic activity at human 5HT1A receptor by [35S]GTP-gamma-S binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
162646896 179678 None 0 Human Functional pEC50 = 9.3 9.3 3 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 421 6 0 5 4.2 O=C1COc2ccccc2N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2020.112572
CHEMBL4741908 179678 None 0 Human Functional pEC50 = 9.3 9.3 3 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 421 6 0 5 4.2 O=C1COc2ccccc2N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2020.112572
145961773 161643 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 464 6 2 5 4.8 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4128689 161643 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 464 6 2 5 4.8 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
145962474 161741 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 467 6 2 4 5.6 Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4130230 161741 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 467 6 2 4 5.6 Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
73346042 91868 None 6 Human Functional pEC50 = 9.2 9.2 - 1
Partial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS bindingPartial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS binding
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91868 None 6 Human Functional pEC50 = 9.2 9.2 - 1
Partial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS bindingPartial agonist activity at human 5HT1A receptor expressed in CHO cells assessed as increase in [35S]GTPgammaS binding
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
132247308 181867 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 451 8 2 4 3.2 NC(=O)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4777581 181867 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 451 8 2 4 3.2 NC(=O)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
5 139 None 45 Human Functional pEC50 = 9.2 9.2 -33 26
Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cellsAgonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.01.052
5202 139 None 45 Human Functional pEC50 = 9.2 9.2 -33 26
Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cellsAgonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.01.052
CHEMBL39 139 None 45 Human Functional pEC50 = 9.2 9.2 -33 26
Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cellsAgonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.01.052
DB08839 139 None 45 Human Functional pEC50 = 9.2 9.2 -33 26
Agonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cellsAgonist activity assessed by stimulation of [35S]GTP-gamma-S binding to human 5HT1A receptor expressed in CHO cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2006.01.052
145974939 164792 None 0 Human Functional pEC50 = 9.2 9.2 11 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 442 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sc(F)cc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4217182 164792 None 0 Human Functional pEC50 = 9.2 9.2 11 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 442 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sc(F)cc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
145963079 161672 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 471 6 2 4 5.5 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(F)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
CHEMBL4129170 161672 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 471 6 2 4 5.5 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(F)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
10694660 178488 None 0 Human Functional pEC50 = 9.1 9.1 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 445 6 2 4 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cc[nH]n3)n2)CC1 10.1021/jm9806906
CHEMBL46539 178488 None 0 Human Functional pEC50 = 9.1 9.1 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 445 6 2 4 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cc[nH]n3)n2)CC1 10.1021/jm9806906
145962581 161572 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 487 6 2 4 6.0 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(Cl)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
CHEMBL4127774 161572 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 487 6 2 4 6.0 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(Cl)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
10474042 170356 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 365 6 0 4 4.1 COc1cccc2c1CCCC2CCCN1CCN(c2ccccn2)CC1 10.1016/j.bmc.2015.05.042
CHEMBL444590 170356 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 365 6 0 4 4.1 COc1cccc2c1CCCC2CCCN1CCN(c2ccccn2)CC1 10.1016/j.bmc.2015.05.042
44336170 107320 None 0 Human Functional pEC50 = 9.1 9.1 - 1
In vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMPIn vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMP
ChEMBL 413 5 1 5 2.9 CC1CN(c2cccc3c2OCCO3)CC(C)N1CCNC(=O)c1ccc(F)cc1 10.1021/jm960496o
CHEMBL316960 107320 None 0 Human Functional pEC50 = 9.1 9.1 - 1
In vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMPIn vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMP
ChEMBL 413 5 1 5 2.9 CC1CN(c2cccc3c2OCCO3)CC(C)N1CCNC(=O)c1ccc(F)cc1 10.1021/jm960496o
10430183 208086 None 0 Human Functional pEC50 = 9.1 9.1 - 1
In vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMPIn vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMP
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/jm960496o
CHEMBL81728 208086 None 0 Human Functional pEC50 = 9.1 9.1 - 1
In vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMPIn vitro potency at human 5-hydroxytryptamine 1A receptor in inhibiting forskolin-stimulated accumulation of intracellular cAMP
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/jm960496o
4223 3992 None 57 Human Functional pEC50 = 9.1 9.1 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.ejmech.2021.114045
6918314 3992 None 57 Human Functional pEC50 = 9.1 9.1 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.ejmech.2021.114045
6918314.0 3992 None 57 Human Functional pEC50 = 9.1 9.1 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.ejmech.2021.114045
7427 3992 None 57 Human Functional pEC50 = 9.1 9.1 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.ejmech.2021.114045
CHEMBL439849 3992 None 57 Human Functional pEC50 = 9.1 9.1 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.ejmech.2021.114045
DB06684 3992 None 57 Human Functional pEC50 = 9.1 9.1 7 17
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1016/j.ejmech.2021.114045
162652355 180472 None 0 Human Functional pEC50 = 9.1 9.1 3 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 470 6 1 6 3.8 Nc1ccc2c(c1)N(CCCCN1CCN(c3cccc4sccc34)CC1)S(=O)(=O)CC2 10.1016/j.ejmech.2020.112572
CHEMBL4751542 180472 None 0 Human Functional pEC50 = 9.1 9.1 3 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 470 6 1 6 3.8 Nc1ccc2c(c1)N(CCCCN1CCN(c3cccc4sccc34)CC1)S(=O)(=O)CC2 10.1016/j.ejmech.2020.112572
10020855 189379 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 351 4 0 4 3.9 COc1cccc([C@H]2CC[C@H](N3CCN(c4ccccn4)CC3)CC2)c1 10.1016/j.bmc.2015.05.042
CHEMBL511857 189379 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 351 4 0 4 3.9 COc1cccc([C@H]2CC[C@H](N3CCN(c4ccccn4)CC3)CC2)c1 10.1016/j.bmc.2015.05.042
118713100 114348 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
ChEMBL 362 6 0 8 0.1 Cn1c(=O)cnn(CCCCN2CCN(c3ncccc3F)CC2)c1=O 10.1016/j.bmcl.2014.07.048
CHEMBL3330614 114348 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometryAgonist activity at human 5HT1AR expressed in CHO cells assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry
ChEMBL 362 6 0 8 0.1 Cn1c(=O)cnn(CCCCN2CCN(c3ncccc3F)CC2)c1=O 10.1016/j.bmcl.2014.07.048
10430183 208086 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL81728 208086 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
145993172 167092 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 423 6 0 5 3.8 O=C1C2CC=CCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4287980 167092 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 423 6 0 5 3.8 O=C1C2CC=CCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
145971556 164593 None 0 Human Functional pEC50 = 9.1 9.1 29 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 436 8 1 5 3.7 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4214528 164593 None 0 Human Functional pEC50 = 9.1 9.1 29 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 436 8 1 5 3.7 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccn1 10.1016/j.bmcl.2018.01.038
10082834 34490 None 1 Human Functional pEC50 = 9.0 9.0 - 1
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 236 4 1 2 2.4 COc1ccc2[nH]cc(CCN(C)C)c2c1F 10.1021/jm000339w
CHEMBL142862 34490 None 1 Human Functional pEC50 = 9.0 9.0 - 1
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 236 4 1 2 2.4 COc1ccc2[nH]cc(CCN(C)C)c2c1F 10.1021/jm000339w
10430183 208086 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL81728 208086 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
5 139 None 45 Human Functional pEC50 = 9 9.0 -33 26
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulationAgonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
5202 139 None 45 Human Functional pEC50 = 9 9.0 -33 26
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulationAgonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
CHEMBL39 139 None 45 Human Functional pEC50 = 9 9.0 -33 26
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulationAgonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
DB08839 139 None 45 Human Functional pEC50 = 9 9.0 -33 26
Agonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulationAgonistic activity at human 5HT1A in CHO cells by the inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm050725j
138692457 182539 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 438 8 1 4 4.1 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4786067 182539 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 438 8 1 4 4.1 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
145991127 167026 None 0 Human Functional pEC50 = 9.0 9.0 34 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 437 6 0 5 4.2 O=C1c2cccc(F)c2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4286905 167026 None 0 Human Functional pEC50 = 9.0 9.0 34 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 437 6 0 5 4.2 O=C1c2cccc(F)c2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
162658259 181139 None 0 Human Functional pEC50 = 9.0 9.0 16 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 471 6 1 6 3.9 O=S1(=O)CCc2ccc(O)cc2N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2020.112572
CHEMBL4759331 181139 None 0 Human Functional pEC50 = 9.0 9.0 16 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 471 6 1 6 3.9 O=S1(=O)CCc2ccc(O)cc2N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2020.112572
10813901 178504 None 0 Human Functional pEC50 = 9.0 9.0 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 461 6 2 4 4.5 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cc[nH]n3)n2)CC1 10.1021/jm9806906
CHEMBL46582 178504 None 0 Human Functional pEC50 = 9.0 9.0 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 461 6 2 4 4.5 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cc[nH]n3)n2)CC1 10.1021/jm9806906
145993577 167482 None 0 Human Functional pEC50 = 8.9 8.9 9 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 453 6 0 5 4.9 O=C1CC2(CCCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4295055 167482 None 0 Human Functional pEC50 = 8.9 8.9 9 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 453 6 0 5 4.9 O=C1CC2(CCCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
156014350 177316 None 0 Human Functional pEC50 = 8.9 8.9 22 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 443 6 0 7 3.6 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(F)cc(F)cn12 10.1016/j.bmcl.2020.127027
CHEMBL4635414 177316 None 0 Human Functional pEC50 = 8.9 8.9 22 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 443 6 0 7 3.6 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(F)cc(F)cn12 10.1016/j.bmcl.2020.127027
145952639 161512 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 453 6 2 4 5.3 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccccc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
CHEMBL4126818 161512 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 453 6 2 4 5.3 Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccccc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
21689040 41983 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human 5-HT1AR expressed in HEK293 cells assessed as increase in calcium flux by fluorimetric methodAgonist activity at human 5-HT1AR expressed in HEK293 cells assessed as increase in calcium flux by fluorimetric method
ChEMBL 261 6 1 2 3.8 CCCCN(CCC)C1CCc2cccc(O)c2C1 10.1016/j.ejmech.2018.01.002
CHEMBL149482 41983 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human 5-HT1AR expressed in HEK293 cells assessed as increase in calcium flux by fluorimetric methodAgonist activity at human 5-HT1AR expressed in HEK293 cells assessed as increase in calcium flux by fluorimetric method
ChEMBL 261 6 1 2 3.8 CCCCN(CCC)C1CCc2cccc(O)c2C1 10.1016/j.ejmech.2018.01.002
145966333 164155 None 0 Human Functional pEC50 = 8.9 8.9 19 6
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4209188 164155 None 0 Human Functional pEC50 = 8.9 8.9 19 6
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
145993117 167017 None 0 Human Functional pEC50 = 8.9 8.9 8 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
CHEMBL4286717 167017 None 0 Human Functional pEC50 = 8.9 8.9 8 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
11046644 30712 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 361 6 0 4 4.0 COc1cccc2c(CCCN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2015.05.042
CHEMBL139505 30712 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 361 6 0 4 4.0 COc1cccc2c(CCCN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2015.05.042
10047814 104920 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 421 6 0 6 2.7 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
CHEMBL311015 104920 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 421 6 0 6 2.7 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
156011408 177516 None 0 Human Functional pEC50 = 8.9 8.9 1 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 432 6 0 8 3.2 N#Cc1cccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc12 10.1016/j.bmcl.2020.127027
CHEMBL4638430 177516 None 0 Human Functional pEC50 = 8.9 8.9 1 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 432 6 0 8 3.2 N#Cc1cccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc12 10.1016/j.bmcl.2020.127027
9798593 112899 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 352 8 3 3 3.8 Fc1ccc2[nH]cc(CCCNCCOc3cccc4[nH]cnc34)c2c1 10.1021/jm0304010
CHEMBL330827 112899 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 352 8 3 3 3.8 Fc1ccc2[nH]cc(CCCNCCOc3cccc4[nH]cnc34)c2c1 10.1021/jm0304010
9822317 69218 None 2 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 400 7 1 5 2.6 O=C1c2ccccc2S(=O)(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926761 69218 None 2 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 400 7 1 5 2.6 O=C1c2ccccc2S(=O)(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
156021344 178274 None 0 Human Functional pEC50 = 8.8 8.8 7 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 443 6 0 7 3.6 O=c1n(CCCCN2CCN(c3cccc4sc(F)cc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
CHEMBL4649106 178274 None 0 Human Functional pEC50 = 8.8 8.8 7 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 443 6 0 7 3.6 O=c1n(CCCCN2CCN(c3cccc4sc(F)cc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
145963146 161431 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5c(N)c6c(nc45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4125762 161431 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5c(N)c6c(nc45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
10949698 207745 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Ability to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptorAbility to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptor
ChEMBL 413 8 1 8 1.9 COc1ccccc1N1CCN(CCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
CHEMBL79161 207745 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Ability to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptorAbility to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptor
ChEMBL 413 8 1 8 1.9 COc1ccccc1N1CCN(CCCNc2c(C(C)=O)c(C)nn(C)c2=O)CC1 10.1021/jm0009336
145988038 167272 None 0 Human Functional pEC50 = 8.8 8.8 4 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 413 6 0 5 4.0 CC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
CHEMBL4291215 167272 None 0 Human Functional pEC50 = 8.8 8.8 4 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 413 6 0 5 4.0 CC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
11232913 113389 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 334 8 3 3 3.6 c1ccc2c(CCCNCCOc3cccc4[nH]cnc34)c[nH]c2c1 10.1021/jm0304010
CHEMBL331609 113389 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 334 8 3 3 3.6 c1ccc2c(CCCNCCOc3cccc4[nH]cnc34)c[nH]c2c1 10.1021/jm0304010
145990126 166848 None 0 Human Functional pEC50 = 8.8 8.8 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 425 6 0 5 4.0 O=C1C2CCCCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4283546 166848 None 0 Human Functional pEC50 = 8.8 8.8 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 425 6 0 5 4.0 O=C1C2CCCCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
156011945 177532 None 0 Human Functional pEC50 = 8.8 8.8 7 5
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 407 6 0 7 3.3 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccccn12 10.1016/j.bmcl.2020.127027
CHEMBL4638599 177532 None 0 Human Functional pEC50 = 8.8 8.8 7 5
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 407 6 0 7 3.3 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccccn12 10.1016/j.bmcl.2020.127027
156018107 177970 None 0 Human Functional pEC50 = 8.7 8.7 9 6
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 425 6 0 7 3.5 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
CHEMBL4644352 177970 None 0 Human Functional pEC50 = 8.7 8.7 9 6
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 425 6 0 7 3.5 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(F)cccn12 10.1016/j.bmcl.2020.127027
145973003 164629 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
Agonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 450 8 0 7 3.9 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2C(C)=O)CC1 10.1016/j.bmc.2017.12.016
CHEMBL4215022 164629 None 0 Rat Functional pEC50 = 8.7 8.7 - 1
Agonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 450 8 0 7 3.9 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2C(C)=O)CC1 10.1016/j.bmc.2017.12.016
11307899 78899 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
ChEMBL 597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12 10.1021/jm0341204
CHEMBL2112882 78899 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
ChEMBL 597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12 10.1021/jm0341204
10411236 101432 None 0 Human Functional pEC50 = 8.7 8.7 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 444 6 1 5 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cnco3)n2)CC1 10.1021/jm9806906
CHEMBL297138 101432 None 0 Human Functional pEC50 = 8.7 8.7 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 444 6 1 5 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cnco3)n2)CC1 10.1021/jm9806906
5 139 None 45 Human Functional pEC50 = 8 8.0 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
5202 139 None 45 Human Functional pEC50 = 8 8.0 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
CHEMBL39 139 None 45 Human Functional pEC50 = 8 8.0 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
DB08839 139 None 45 Human Functional pEC50 = 8 8.0 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
23625537 86511 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 446 6 1 5 4.3 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2nccc(-c3ccco3)n2)CC1 10.1021/jm070714l
CHEMBL231471 86511 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 446 6 1 5 4.3 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2nccc(-c3ccco3)n2)CC1 10.1021/jm070714l
15980895 202420 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 439 6 2 3 4.0 CCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2c(F)cc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
CHEMBL595055 202420 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 439 6 2 3 4.0 CCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2c(F)cc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
10248159 83185 None 4 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 363 7 1 3 5.1 CC1(C)Cc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
CHEMBL218261 83185 None 4 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 363 7 1 3 5.1 CC1(C)Cc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
5 139 None 45 Human Functional pEC50 = 8 8.0 -33 26
Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
5202 139 None 45 Human Functional pEC50 = 8 8.0 -33 26
Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
CHEMBL39 139 None 45 Human Functional pEC50 = 8 8.0 -33 26
Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
DB08839 139 None 45 Human Functional pEC50 = 8 8.0 -33 26
Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
10549236 166482 None 0 Human Functional pEC50 = 8 8.0 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 404 6 1 4 3.5 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3cccc(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL42766 166482 None 0 Human Functional pEC50 = 8 8.0 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 404 6 1 4 3.5 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3cccc(Cl)c3)CC2)n1 10.1021/jm9806906
5 139 None 45 Rat Functional pEC50 = 8 8.0 -19 26
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00042a003
5202 139 None 45 Rat Functional pEC50 = 8 8.0 -19 26
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00042a003
CHEMBL39 139 None 45 Rat Functional pEC50 = 8 8.0 -19 26
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00042a003
DB08839 139 None 45 Rat Functional pEC50 = 8 8.0 -19 26
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00042a003
42606339 17938 None 0 Human Functional pEC50 = 8 8.0 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1259241 17938 None 0 Human Functional pEC50 = 8 8.0 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
137657949 159643 None 0 Human Functional pEC50 = 8.0 8.0 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 420 4 1 7 3.3 Cc1nc2c(O)cccn2c(=O)c1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.bmc.2017.07.040
CHEMBL4102561 159643 None 0 Human Functional pEC50 = 8.0 8.0 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 420 4 1 7 3.3 Cc1nc2c(O)cccn2c(=O)c1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.bmc.2017.07.040
129186563 161133 None 0 Human Functional pEC50 = 8.0 8.0 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 406 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCC=C2 10.1016/j.bmc.2017.07.040
CHEMBL4074326 161133 None 0 Human Functional pEC50 = 8.0 8.0 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 406 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCC=C2 10.1016/j.bmc.2017.07.040
CHEMBL4116465 161133 None 0 Human Functional pEC50 = 8.0 8.0 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 406 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCC=C2 10.1016/j.bmc.2017.07.040
137653567 158939 None 0 Human Functional pEC50 = 8.0 8.0 -3 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 404 4 0 6 3.6 Cc1nc2ccccn2c(=O)c1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.bmc.2017.07.040
CHEMBL4094825 158939 None 0 Human Functional pEC50 = 8.0 8.0 -3 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 404 4 0 6 3.6 Cc1nc2ccccn2c(=O)c1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.bmc.2017.07.040
145982353 166680 None 0 Human Functional pEC50 = 8.0 8.0 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 457 6 2 7 1.9 O=C1C2CC(O)C(O)CC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4280084 166680 None 0 Human Functional pEC50 = 8.0 8.0 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 457 6 2 7 1.9 O=C1C2CC(O)C(O)CC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
145987942 167157 None 0 Human Functional pEC50 = 8.0 8.0 -4 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 453 6 0 5 3.8 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sc(F)cc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4289238 167157 None 0 Human Functional pEC50 = 8.0 8.0 -4 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 453 6 0 5 3.8 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sc(F)cc23)CC1 10.1016/j.ejmech.2017.12.099
10789756 174093 None 0 Human Functional pEC50 = 8.0 8.0 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 450 6 1 4 4.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(N3CCC3)n2)CC1 10.1021/jm9806906
CHEMBL45423 174093 None 0 Human Functional pEC50 = 8.0 8.0 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 450 6 1 4 4.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(N3CCC3)n2)CC1 10.1021/jm9806906
1220 187 None 44 Human Functional pEC50 = 8.0 8.0 -1 9
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
31 187 None 44 Human Functional pEC50 = 8.0 8.0 -1 9
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
7 187 None 44 Human Functional pEC50 = 8.0 8.0 -1 9
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
CHEMBL56 187 None 44 Human Functional pEC50 = 8.0 8.0 -1 9
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
162643462 181836 None 0 Human Functional pEC50 = 8.0 8.0 3 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 462 6 0 5 3.9 CN1CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)c2ccccc2C1=O 10.1016/j.ejmech.2020.112572
CHEMBL4777098 181836 None 0 Human Functional pEC50 = 8.0 8.0 3 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 462 6 0 5 3.9 CN1CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)c2ccccc2C1=O 10.1016/j.ejmech.2020.112572
5 139 None 45 Human Functional pEC50 = 8.0 8.0 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
5202 139 None 45 Human Functional pEC50 = 8.0 8.0 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
CHEMBL39 139 None 45 Human Functional pEC50 = 8.0 8.0 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
DB08839 139 None 45 Human Functional pEC50 = 8.0 8.0 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
172465729 196945 None 0 Rat Functional pEC50 = 7 7.0 83 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 607 8 0 5 6.1 CC12C(=O)C(C)(C(c3ccccc3)=C1c1ccccc1)C1C(=O)N(CCCCN3CCN(c4ccccc4Cl)CC3)C(=O)C12 10.1016/j.bmc.2023.117518
CHEMBL5435378 196945 None 0 Rat Functional pEC50 = 7 7.0 83 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 607 8 0 5 6.1 CC12C(=O)C(C)(C(c3ccccc3)=C1c1ccccc1)C1C(=O)N(CCCCN3CCN(c4ccccc4Cl)CC3)C(=O)C12 10.1016/j.bmc.2023.117518
132257061 180133 None 0 Human Functional pEC50 = 7 7.0 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4747425 180133 None 0 Human Functional pEC50 = 7 7.0 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c00814
49782389 17876 None 0 Human Functional pEC50 = 7 7.0 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 380 5 2 3 3.6 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc4[nH]ccc4c3)CC2)nc1 10.1021/jm100835q
CHEMBL1259055 17876 None 0 Human Functional pEC50 = 7 7.0 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 380 5 2 3 3.6 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc4[nH]ccc4c3)CC2)nc1 10.1021/jm100835q
15980854 202109 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 465 7 2 3 4.4 O=C1NCCc2cc(F)c3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL592939 202109 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 465 7 2 3 4.4 O=C1NCCc2cc(F)c3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
127051039 140362 None 0 Human Functional pEC50 = 7 7.0 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 449 9 1 4 4.7 CCNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805772 140362 None 0 Human Functional pEC50 = 7 7.0 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 449 9 1 4 4.7 CCNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
132257265 182215 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4781985 182215 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
138692456 182811 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 407 7 2 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4789505 182811 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 407 7 2 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
11288 3418 None 1 Human Functional pEC50 = 6.0 6.0 -56 2
Agonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 454 8 3 4 3.7 CCc1cccc(c1Cl)N1CCN(CC1)C[C@@H](CCNC(=O)c1cc2c([nH]1)cccc2)O 10.1021/acs.jmedchem.9b00607
130431314 3418 None 1 Human Functional pEC50 = 6.0 6.0 -56 2
Agonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 454 8 3 4 3.7 CCc1cccc(c1Cl)N1CCN(CC1)C[C@@H](CCNC(=O)c1cc2c([nH]1)cccc2)O 10.1021/acs.jmedchem.9b00607
CHEMBL4519938 3418 None 1 Human Functional pEC50 = 6.0 6.0 -56 2
Agonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 454 8 3 4 3.7 CCc1cccc(c1Cl)N1CCN(CC1)C[C@@H](CCNC(=O)c1cc2c([nH]1)cccc2)O 10.1021/acs.jmedchem.9b00607
CHEMBL5092918 217884 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6cccc(F)c6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
145987659 167345 None 0 Human Functional pEC50 = 7.0 7.0 -3 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 421 5 0 5 3.2 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4292655 167345 None 0 Human Functional pEC50 = 7.0 7.0 -3 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 421 5 0 5 3.2 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
155547346 173694 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 449 6 1 4 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4c5c(nc6ccccc46)CCC5)CC3)c2c1 10.1016/j.bmc.2019.01.025
CHEMBL4533184 173694 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 449 6 1 4 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4c5c(nc6ccccc46)CCC5)CC3)c2c1 10.1016/j.bmc.2019.01.025
6540428 184970 None 1 Human Functional pEC50 = 6.0 6.0 37 2
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 nan
6540428.0 184970 None 1 Human Functional pEC50 = 6.0 6.0 37 2
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 nan
CHEMBL3989558 184970 None 1 Human Functional pEC50 = 6.0 6.0 37 2
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 nan
CHEMBL485253 184970 None 1 Human Functional pEC50 = 6.0 6.0 37 2
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 nan
DB00247 184970 None 1 Human Functional pEC50 = 6.0 6.0 37 2
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 353 4 2 4 1.9 CCC(CO)NC(=O)[C@@H]1C=C2c3cccc4c3c(cn4C)C[C@H]2N(C)C1 nan
53248159 62009 None 0 Human Functional pEC50 = 6.0 6.0 -4 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
CHEMBL1774384 62009 None 0 Human Functional pEC50 = 6.0 6.0 -4 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
49781933 17929 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 399 5 1 3 4.0 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(C5)C3)C4)CC2)nc1 10.1021/jm100835q
CHEMBL1259209 17929 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 399 5 1 3 4.0 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(C5)C3)C4)CC2)nc1 10.1021/jm100835q
118626142 165915 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Partial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assayPartial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assay
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4248491 165915 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Partial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assayPartial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assay
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
145976732 163605 None 0 Human Functional pEC50 = 8.0 8.0 7 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4sccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
CHEMBL4202443 163605 None 0 Human Functional pEC50 = 8.0 8.0 7 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4sccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
145989183 167326 None 0 Human Functional pEC50 = 7.9 7.9 7 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 473 7 0 5 4.4 Cc1ccc(C23CC2C(=O)N(CCCCN2CCN(c4cccc5sccc45)CC2)C3=O)cc1 10.1016/j.ejmech.2017.12.099
CHEMBL4292254 167326 None 0 Human Functional pEC50 = 7.9 7.9 7 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 473 7 0 5 4.4 Cc1ccc(C23CC2C(=O)N(CCCCN2CCN(c4cccc5sccc45)CC2)C3=O)cc1 10.1016/j.ejmech.2017.12.099
56850665 71529 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 334 7 1 5 2.4 O=C1CSC(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926749 71529 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 334 7 1 5 2.4 O=C1CSC(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962697 71529 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 334 7 1 5 2.4 O=C1CSC(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
10385855 14430 None 0 Human Functional pEC50 = 7.0 7.0 -181 3
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/0960-894X(95)00091-7
CHEMBL120055 14430 None 0 Human Functional pEC50 = 7.0 7.0 -181 3
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/0960-894X(95)00091-7
CHEMBL321818 14430 None 0 Human Functional pEC50 = 7.0 7.0 -181 3
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/0960-894X(95)00091-7
137630811 161204 None 0 Human Functional pEC50 = 6.0 6.0 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1 10.1016/j.bmc.2017.07.040
CHEMBL4082150 161204 None 0 Human Functional pEC50 = 6.0 6.0 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1 10.1016/j.bmc.2017.07.040
CHEMBL4117087 161204 None 0 Human Functional pEC50 = 6.0 6.0 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 504 6 1 7 4.5 Cc1ccc(Sc2ccccc2N2CCN(CCc3c(C)nc4n(c3=O)CCCC4O)CC2)c(C)c1 10.1016/j.bmc.2017.07.040
16109488 84291 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 363 7 1 3 5.1 CC1(C)COc2c(OCCNCc3cccc(C4=CCCC4)c3)cccc21 10.1021/jm061180b
CHEMBL221183 84291 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 363 7 1 3 5.1 CC1(C)COc2c(OCCNCc3cccc(C4=CCCC4)c3)cccc21 10.1021/jm061180b
132257069 181162 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 425 7 1 4 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCSc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4759629 181162 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 425 7 1 4 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCSc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
9928161 75946 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 345 3 2 3 4.1 C1=C(c2c[nH]c3ccccc23)CCN(CC2CNc3ccccc3O2)C1 10.1016/j.bmcl.2005.11.054
CHEMBL205031 75946 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 345 3 2 3 4.1 C1=C(c2c[nH]c3ccccc23)CCN(CC2CNc3ccccc3O2)C1 10.1016/j.bmcl.2005.11.054
45483512 200675 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
ChEMBL 287 3 1 2 4.6 Clc1cccc(Oc2ccccc2C2CCNCC2)c1 10.1016/j.bmcl.2009.10.014
CHEMBL575290 200675 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
ChEMBL 287 3 1 2 4.6 Clc1cccc(Oc2ccccc2C2CCNCC2)c1 10.1016/j.bmcl.2009.10.014
9799764 88375 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4ccc5ncccc5c4C3)c2c1 10.1016/j.bmcl.2007.03.049
CHEMBL234853 88375 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4ccc5ncccc5c4C3)c2c1 10.1016/j.bmcl.2007.03.049
145965041 164350 None 0 Human Functional pEC50 = 6.9 6.9 3 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3ccc4ccsc4c3)CC2)n1 10.1016/j.bmcl.2018.01.038
CHEMBL4211473 164350 None 0 Human Functional pEC50 = 6.9 6.9 3 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3ccc4ccsc4c3)CC2)n1 10.1016/j.bmcl.2018.01.038
130431317 173053 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4517102 173053 None 0 Human Functional pEC50 = 6.9 6.9 1 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
155510732 169623 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay
ChEMBL 430 6 1 1 6.9 Fc1ccc(C2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1 10.1016/j.bmcl.2019.126703
CHEMBL4434876 169623 None 0 Human Functional pEC50 = 5.9 5.9 -1 2
Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay
ChEMBL 430 6 1 1 6.9 Fc1ccc(C2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)c(-c2ccccc2)c1 10.1016/j.bmcl.2019.126703
11667626 102639 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Partial agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAPartial agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 359 10 1 4 2.4 CCc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
CHEMBL2431042 102639 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Partial agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAPartial agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 359 10 1 4 2.4 CCc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
CHEMBL3040827 102639 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Partial agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAPartial agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 359 10 1 4 2.4 CCc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
127049163 140311 None 0 Human Functional pEC50 = 7.9 7.9 -2 2
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 8 1 6 3.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4c3OC(F)(F)O4)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805165 140311 None 0 Human Functional pEC50 = 7.9 7.9 -2 2
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 8 1 6 3.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4c3OC(F)(F)O4)CC2)c1 10.1016/j.bmcl.2016.04.087
42606222 17867 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 347 5 1 4 3.2 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccsc3)CC2)nc1 10.1021/jm100835q
CHEMBL1259033 17867 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 347 5 1 4 3.2 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccsc3)CC2)nc1 10.1021/jm100835q
1220 187 None 44 Human Functional pEC50 = 7.9 7.9 -1 9
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2015.05.042
31 187 None 44 Human Functional pEC50 = 7.9 7.9 -1 9
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2015.05.042
7 187 None 44 Human Functional pEC50 = 7.9 7.9 -1 9
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2015.05.042
CHEMBL56 187 None 44 Human Functional pEC50 = 7.9 7.9 -1 9
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2015.05.042
10719425 100247 None 0 Human Functional pEC50 = 7.9 7.9 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 477 6 1 4 5.9 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cccs3)n2)CC1 10.1021/jm9806906
CHEMBL288244 100247 None 0 Human Functional pEC50 = 7.9 7.9 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 477 6 1 4 5.9 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cccs3)n2)CC1 10.1021/jm9806906
156013716 177385 None 0 Human Functional pEC50 = 7.9 7.9 7 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 441 6 0 7 4.0 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Cl)cccn12 10.1016/j.bmcl.2020.127027
CHEMBL4636321 177385 None 0 Human Functional pEC50 = 7.9 7.9 7 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 441 6 0 7 4.0 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Cl)cccn12 10.1016/j.bmcl.2020.127027
10718220 169414 None 0 Human Functional pEC50 = 7.9 7.9 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 445 6 1 5 3.8 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
CHEMBL44159 169414 None 0 Human Functional pEC50 = 7.9 7.9 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 445 6 1 5 3.8 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
11795765 173706 None 0 Human Functional pEC50 = 7.9 7.9 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 408 6 2 4 3.7 CNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL45334 173706 None 0 Human Functional pEC50 = 7.9 7.9 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 408 6 2 4 3.7 CNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm9806906
44461162 208009 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 413 7 1 5 2.9 O=C(NCCCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL81095 208009 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 413 7 1 5 2.9 O=C(NCCCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
145972513 164601 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 443 8 1 7 3.2 CNC(=O)c1cccc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
CHEMBL4214642 164601 None 0 Human Functional pEC50 = 7.9 7.9 -1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 443 8 1 7 3.2 CNC(=O)c1cccc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)n1 10.1016/j.bmcl.2018.01.038
127048533 140338 None 0 Human Functional pEC50 = 6.9 6.9 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 465 9 1 5 4.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1016/j.bmcl.2016.04.087
CHEMBL3805515 140338 None 0 Human Functional pEC50 = 6.9 6.9 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 465 9 1 5 4.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1016/j.bmcl.2016.04.087
152215 97051 None 42 Human Functional pEC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 212 1 1 1 2.9 CN1CC=C(c2c[nH]c3ccccc23)CC1 nan
CHEMBL26655 97051 None 42 Human Functional pEC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 212 1 1 1 2.9 CN1CC=C(c2c[nH]c3ccccc23)CC1 nan
168281650 191311 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assayAgonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay
ChEMBL 467 6 0 7 3.9 COc1cc2ncnc(N3CCC(CN4CCN(c5ccc(Cl)cc5)CC4)C3)c2cc1OC 10.1016/j.ejmech.2022.114218
CHEMBL5189417 191311 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assayAgonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay
ChEMBL 467 6 0 7 3.9 COc1cc2ncnc(N3CCC(CN4CCN(c5ccc(Cl)cc5)CC4)C3)c2cc1OC 10.1016/j.ejmech.2022.114218
44578448 183020 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
ChEMBL 433 6 1 9 1.8 CCC1=CC2C(=O)N(N)C(SCCCN3CCN(c4ncccn4)CC3)=NC2S1 10.1021/jm800176x
CHEMBL479243 183020 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
ChEMBL 433 6 1 9 1.8 CCC1=CC2C(=O)N(N)C(SCCCN3CCN(c4ncccn4)CC3)=NC2S1 10.1021/jm800176x
127049861 140327 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 435 8 1 4 4.3 CNC(=O)c1ccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmcl.2016.04.087
CHEMBL3805376 140327 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 435 8 1 4 4.3 CNC(=O)c1ccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmcl.2016.04.087
127049516 140390 None 0 Human Functional pEC50 = 6.9 6.9 6 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 449 8 1 4 4.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2016.04.087
CHEMBL3806091 140390 None 0 Human Functional pEC50 = 6.9 6.9 6 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 449 8 1 4 4.6 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2016.04.087
CHEMBL5070726 216730 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc(C(=O)CCC5CCN(Cc6ccccc6)CC5)c4)CC3)c2c1 10.1016/j.ejmech.2021.114045
56850658 71544 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 371 7 1 4 1.6 O=C1C2CCCN2C(=O)CN1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926745 71544 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 371 7 1 4 1.6 O=C1C2CCCN2C(=O)CN1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962804 71544 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 371 7 1 4 1.6 O=C1C2CCCN2C(=O)CN1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL5088314 217642 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None COc1cccc(CN2CCC(CCC(=O)c3ccc(N4CCN(CCCCc5c[nH]c6ccc(C#N)cc56)CC4)cc3)CC2)c1 10.1016/j.ejmech.2021.114045
168295269 192621 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assay
ChEMBL 463 7 0 8 3.3 COc1cccc(N2CCN(CC3CCN(c4ncnc5cc(OC)c(OC)cc45)C3)CC2)c1 10.1016/j.ejmech.2022.114218
CHEMBL5209272 192621 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assay
ChEMBL 463 7 0 8 3.3 COc1cccc(N2CCN(CC3CCN(c4ncnc5cc(OC)c(OC)cc45)C3)CC2)c1 10.1016/j.ejmech.2022.114218
145969406 164924 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAntagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 498 7 0 6 4.7 CC(=O)c1c(OCCCN2CCN(c3ccccc3Br)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.bmc.2017.12.016
CHEMBL4218720 164924 None 0 Rat Functional pEC50 = 6.9 6.9 - 1
Antagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAntagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 498 7 0 6 4.7 CC(=O)c1c(OCCCN2CCN(c3ccccc3Br)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.bmc.2017.12.016
3658 4107 None 38 Human Functional pEC50 = 6.9 6.9 -5 18
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
517 4107 None 38 Human Functional pEC50 = 6.9 6.9 -5 18
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
5709 4107 None 38 Human Functional pEC50 = 6.9 6.9 -5 18
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
5709.0 4107 None 38 Human Functional pEC50 = 6.9 6.9 -5 18
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
CHEMBL312448 4107 None 38 Human Functional pEC50 = 6.9 6.9 -5 18
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
DB06694 4107 None 38 Human Functional pEC50 = 6.9 6.9 -5 18
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C nan
127049863 140339 None 0 Human Functional pEC50 = 7.9 7.9 1 6
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
CHEMBL3805518 140339 None 0 Human Functional pEC50 = 7.9 7.9 1 6
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 443 8 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
127049862 140344 None 0 Human Functional pEC50 = 7.9 7.9 -1 6
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 425 8 1 5 4.4 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805559 140344 None 0 Human Functional pEC50 = 7.9 7.9 -1 6
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 425 8 1 5 4.4 CNC(=O)c1cccc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
11381753 78800 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 324 9 2 3 3.8 COc1ccccc1OCCNCCCc1c[nH]c2ccccc12 10.1021/jm0304010
CHEMBL2112645 78800 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 324 9 2 3 3.8 COc1ccccc1OCCNCCCc1c[nH]c2ccccc12 10.1021/jm0304010
49780599 17910 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 341 5 1 3 3.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccccc3)CC2)nc1 10.1021/jm100835q
CHEMBL1259151 17910 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 341 5 1 3 3.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccccc3)CC2)nc1 10.1021/jm100835q
10812183 100330 None 0 Human Functional pEC50 = 7.9 7.9 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 422 7 2 4 4.0 CCNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL288992 100330 None 0 Human Functional pEC50 = 7.9 7.9 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 422 7 2 4 4.0 CCNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm9806906
145984151 166542 None 0 Human Functional pEC50 = 7.9 7.9 16 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 437 6 0 5 4.2 O=C1c2ccc(F)cc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4277751 166542 None 0 Human Functional pEC50 = 7.9 7.9 16 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 437 6 0 5 4.2 O=C1c2ccc(F)cc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
132256724 180853 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4756041 180853 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 459 7 1 4 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.0c00814
23155650 18668 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 446 6 1 7 2.8 Cc1cc(N2CCN(CCCCc3nc4c(c(=O)n3N)CCCC4)CC2)nc2ccccc12 10.1021/jm1002292
CHEMBL1277007 18668 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 446 6 1 7 2.8 Cc1cc(N2CCN(CCCCc3nc4c(c(=O)n3N)CCCC4)CC2)nc2ccccc12 10.1021/jm1002292
145991746 166947 None 0 Human Functional pEC50 = 7.9 7.9 6 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 407 4 0 5 2.8 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4285479 166947 None 0 Human Functional pEC50 = 7.9 7.9 6 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 407 4 0 5 2.8 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
42606340 17896 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 403 5 1 5 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4sccc4s3)CC2)nc1 10.1021/jm100835q
CHEMBL1259108 17896 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 403 5 1 5 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4sccc4s3)CC2)nc1 10.1021/jm100835q
137635294 156183 None 0 Human Functional pEC50 = 5.9 5.9 -245 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 445 4 0 7 3.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2(F)F 10.1016/j.bmc.2017.07.040
CHEMBL4062992 156183 None 0 Human Functional pEC50 = 5.9 5.9 -245 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 445 4 0 7 3.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2(F)F 10.1016/j.bmc.2017.07.040
2543 3707 None 46 Rat Functional pEC50 = 5.9 5.9 -19 14
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
5358 3707 None 46 Rat Functional pEC50 = 5.9 5.9 -19 14
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
5358.0 3707 None 46 Rat Functional pEC50 = 5.9 5.9 -19 14
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
54 3707 None 46 Rat Functional pEC50 = 5.9 5.9 -19 14
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
CHEMBL128 3707 None 46 Rat Functional pEC50 = 5.9 5.9 -19 14
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
DB00669 3707 None 46 Rat Functional pEC50 = 5.9 5.9 -19 14
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00042a003
132256814 180624 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 454 8 1 4 4.6 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1021/acs.jmedchem.0c00814
CHEMBL4753394 180624 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 454 8 1 4 4.6 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1021/acs.jmedchem.0c00814
53248208 62010 None 0 Human Functional pEC50 = 6.9 6.9 3 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 425 8 1 5 3.7 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm200288r
CHEMBL1774385 62010 None 0 Human Functional pEC50 = 6.9 6.9 3 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 425 8 1 5 3.7 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm200288r
16109510 169409 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 337 7 1 4 4.2 C1=C(c2cccc(CNCCOc3cccc4c3OCO4)c2)CCC1 10.1021/jm061180b
CHEMBL441546 169409 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 337 7 1 4 4.2 C1=C(c2cccc(CNCCOc3cccc4c3OCO4)c2)CCC1 10.1021/jm061180b
9932697 141065 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 435 6 1 4 5.1 CCCN1CC(CN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)Oc2c(OC)cccc21 10.1016/j.bmcl.2005.11.054
CHEMBL382333 141065 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 435 6 1 4 5.1 CCCN1CC(CN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)Oc2c(OC)cccc21 10.1016/j.bmcl.2005.11.054
3246443 37697 None 0 Human Functional pEC50 = 4.9 4.9 -13 3
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL1457510 37697 None 0 Human Functional pEC50 = 4.9 4.9 -13 3
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
127049849 140333 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 477 9 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(C(C)=O)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805434 140333 None 0 Human Functional pEC50 = 6.9 6.9 -3 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 477 9 1 5 4.5 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(C(C)=O)c1 10.1016/j.bmcl.2016.04.087
45375938 200492 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
ChEMBL 289 3 1 2 4.2 Fc1cccc(Oc2cccc(F)c2C2CCNCC2)c1 10.1016/j.bmcl.2009.10.014
CHEMBL574004 200492 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
ChEMBL 289 3 1 2 4.2 Fc1cccc(Oc2cccc(F)c2C2CCNCC2)c1 10.1016/j.bmcl.2009.10.014
44591228 179414 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 361 6 2 4 4.0 c1ccc2c(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2008.12.087
CHEMBL473282 179414 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 361 6 2 4 4.0 c1ccc2c(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2008.12.087
132247311 181246 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4760666 181246 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
2998814 55038 None 0 Human Functional pEC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 245 1 1 2 1.8 C[N+]1=C2CCCCCN2C(O)(c2ccccc2)C1 nan
CHEMBL1301276 55038 None 0 Human Functional pEC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 245 1 1 2 1.8 C[N+]1=C2CCCCCN2C(O)(c2ccccc2)C1 nan
CHEMBL1616268 55038 None 0 Human Functional pEC50 = 4.9 4.9 - 1
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 245 1 1 2 1.8 C[N+]1=C2CCCCCN2C(O)(c2ccccc2)C1 nan
9909555 140778 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 411 8 2 3 5.2 c1ccc(CN2CC(CNCCCc3c[nH]c4ccccc34)Oc3ccccc32)cc1 10.1016/j.bmcl.2005.11.054
CHEMBL381542 140778 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 411 8 2 3 5.2 c1ccc(CN2CC(CNCCCc3c[nH]c4ccccc34)Oc3ccccc32)cc1 10.1016/j.bmcl.2005.11.054
15057516 155992 None 0 Human Functional pEC50 = 5.9 5.9 -269 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4060678 155992 None 0 Human Functional pEC50 = 5.9 5.9 -269 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
10550893 166536 None 0 Human Functional pEC50 = 7.9 7.9 -3 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 436 6 0 6 3.0 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4277532 166536 None 0 Human Functional pEC50 = 7.9 7.9 -3 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 436 6 0 6 3.0 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2nsc3ccccc23)CC1 10.1016/j.ejmech.2017.12.099
1220 187 None 44 Rat Functional pEC50 = 7.9 7.9 1 9
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2023.117518
31 187 None 44 Rat Functional pEC50 = 7.9 7.9 1 9
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2023.117518
7 187 None 44 Rat Functional pEC50 = 7.9 7.9 1 9
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2023.117518
CHEMBL56 187 None 44 Rat Functional pEC50 = 7.9 7.9 1 9
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmc.2023.117518
132247301 180875 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4756233 180875 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 447 7 2 3 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3[nH]ccc23)CC1 10.1021/acs.jmedchem.0c00814
132256713 182576 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 407 7 1 3 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCCc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4786537 182576 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 407 7 1 3 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCCc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
132256749 181239 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4760621 181239 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
21797090 106814 None 0 Human Functional pEC50 = 7.8 7.8 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 503 11 1 7 5.2 S=c1[nH]ncn1[C@@H]1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9806906
CHEMBL3144354 106814 None 0 Human Functional pEC50 = 7.8 7.8 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 503 11 1 7 5.2 S=c1[nH]ncn1[C@@H]1O[C@H](COCc2ccccc2)[C@@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9806906
10647621 163744 None 0 Human Functional pEC50 = 7.8 7.8 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 459 6 1 5 4.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1-n1cccn1 10.1021/jm9806906
CHEMBL42042 163744 None 0 Human Functional pEC50 = 7.8 7.8 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 459 6 1 5 4.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1-n1cccn1 10.1021/jm9806906
145963710 161716 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5nc6c(c(N)c5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4129917 161716 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5nc6c(c(N)c5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
44591230 180416 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 389 7 2 4 4.6 CC(Nc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1)C1CC1 10.1016/j.bmcl.2008.12.087
CHEMBL475105 180416 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 389 7 2 4 4.6 CC(Nc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1)C1CC1 10.1016/j.bmcl.2008.12.087
16109481 83178 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 361 9 1 3 5.3 CC(C)Oc1ccccc1OCCNCc1cccc(-c2ccccc2)c1 10.1021/jm061180b
CHEMBL218217 83178 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 361 9 1 3 5.3 CC(C)Oc1ccccc1OCCNCc1cccc(-c2ccccc2)c1 10.1021/jm061180b
53248212 62053 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
CHEMBL1774534 62053 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
145962678 161730 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 492 6 2 5 5.6 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4130059 161730 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 492 6 2 5 5.6 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5nc6c(c(N)c45)CCCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
135453290 133675 None 29 Human Functional pEC50 = 5.8 5.8 -724 7
Agonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP productionAgonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP production
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL371300 133675 None 29 Human Functional pEC50 = 5.8 5.8 -724 7
Agonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP productionAgonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP production
ChEMBL 191 2 2 4 1.1 C[C@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
5 139 None 45 Human Functional pEC50 = 6.8 6.8 -33 26
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm9015763
5202 139 None 45 Human Functional pEC50 = 6.8 6.8 -33 26
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm9015763
CHEMBL39 139 None 45 Human Functional pEC50 = 6.8 6.8 -33 26
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm9015763
DB08839 139 None 45 Human Functional pEC50 = 6.8 6.8 -33 26
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm9015763
44591229 189806 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 375 7 2 4 4.2 c1ccc2c(CCN3CCCC(c4ccnc(NCC5CC5)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2008.12.087
CHEMBL515438 189806 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 375 7 2 4 4.2 c1ccc2c(CCN3CCCC(c4ccnc(NCC5CC5)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2008.12.087
132256749 181239 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4760621 181239 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 422 7 1 3 4.4 Cc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
130431337 174191 None 0 Human Functional pEC50 = 6.8 6.8 -15 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4544583 174191 None 0 Human Functional pEC50 = 6.8 6.8 -15 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
1220 187 None 44 Human Functional pEC50 = 7.8 7.8 -1 9
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2012.11.042
31 187 None 44 Human Functional pEC50 = 7.8 7.8 -1 9
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2012.11.042
7 187 None 44 Human Functional pEC50 = 7.8 7.8 -1 9
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2012.11.042
CHEMBL56 187 None 44 Human Functional pEC50 = 7.8 7.8 -1 9
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2012.11.042
42606459 17868 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 331 5 1 4 2.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccco3)CC2)nc1 10.1021/jm100835q
CHEMBL1259034 17868 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 331 5 1 4 2.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccco3)CC2)nc1 10.1021/jm100835q
132257265 182215 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4781985 182215 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 437 8 2 4 4.1 CNc1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
9885700 163457 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 370 8 2 4 3.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4c3OCCO4)c2c1 10.1021/jm0304010
CHEMBL419240 163457 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 370 8 2 4 3.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4c3OCCO4)c2c1 10.1021/jm0304010
138692460 179501 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4739908 179501 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1 10.1021/acs.jmedchem.0c00814
5 139 None 45 Human Functional pEC50 = 6.8 6.8 -33 26
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2009.06.019
5202 139 None 45 Human Functional pEC50 = 6.8 6.8 -33 26
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2009.06.019
CHEMBL39 139 None 45 Human Functional pEC50 = 6.8 6.8 -33 26
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2009.06.019
DB08839 139 None 45 Human Functional pEC50 = 6.8 6.8 -33 26
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2009.06.019
11291892 133582 None 3 Human Functional pEC50 = 6.8 6.8 - 1
Inhibition of forskolin-induced increase in cAMP in human 5-hydroxytryptamine 1A receptor expressed HeLa cellsInhibition of forskolin-induced increase in cAMP in human 5-hydroxytryptamine 1A receptor expressed HeLa cells
ChEMBL 378 3 0 4 1.8 O=C1[C@@H]2CCCN2C(=O)CN1CN1CCN(c2cccc3ccccc23)CC1 10.1021/jm048999e
CHEMBL370758 133582 None 3 Human Functional pEC50 = 6.8 6.8 - 1
Inhibition of forskolin-induced increase in cAMP in human 5-hydroxytryptamine 1A receptor expressed HeLa cellsInhibition of forskolin-induced increase in cAMP in human 5-hydroxytryptamine 1A receptor expressed HeLa cells
ChEMBL 378 3 0 4 1.8 O=C1[C@@H]2CCCN2C(=O)CN1CN1CCN(c2cccc3ccccc23)CC1 10.1021/jm048999e
172445107 195412 None 0 Rat Functional pEC50 = 5.8 5.8 14 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 575 8 0 7 4.2 CC12C(=O)C(C)(C(c3ccccc3)=C1c1ccccc1)C1C(=O)N(CCCCN3CCN(c4ncccn4)CC3)C(=O)C12 10.1016/j.bmc.2023.117518
CHEMBL5403228 195412 None 0 Rat Functional pEC50 = 5.8 5.8 14 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 575 8 0 7 4.2 CC12C(=O)C(C)(C(c3ccccc3)=C1c1ccccc1)C1C(=O)N(CCCCN3CCN(c4ncccn4)CC3)C(=O)C12 10.1016/j.bmc.2023.117518
71574204 86301 None 0 Human Functional pEC50 = 4.8 4.8 -18 2
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12 10.1016/j.ejmech.2012.11.042
CHEMBL2312640 86301 None 0 Human Functional pEC50 = 4.8 4.8 -18 2
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cncc2ccccc12 10.1016/j.ejmech.2012.11.042
132257139 181218 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4760271 181218 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1 10.1021/acs.jmedchem.0c00814
23625383 86314 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 5 1 4 3.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ncc(Cl)cn2)CC1 10.1021/jm070714l
CHEMBL231273 86314 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 5 1 4 3.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ncc(Cl)cn2)CC1 10.1021/jm070714l
16109508 84421 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 379 9 1 3 6.0 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCCCC2)c1 10.1021/jm061180b
CHEMBL221957 84421 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 379 9 1 3 6.0 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCCCC2)c1 10.1021/jm061180b
44408946 159663 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 325 5 3 3 3.3 Fc1ccc2[nH]cc(CCNCC3CNc4ccccc4O3)c2c1 10.1016/j.bmcl.2005.11.054
CHEMBL410273 159663 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 325 5 3 3 3.3 Fc1ccc2[nH]cc(CCNCC3CNc4ccccc4O3)c2c1 10.1016/j.bmcl.2005.11.054
71574306 86300 None 0 Human Functional pEC50 = 4.8 4.8 -2 2
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1016/j.ejmech.2012.11.042
CHEMBL2312639 86300 None 0 Human Functional pEC50 = 4.8 4.8 -2 2
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1016/j.ejmech.2012.11.042
145960879 161546 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4ccc5nc6c(c(N)c5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4127445 161546 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4ccc5nc6c(c(N)c5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
56850796 71556 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 371 8 1 4 2.6 O=C1C2CCCN2C(=O)N1CCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926686 71556 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 371 8 1 4 2.6 O=C1C2CCCN2C(=O)N1CCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962913 71556 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 371 8 1 4 2.6 O=C1C2CCCN2C(=O)N1CCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
168355520 196760 None 2 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 395 7 2 4 3.0 O=C(NCCCCN1CCN(c2ccc(F)cc2)CC1)c1n[nH]c2ccccc12 10.1016/j.ejmech.2023.115285
CHEMBL5431642 196760 None 2 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 395 7 2 4 3.0 O=C(NCCCCN1CCN(c2ccc(F)cc2)CC1)c1n[nH]c2ccccc12 10.1016/j.ejmech.2023.115285
42606573 17853 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1258999 17853 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
56850390 71508 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 357 7 1 4 2.2 O=C1C2CCCN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926733 71508 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 357 7 1 4 2.2 O=C1C2CCCN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962486 71508 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 357 7 1 4 2.2 O=C1C2CCCN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
145968927 164862 None 0 Human Functional pEC50 = 7.8 7.8 2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 411 8 1 7 2.8 NC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4217986 164862 None 0 Human Functional pEC50 = 7.8 7.8 2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 411 8 1 7 2.8 NC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
137629633 161228 None 0 Human Functional pEC50 = 7.8 7.8 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 432 4 0 7 2.6 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2 10.1016/j.bmc.2017.07.040
CHEMBL4077006 161228 None 0 Human Functional pEC50 = 7.8 7.8 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 432 4 0 7 2.6 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2 10.1016/j.bmc.2017.07.040
CHEMBL4117235 161228 None 0 Human Functional pEC50 = 7.8 7.8 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 432 4 0 7 2.6 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2 10.1016/j.bmc.2017.07.040
132247311 181246 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4760666 181246 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 451 8 1 4 4.2 CN(C)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
168355520 196760 None 2 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 395 7 2 4 3.0 O=C(NCCCCN1CCN(c2ccc(F)cc2)CC1)c1n[nH]c2ccccc12 10.1016/j.ejmech.2023.115285
CHEMBL5431642 196760 None 2 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 395 7 2 4 3.0 O=C(NCCCCN1CCN(c2ccc(F)cc2)CC1)c1n[nH]c2ccccc12 10.1016/j.ejmech.2023.115285
CHEMBL5086036 217497 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccsc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
CHEMBL5089630 217708 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccc(F)cc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
10528303 101444 None 0 Human Functional pEC50 = 6.8 6.8 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 468 6 1 6 4.1 N#CC1(CNCc2cccc(-n3cccn3)n2)CCN(C(=O)c2ccc(Cl)c(Cl)c2)CC1 10.1021/jm9806906
CHEMBL297208 101444 None 0 Human Functional pEC50 = 6.8 6.8 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 468 6 1 6 4.1 N#CC1(CNCc2cccc(-n3cccn3)n2)CCN(C(=O)c2ccc(Cl)c(Cl)c2)CC1 10.1021/jm9806906
25130235 187693 None 1 Human Functional pEC50 = 5.8 5.8 -13 3
Agonist activity at 5HT1A receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
CHEMBL494678 187693 None 1 Human Functional pEC50 = 5.8 5.8 -13 3
Agonist activity at 5HT1A receptor expressed in CHO cells by GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by GTPgammaS binding assay
ChEMBL 294 2 1 6 1.3 CN1CCN(c2cc(-c3ccc(C#N)cc3)nc(N)n2)CC1 10.1021/jm8005959
71574212 86318 None 0 Human Functional pEC50 = 5.8 5.8 4 2
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312935 86318 None 0 Human Functional pEC50 = 5.8 5.8 4 2
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cnc2ccccc2c1 10.1016/j.ejmech.2012.11.042
44408888 138792 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 339 5 2 3 3.3 CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL377941 138792 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 339 5 2 3 3.3 CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL5085109 217439 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None O=C(CCC1CCN(Cc2ccccc2)CC1)c1ccc(N2CCN(CCCCc3c[nH]c4ccc(Br)cc34)CC2)cc1 10.1016/j.ejmech.2021.114045
44591246 179487 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 6 2 4 4.1 Fc1ccc2[nH]cc(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c2c1 10.1016/j.bmcl.2008.12.087
CHEMBL473903 179487 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 6 2 4 4.1 Fc1ccc2[nH]cc(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c2c1 10.1016/j.bmcl.2008.12.087
122183764 122299 None 0 Human Functional pEC50 = 7.8 7.8 1 3
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 454 7 2 5 3.7 O=C(NCCC(O)CN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1 10.1021/acs.jmedchem.5b00776
CHEMBL3597636 122299 None 0 Human Functional pEC50 = 7.8 7.8 1 3
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 454 7 2 5 3.7 O=C(NCCC(O)CN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1 10.1021/acs.jmedchem.5b00776
42605994 17881 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259071 17881 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
132256735 180616 None 13 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 409 7 1 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4753328 180616 None 13 Human Functional pEC50 = 7.8 7.8 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 409 7 1 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
145978965 166653 None 0 Human Functional pEC50 = 7.8 7.8 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 469 6 2 7 1.8 O=C1[C@@H]2[C@H](C(=O)N1CCCCN1CCN(c3cccc4sccc34)CC1)[C@@H]1C[C@H]2[C@@H](O)[C@H]1O 10.1016/j.ejmech.2017.12.099
CHEMBL4279645 166653 None 0 Human Functional pEC50 = 7.8 7.8 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 469 6 2 7 1.8 O=C1[C@@H]2[C@H](C(=O)N1CCCCN1CCN(c3cccc4sccc34)CC1)[C@@H]1C[C@H]2[C@@H](O)[C@H]1O 10.1016/j.ejmech.2017.12.099
145967359 164276 None 0 Human Functional pEC50 = 7.8 7.8 2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 440 9 1 6 4.2 CCNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4210637 164276 None 0 Human Functional pEC50 = 7.8 7.8 2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 440 9 1 6 4.2 CCNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL5078724 217069 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None Cc1cccc(CN2CCC(CCC(=O)c3ccc(N4CCN(CCCCc5c[nH]c6ccc(C#N)cc56)CC4)cc3)CC2)c1 10.1016/j.ejmech.2021.114045
10381677 106619 None 0 Rat Functional pEC50 = 6.8 6.8 -24 2
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 325 6 2 5 3.3 CN(C)CCc1c[nH]c2ccc(Nc3ncccc3[N+](=O)[O-])cc12 10.1021/jm00042a003
CHEMBL314213 106619 None 0 Rat Functional pEC50 = 6.8 6.8 -24 2
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 325 6 2 5 3.3 CN(C)CCc1c[nH]c2ccc(Nc3ncccc3[N+](=O)[O-])cc12 10.1021/jm00042a003
172442572 195028 None 0 Rat Functional pEC50 = 5.8 5.8 10 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 591 8 0 5 5.5 CC12C(=O)C(C)(C(c3ccccc3)=C1c1ccccc1)C1C(=O)N(CCCCN3CCN(c4ccccc4F)CC3)C(=O)C12 10.1016/j.bmc.2023.117518
CHEMBL5395179 195028 None 0 Rat Functional pEC50 = 5.8 5.8 10 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 591 8 0 5 5.5 CC12C(=O)C(C)(C(c3ccccc3)=C1c1ccccc1)C1C(=O)N(CCCCN3CCN(c4ccccc4F)CC3)C(=O)C12 10.1016/j.bmc.2023.117518
11188024 145669 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4c(ccc5ncccc45)C3)c2c1 10.1016/j.bmcl.2007.03.049
CHEMBL391531 145669 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4c(ccc5ncccc45)C3)c2c1 10.1016/j.bmcl.2007.03.049
162642953 181844 None 0 Human Functional pEC50 = 6.8 6.8 2 3
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 445 8 0 3 5.1 O=C(c1ccccc1)N(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)CC1CC1 10.1016/j.ejmech.2020.112214
CHEMBL4777207 181844 None 0 Human Functional pEC50 = 6.8 6.8 2 3
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 445 8 0 3 5.1 O=C(c1ccccc1)N(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)CC1CC1 10.1016/j.ejmech.2020.112214
CHEMBL5082850 217316 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6cccc(Br)c6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
145974143 164631 None 0 Human Functional pEC50 = 6.8 6.8 -3 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 443 8 1 7 3.2 CNC(=O)c1ccnc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2018.01.038
CHEMBL4215048 164631 None 0 Human Functional pEC50 = 6.8 6.8 -3 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 443 8 1 7 3.2 CNC(=O)c1ccnc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2018.01.038
5 139 None 45 Human Functional pEC50 = 7.8 7.8 -33 26
Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2019.126703
5202 139 None 45 Human Functional pEC50 = 7.8 7.8 -33 26
Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2019.126703
CHEMBL39 139 None 45 Human Functional pEC50 = 7.8 7.8 -33 26
Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2019.126703
DB08839 139 None 45 Human Functional pEC50 = 7.8 7.8 -33 26
Agonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assayAgonist activity at human recombinant 5HT1A receptor (unknown origin) stably expressed in CHO-K1 incubated for 30 mins by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2019.126703
25265257 17866 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 347 5 1 4 3.2 Cc1ccc(CNCC2(F)CCN(C(=O)c3cccs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259032 17866 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 347 5 1 4 3.2 Cc1ccc(CNCC2(F)CCN(C(=O)c3cccs3)CC2)nc1 10.1021/jm100835q
52948486 17927 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 417 5 2 4 3.5 Cc1ccc(CNCC2(O)CC3CCC(C2)N3C(=O)c2ccc(F)c(Cl)c2)nc1 10.1021/jm100835q
CHEMBL1259200 17927 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 417 5 2 4 3.5 Cc1ccc(CNCC2(O)CC3CCC(C2)N3C(=O)c2ccc(F)c(Cl)c2)nc1 10.1021/jm100835q
132257139 181218 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4760271 181218 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2F)CC1 10.1021/acs.jmedchem.0c00814
57397588 71503 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 375 7 1 5 2.4 O=C1C2CCSN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926747 71503 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 375 7 1 5 2.4 O=C1C2CCSN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962460 71503 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 375 7 1 5 2.4 O=C1C2CCSN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
46180256 202686 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 289 2 0 2 3.5 C#CCOc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm9015763
CHEMBL596885 202686 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 289 2 0 2 3.5 C#CCOc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm9015763
24769156 116281 None 0 Human Functional pEC50 = 5.8 5.8 -6 2
Agonist activity at human 5HT1A receptor (unknown origin) expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human 5HT1A receptor (unknown origin) expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 388 7 1 4 3.6 O=C(NCCCCN1CCN(c2ccccc2)CC1)c1ccc2ncccc2c1 10.1021/jm501119j
CHEMBL3358509 116281 None 0 Human Functional pEC50 = 5.8 5.8 -6 2
Agonist activity at human 5HT1A receptor (unknown origin) expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human 5HT1A receptor (unknown origin) expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 388 7 1 4 3.6 O=C(NCCCCN1CCN(c2ccccc2)CC1)c1ccc2ncccc2c1 10.1021/jm501119j
44408784 166192 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 355 6 3 4 3.3 COc1ccc2c(c1)OC(CNCCc1c[nH]c3ccc(F)cc13)CN2 10.1016/j.bmcl.2005.11.054
CHEMBL425936 166192 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 355 6 3 4 3.3 COc1ccc2c(c1)OC(CNCCc1c[nH]c3ccc(F)cc13)CN2 10.1016/j.bmcl.2005.11.054
9799764 88375 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4ccc5ncccc5c4C3)c2c1 10.1016/j.bmcl.2007.03.049
CHEMBL234853 88375 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4ccc5ncccc5c4C3)c2c1 10.1016/j.bmcl.2007.03.049
187811 55090 None 7 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 216 5 2 1 3.0 CCCCc1ccc2[nH]cc(CCN)c2c1 nan
CHEMBL1309229 55090 None 7 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 216 5 2 1 3.0 CCCCc1ccc2[nH]cc(CCN)c2c1 nan
CHEMBL1616674 55090 None 7 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 216 5 2 1 3.0 CCCCc1ccc2[nH]cc(CCN)c2c1 nan
23155625 18694 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 450 6 1 8 2.7 Nn1c(SCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2 10.1021/jm1002292
CHEMBL1277281 18694 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 450 6 1 8 2.7 Nn1c(SCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2 10.1021/jm1002292
CHEMBL5087922 217616 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None O=C(CCC1CCN(Cc2ccccc2)CC1)c1ccc(N2CCN(CCCCc3c[nH]c4ccc(F)cc34)CC2)cc1 10.1016/j.ejmech.2021.114045
138692456 182811 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 407 7 2 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4789505 182811 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 407 7 2 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL5080308 217166 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccoc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
11646498 102559 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 375 11 1 5 2.3 CCOc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
CHEMBL2431051 102559 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 375 11 1 5 2.3 CCOc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
CHEMBL3040382 102559 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 375 11 1 5 2.3 CCOc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
46225309 202596 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 454 8 2 4 4.3 N#Cc1ccc2[nH]cc(CCCCN(CC3CC3)C3COc4ccc5c(c4C3)C(=O)NC5)c2c1 10.1016/j.bmcl.2009.10.134
CHEMBL596297 202596 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 454 8 2 4 4.3 N#Cc1ccc2[nH]cc(CCCCN(CC3CC3)C3COc4ccc5c(c4C3)C(=O)NC5)c2c1 10.1016/j.bmcl.2009.10.134
5 139 None 45 Human Functional pEC50 = 7.7 7.7 -33 26
Agonist activity at serotonin 5-HT1A 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-HT1A 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 = 7.7 7.7 -33 26
Agonist activity at serotonin 5-HT1A 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-HT1A 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 = 7.7 7.7 -33 26
Agonist activity at serotonin 5-HT1A 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-HT1A 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 = 7.7 7.7 -33 26
Agonist activity at serotonin 5-HT1A 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-HT1A 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
75 3514 None 10 Human Functional pEC50 = 7.7 7.7 - 1
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1021/jm0341204
9870500 3514 None 10 Human Functional pEC50 = 7.7 7.7 - 1
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1021/jm0341204
CHEMBL191971 3514 None 10 Human Functional pEC50 = 7.7 7.7 - 1
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1021/jm0341204
132256730 183421 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4797282 183421 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
56850926 71513 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 362 9 1 5 3.2 O=C1CSC(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926759 71513 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 362 9 1 5 3.2 O=C1CSC(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962491 71513 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 362 9 1 5 3.2 O=C1CSC(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
161665 172688 None 26 Human Functional pEC50 = 6.7 6.7 28 3
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL448891 172688 None 26 Human Functional pEC50 = 6.7 6.7 28 3
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
46176231 63986 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at 5-HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 minsAgonist activity at 5-HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins
ChEMBL 467 8 0 5 6.8 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CCCCC2CCSS2)c1-3 10.1021/jm200347t
CHEMBL1806874 63986 None 0 Human Functional pEC50 = 6.7 6.7 1 2
Agonist activity at 5-HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 minsAgonist activity at 5-HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins
ChEMBL 467 8 0 5 6.8 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CCCCC2CCSS2)c1-3 10.1021/jm200347t
9844300 74704 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 407 4 1 4 4.3 COc1cccc2c1OC(CN1CC=C(c3c[nH]c4ccc(F)cc34)CC1)CN2C 10.1016/j.bmcl.2005.11.054
CHEMBL203018 74704 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 407 4 1 4 4.3 COc1cccc2c1OC(CN1CC=C(c3c[nH]c4ccc(F)cc34)CC1)CN2C 10.1016/j.bmcl.2005.11.054
44408681 141408 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 367 6 2 3 4.1 CC(C)N1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL383446 141408 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 367 6 2 3 4.1 CC(C)N1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
16109485 161839 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 353 9 1 3 5.3 CC(C)Oc1ccccc1OCCNCc1cccc(C2CCCC2)c1 10.1021/jm061180b
CHEMBL413777 161839 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 353 9 1 3 5.3 CC(C)Oc1ccccc1OCCNCc1cccc(C2CCCC2)c1 10.1021/jm061180b
44408702 140994 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 349 7 2 3 4.0 CCCN1CC(CNCCc2c[nH]c3ccccc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL382179 140994 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 349 7 2 3 4.0 CCCN1CC(CNCCc2c[nH]c3ccccc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
45102635 57141 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
ChEMBL 311 4 1 3 3.8 Fc1cccc(Cl)c1Oc1cccc(F)c1OC1CNC1 10.1016/j.bmcl.2010.11.066
CHEMBL1645600 57141 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
ChEMBL 311 4 1 3 3.8 Fc1cccc(Cl)c1Oc1cccc(F)c1OC1CNC1 10.1016/j.bmcl.2010.11.066
145 140 None 16 Human Functional pEC50 = 6.7 6.7 -27 12
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
1832 140 None 16 Human Functional pEC50 = 6.7 6.7 -27 12
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
CHEMBL7257 140 None 16 Human Functional pEC50 = 6.7 6.7 -27 12
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
DB14010 140 None 16 Human Functional pEC50 = 6.7 6.7 -27 12
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
156011035 177253 None 0 Human Functional pEC50 = 8.7 8.7 6 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 437 7 0 8 3.3 COc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12 10.1016/j.bmcl.2020.127027
CHEMBL4634009 177253 None 0 Human Functional pEC50 = 8.7 8.7 6 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 437 7 0 8 3.3 COc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12 10.1016/j.bmcl.2020.127027
11428089 18036 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 351 8 3 2 4.4 Fc1ccc2[nH]cc(CCCNCCOc3cccc4[nH]ccc34)c2c1 10.1021/jm0304010
CHEMBL126424 18036 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 351 8 3 2 4.4 Fc1ccc2[nH]cc(CCCNCCOc3cccc4[nH]ccc34)c2c1 10.1021/jm0304010
5 139 None 45 Human Functional pEC50 = 8.7 8.7 -33 26
Agonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2021.113243
5202 139 None 45 Human Functional pEC50 = 8.7 8.7 -33 26
Agonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2021.113243
CHEMBL39 139 None 45 Human Functional pEC50 = 8.7 8.7 -33 26
Agonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2021.113243
DB08839 139 None 45 Human Functional pEC50 = 8.7 8.7 -33 26
Agonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2021.113243
9802369 174089 None 17 Human Functional pEC50 = 8.7 8.7 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 422 6 2 4 4.0 CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C 10.1021/jm9806906
CHEMBL45422 174089 None 17 Human Functional pEC50 = 8.7 8.7 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 422 6 2 4 4.0 CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C 10.1021/jm9806906
156017961 177978 None 0 Human Functional pEC50 = 8.7 8.7 38 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 437 7 0 8 3.3 COc1cccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc12 10.1016/j.bmcl.2020.127027
CHEMBL4644500 177978 None 0 Human Functional pEC50 = 8.7 8.7 38 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 437 7 0 8 3.3 COc1cccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc12 10.1016/j.bmcl.2020.127027
145963961 164498 None 0 Human Functional pEC50 = 8.7 8.7 5 6
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4213342 164498 None 0 Human Functional pEC50 = 8.7 8.7 5 6
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
145981408 166594 None 0 Human Functional pEC50 = 8.6 8.6 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3ccsc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4278581 166594 None 0 Human Functional pEC50 = 8.6 8.6 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3ccsc23)CC1 10.1016/j.ejmech.2017.12.099
49837354 18727 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 549 6 1 10 2.9 CC(=O)N1CCc2c(sc3nc(SCCCN4CCN(c5ccc6ccccc6n5)CC4)n(N)c(=O)c23)C1 10.1021/jm1002292
CHEMBL1277558 18727 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 549 6 1 10 2.9 CC(=O)N1CCc2c(sc3nc(SCCCN4CCN(c5ccc6ccccc6n5)CC4)n(N)c(=O)c23)C1 10.1021/jm1002292
10005161 207707 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Ability to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptorAbility to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptor
ChEMBL 475 9 1 8 3.3 CCC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm0009336
CHEMBL78874 207707 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Ability to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptorAbility to influence the binding of [35S]GTP-gamma-S, to HeLa cell membranes expressing the human 5-hydroxytryptamine 1A receptor
ChEMBL 475 9 1 8 3.3 CCC(=O)c1c(-c2ccccc2)nn(C)c(=O)c1NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm0009336
1220 187 None 44 Human Functional pEC50 = 8.6 8.6 -1 9
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
31 187 None 44 Human Functional pEC50 = 8.6 8.6 -1 9
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
7 187 None 44 Human Functional pEC50 = 8.6 8.6 -1 9
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
CHEMBL56 187 None 44 Human Functional pEC50 = 8.6 8.6 -1 9
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm049493z
16109489 84412 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 362 7 1 4 4.3 C1=C(c2cncc(CNCCOc3cccc4c3OC3(CC3)C4)c2)CCC1 10.1021/jm061180b
CHEMBL221920 84412 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 362 7 1 4 4.3 C1=C(c2cncc(CNCCOc3cccc4c3OC3(CC3)C4)c2)CCC1 10.1021/jm061180b
10718870 168033 None 0 Human Functional pEC50 = 8.6 8.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 461 6 1 4 5.4 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3ccco3)n2)CC1 10.1021/jm9806906
CHEMBL43146 168033 None 0 Human Functional pEC50 = 8.6 8.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 461 6 1 4 5.4 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3ccco3)n2)CC1 10.1021/jm9806906
162651961 180284 None 0 Human Functional pEC50 = 8.6 8.6 7 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 448 7 0 7 4.2 COc1ccc2ncc(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)c2c1 10.1016/j.ejmech.2020.112572
CHEMBL4749223 180284 None 0 Human Functional pEC50 = 8.6 8.6 7 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 448 7 0 7 4.2 COc1ccc2ncc(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)c2c1 10.1016/j.ejmech.2020.112572
127049865 140304 None 0 Human Functional pEC50 = 8.6 8.6 4 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 442 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
CHEMBL3805099 140304 None 0 Human Functional pEC50 = 8.6 8.6 4 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 442 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
164609529 184570 None 0 Human Functional pEC50 = 8.6 8.6 36 2
Agonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4846823 184570 None 0 Human Functional pEC50 = 8.6 8.6 36 2
Agonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human 5-HT1A receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
10647622 166108 None 0 Human Functional pEC50 = 8.6 8.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 459 6 2 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1-c1cc[nH]n1 10.1021/jm9806906
CHEMBL42545 166108 None 0 Human Functional pEC50 = 8.6 8.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 459 6 2 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1-c1cc[nH]n1 10.1021/jm9806906
156013636 177351 None 0 Human Functional pEC50 = 8.6 8.6 41 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 408 6 0 8 2.7 O=c1n(CCCCN2CCN(c3cccc4scnc34)CC2)nc2ccccn12 10.1016/j.bmcl.2020.127027
CHEMBL4635890 177351 None 0 Human Functional pEC50 = 8.6 8.6 41 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 408 6 0 8 2.7 O=c1n(CCCCN2CCN(c3cccc4scnc34)CC2)nc2ccccn12 10.1016/j.bmcl.2020.127027
10474089 208140 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
CHEMBL542671 208140 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
CHEMBL82215 208140 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
10067360 141618 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 364 7 1 4 4.5 CC1(C)Cc2cccc(OCCNCc3cncc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
CHEMBL384657 141618 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 364 7 1 4 4.5 CC1(C)Cc2cccc(OCCNCc3cncc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
10474089 208140 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
CHEMBL542671 208140 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
CHEMBL82215 208140 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 366 6 0 5 3.2 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccccc1 10.1016/s0960-894x(98)00406-5
9928432 18033 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 352 8 2 3 4.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4ccoc34)c2c1 10.1021/jm0304010
CHEMBL126407 18033 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 352 8 2 3 4.7 Fc1ccc2[nH]cc(CCCNCCOc3cccc4ccoc34)c2c1 10.1021/jm0304010
10248163 31571 None 0 Human Functional pEC50 = 8.5 8.5 -288 3
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 363 5 0 4 4.0 COc1cccc2c1CCC/C2=C\CCN1CCN(c2ccccn2)CC1 10.1016/j.bmc.2015.05.042
CHEMBL140406 31571 None 0 Human Functional pEC50 = 8.5 8.5 -288 3
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 363 5 0 4 4.0 COc1cccc2c1CCC/C2=C\CCN1CCN(c2ccccn2)CC1 10.1016/j.bmc.2015.05.042
10789182 178976 None 0 Human Functional pEC50 = 8.5 8.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 438 6 1 4 4.2 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL46971 178976 None 0 Human Functional pEC50 = 8.5 8.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 438 6 1 4 4.2 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
11430856 78050 None 28 Human Functional pEC50 = 7.7 7.7 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 450 10 2 5 3.0 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)CC3CCCCC3)CC2)c1 10.1021/jm0508641
CHEMBL209821 78050 None 28 Human Functional pEC50 = 7.7 7.7 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 450 10 2 5 3.0 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)CC3CCCCC3)CC2)c1 10.1021/jm0508641
10343434 78232 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 444 9 2 5 2.8 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm0508641
CHEMBL210537 78232 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 444 9 2 5 2.8 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)c3ccc(C)cc3)CC2)c1 10.1021/jm0508641
42605993 17887 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3Br)CC2)nc1 10.1021/jm100835q
CHEMBL1259087 17887 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3Br)CC2)nc1 10.1021/jm100835q
42606104 17895 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(C)cs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259107 17895 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(C)cs3)CC2)nc1 10.1021/jm100835q
156017859 177994 None 0 Human Functional pEC50 = 7.7 7.7 2 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 432 6 0 8 3.2 N#Cc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12 10.1016/j.bmcl.2020.127027
CHEMBL4644742 177994 None 0 Human Functional pEC50 = 7.7 7.7 2 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 432 6 0 8 3.2 N#Cc1cccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n12 10.1016/j.bmcl.2020.127027
132256796 182905 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 454 8 1 4 4.6 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4790662 182905 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 454 8 1 4 4.6 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
10550097 167575 None 0 Human Functional pEC50 = 7.7 7.7 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 420 6 1 4 4.1 CN(C)c1cccc(CNCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL42994 167575 None 0 Human Functional pEC50 = 7.7 7.7 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 420 6 1 4 4.1 CN(C)c1cccc(CNCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
10948133 165374 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 351 5 0 4 3.4 COc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)CC2 10.1016/j.bmc.2015.05.042
CHEMBL423181 165374 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 351 5 0 4 3.4 COc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)CC2 10.1016/j.bmc.2015.05.042
132257264 180626 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 410 7 1 5 2.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cnccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4753414 180626 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 410 7 1 5 2.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cnccn2)CC1 10.1021/acs.jmedchem.9b00062
10835365 179024 None 0 Human Functional pEC50 = 7.7 7.7 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 409 5 1 3 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)nc1 10.1021/jm9806906
CHEMBL47013 179024 None 0 Human Functional pEC50 = 7.7 7.7 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 409 5 1 3 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)nc1 10.1021/jm9806906
44537925 201200 None 0 Human Functional pEC50 = 6.7 6.7 7 3
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL582945 201200 None 0 Human Functional pEC50 = 6.7 6.7 7 3
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
4806 4008 None 55 Human Functional pEC50 = 6.7 6.7 -1 3
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
71768094 4008 None 55 Human Functional pEC50 = 6.7 6.7 -1 3
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
71768094.0 4008 None 55 Human Functional pEC50 = 6.7 6.7 -1 3
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 4008 None 55 Human Functional pEC50 = 6.7 6.7 -1 3
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 4008 None 55 Human Functional pEC50 = 6.7 6.7 -1 3
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051.0 4008 None 55 Human Functional pEC50 = 6.7 6.7 -1 3
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 4008 None 55 Human Functional pEC50 = 6.7 6.7 -1 3
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 4008 None 55 Human Functional pEC50 = 6.7 6.7 -1 3
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL5074796 216822 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6cccc(Cl)c6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
23625239 86038 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 409 6 2 4 3.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(CO)cn2)CC1 10.1021/jm070714l
CHEMBL230425 86038 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 409 6 2 4 3.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(CO)cn2)CC1 10.1021/jm070714l
130431319 172623 None 0 Human Functional pEC50 = 5.7 5.7 -11 2
Agonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(C[C@@H](O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.9b00607
CHEMBL4483569 172623 None 0 Human Functional pEC50 = 5.7 5.7 -11 2
Agonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(C[C@@H](O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.9b00607
398712 77898 None 2 Human Functional pEC50 = 7.7 7.7 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm0508641
CHEMBL209324 77898 None 2 Human Functional pEC50 = 7.7 7.7 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 417 9 1 5 2.9 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(C)cc2)CC1 10.1021/jm0508641
168290985 193010 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT1A receptor (unknown origin) transfected in HEK293 cells by calcium flux assayAgonist activity at 5-HT1A receptor (unknown origin) transfected in HEK293 cells by calcium flux assay
ChEMBL 235 5 1 2 2.6 NC[C@H]1C[C@@H]1c1cc(F)ccc1COC1CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5199680 193010 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT1A receptor (unknown origin) transfected in HEK293 cells by calcium flux assayAgonist activity at 5-HT1A receptor (unknown origin) transfected in HEK293 cells by calcium flux assay
ChEMBL 235 5 1 2 2.6 NC[C@H]1C[C@@H]1c1cc(F)ccc1COC1CC1 10.1021/acs.jmedchem.2c00633
CHEMBL5222077 193010 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at 5-HT1A receptor (unknown origin) transfected in HEK293 cells by calcium flux assayAgonist activity at 5-HT1A receptor (unknown origin) transfected in HEK293 cells by calcium flux assay
ChEMBL 235 5 1 2 2.6 NC[C@H]1C[C@@H]1c1cc(F)ccc1COC1CC1 10.1021/acs.jmedchem.2c00633
91242334 167468 None 1 Human Functional pEC50 = 7.7 7.7 6 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 419 6 0 5 4.1 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4294797 167468 None 1 Human Functional pEC50 = 7.7 7.7 6 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 419 6 0 5 4.1 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
11395034 71523 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 385 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926751 71523 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 385 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962585 71523 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 385 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
1220 187 None 44 Human Functional pEC50 = 7.7 7.7 -1 9
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
31 187 None 44 Human Functional pEC50 = 7.7 7.7 -1 9
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
7 187 None 44 Human Functional pEC50 = 7.7 7.7 -1 9
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
CHEMBL56 187 None 44 Human Functional pEC50 = 7.7 7.7 -1 9
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
132247312 180761 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4755058 180761 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 465 8 2 4 4.1 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
10787547 172702 None 0 Human Functional pEC50 = 7.7 7.7 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 406 6 2 4 4.1 CNc1cccc(CNCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL44904 172702 None 0 Human Functional pEC50 = 7.7 7.7 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 406 6 2 4 4.1 CNc1cccc(CNCC2CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL5090651 217766 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None O=C(CCC1CCN(Cc2ccccc2)CC1)c1ccc(N2CCN(CCCCc3c[nH]c4ccc(Cl)cc34)CC2)cc1 10.1016/j.ejmech.2021.114045
53248213 62054 None 0 Human Functional pEC50 = 5.7 5.7 -2 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
CHEMBL1774535 62054 None 0 Human Functional pEC50 = 5.7 5.7 -2 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
44591261 180936 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 6 2 4 4.1 Fc1cccc2c(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c[nH]c12 10.1016/j.bmcl.2008.12.087
CHEMBL475694 180936 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 6 2 4 4.1 Fc1cccc2c(CCN3CCCC(c4ccnc(NC5CC5)n4)C3)c[nH]c12 10.1016/j.bmcl.2008.12.087
45375937 201302 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
ChEMBL 271 3 1 2 4.1 Fc1cccc(Oc2ccccc2C2CCNCC2)c1 10.1016/j.bmcl.2009.10.014
CHEMBL583752 201302 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
ChEMBL 271 3 1 2 4.1 Fc1cccc(Oc2ccccc2C2CCNCC2)c1 10.1016/j.bmcl.2009.10.014
CHEMBL5088919 217676 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6cccnc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
46225264 204252 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 386 5 3 4 2.8 N#Cc1ccc2[nH]cc(CCCNC3COc4ccc5c(c4C3)C(=O)NC5)c2c1 10.1016/j.bmcl.2009.10.134
CHEMBL606864 204252 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 386 5 3 4 2.8 N#Cc1ccc2[nH]cc(CCCNC3COc4ccc5c(c4C3)C(=O)NC5)c2c1 10.1016/j.bmcl.2009.10.134
417608 119227 None 24 Human Functional pEC50 = 7.7 7.7 - 1
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 246 6 1 2 3.1 CCN(CC)CCc1c[nH]c2ccc(OC)cc12 10.1021/jm000339w
CHEMBL342986 119227 None 24 Human Functional pEC50 = 7.7 7.7 - 1
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 246 6 1 2 3.1 CCN(CC)CCc1c[nH]c2ccc(OC)cc12 10.1021/jm000339w
CHEMBL5080984 217201 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6cc[nH]c6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
11430418 18793 None 9 Human Functional pEC50 = 7.7 7.7 177 3
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 432 6 1 7 2.5 Nn1c(CCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2 10.1021/jm1002292
CHEMBL1278088 18793 None 9 Human Functional pEC50 = 7.7 7.7 177 3
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 432 6 1 7 2.5 Nn1c(CCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2c(c1=O)CCCC2 10.1021/jm1002292
CHEMBL5087351 217577 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None COC(=O)c1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccccc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
162677377 183646 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 366 7 0 4 3.1 CC(C)N(CCCN1CCN(c2ccccn2)CC1)C(=O)c1ccccc1 10.1016/j.ejmech.2020.112214
CHEMBL4800109 183646 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 366 7 0 4 3.1 CC(C)N(CCCN1CCN(c2ccccn2)CC1)C(=O)c1ccccc1 10.1016/j.ejmech.2020.112214
10743303 178440 None 0 Human Functional pEC50 = 7.6 7.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 478 6 1 5 5.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3nccs3)n2)CC1 10.1021/jm9806906
CHEMBL46512 178440 None 0 Human Functional pEC50 = 7.6 7.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 478 6 1 5 5.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3nccs3)n2)CC1 10.1021/jm9806906
10427186 208378 None 0 Rat Functional pEC50 = 6.7 6.7 -57 2
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 337 5 3 5 3.5 O=[N+]([O-])c1cccnc1Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm00042a003
CHEMBL84107 208378 None 0 Rat Functional pEC50 = 6.7 6.7 -57 2
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 337 5 3 5 3.5 O=[N+]([O-])c1cccnc1Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm00042a003
146 135 None 50 Human Functional pEC50 = 5.7 5.7 -851 2
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 nan
164682 135 None 50 Human Functional pEC50 = 5.7 5.7 -851 2
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 nan
CHEMBL275628 135 None 50 Human Functional pEC50 = 5.7 5.7 -851 2
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 178 2 2 1 1.8 NCCc1c[nH]c2c1cc(F)cc2 nan
168295509 192623 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assayAgonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay
ChEMBL 449 6 1 8 3.0 COc1cc2ncnc(N3CCC(CN4CCN(c5ccccc5O)CC4)C3)c2cc1OC 10.1016/j.ejmech.2022.114218
CHEMBL5209283 192623 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assayAgonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay
ChEMBL 449 6 1 8 3.0 COc1cc2ncnc(N3CCC(CN4CCN(c5ccccc5O)CC4)C3)c2cc1OC 10.1016/j.ejmech.2022.114218
51003382 57142 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
ChEMBL 291 4 1 3 3.4 Cc1cccc(F)c1Oc1cccc(F)c1OC1CNC1 10.1016/j.bmcl.2010.11.066
CHEMBL1645601 57142 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
ChEMBL 291 4 1 3 3.4 Cc1cccc(F)c1Oc1cccc(F)c1OC1CNC1 10.1016/j.bmcl.2010.11.066
5 139 None 45 Human Functional pEC50 = 6.6 6.6 -33 26
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm070714l
5202 139 None 45 Human Functional pEC50 = 6.6 6.6 -33 26
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm070714l
CHEMBL39 139 None 45 Human Functional pEC50 = 6.6 6.6 -33 26
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm070714l
DB08839 139 None 45 Human Functional pEC50 = 6.6 6.6 -33 26
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm070714l
10364325 149447 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 411 6 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(CF)cn2)CC1 10.1021/jm070714l
CHEMBL394530 149447 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 411 6 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(CF)cn2)CC1 10.1021/jm070714l
11595672 102647 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 361 10 1 5 1.9 COc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
CHEMBL2431048 102647 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 361 10 1 5 1.9 COc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
CHEMBL3040882 102647 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 361 10 1 5 1.9 COc1ccccc1OCCNCCCCN1C(=O)C2CCCN2C1=O 10.1021/jm400766k
11573726 71555 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 343 6 1 4 1.8 O=C1C2CCCN2C(=O)N1CCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926750 71555 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 343 6 1 4 1.8 O=C1C2CCCN2C(=O)N1CCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962912 71555 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 343 6 1 4 1.8 O=C1C2CCCN2C(=O)N1CCCNCC1CCc2ccccc2O1 10.1021/jm2007886
9865384 173599 None 32 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm070714l
9865384.0 173599 None 32 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm070714l
CHEMBL45305 173599 None 32 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm070714l
145975214 164013 None 0 Human Functional pEC50 = 7.6 7.6 2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 436 8 1 5 3.7 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.bmcl.2018.01.038
CHEMBL4207328 164013 None 0 Human Functional pEC50 = 7.6 7.6 2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 436 8 1 5 3.7 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)n1 10.1016/j.bmcl.2018.01.038
23626001 86012 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 429 6 1 3 4.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(C(F)F)cn2)CC1 10.1021/jm070714l
CHEMBL230327 86012 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 429 6 1 3 4.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(C(F)F)cn2)CC1 10.1021/jm070714l
46225207 204358 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 433 7 2 3 4.2 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL607419 204358 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 433 7 2 3 4.2 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
242 470 None 70 Human Functional pEC50 = 7.6 7.6 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
34 470 None 70 Human Functional pEC50 = 7.6 7.6 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
60795 470 None 70 Human Functional pEC50 = 7.6 7.6 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
60795.0 470 None 70 Human Functional pEC50 = 7.6 7.6 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
CHEMBL1112 470 None 70 Human Functional pEC50 = 7.6 7.6 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
DB01238 470 None 70 Human Functional pEC50 = 7.6 7.6 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
127050765 140301 None 0 Human Functional pEC50 = 7.6 7.6 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 435 8 1 4 4.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805077 140301 None 0 Human Functional pEC50 = 7.6 7.6 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 435 8 1 4 4.3 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
129186528 157557 None 0 Human Functional pEC50 = 7.6 7.6 -4 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 442 4 0 6 4.2 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2Cl 10.1016/j.bmc.2017.07.040
CHEMBL4079251 157557 None 0 Human Functional pEC50 = 7.6 7.6 -4 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 442 4 0 6 4.2 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2Cl 10.1016/j.bmc.2017.07.040
16109487 83429 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 365 7 1 4 4.9 CC1(C)Oc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
CHEMBL219486 83429 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 365 7 1 4 4.9 CC1(C)Oc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
162666972 182646 None 0 Human Functional pEC50 = 7.6 7.6 309 2
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 378 8 0 4 3.1 O=C(c1ccccc1)N(CCCN1CCN(c2ccccn2)CC1)CC1CC1 10.1016/j.ejmech.2020.112214
CHEMBL4787394 182646 None 0 Human Functional pEC50 = 7.6 7.6 309 2
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 378 8 0 4 3.1 O=C(c1ccccc1)N(CCCN1CCN(c2ccccn2)CC1)CC1CC1 10.1016/j.ejmech.2020.112214
42606461 17875 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 331 5 1 4 2.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccoc3)CC2)nc1 10.1021/jm100835q
CHEMBL1259051 17875 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 331 5 1 4 2.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccoc3)CC2)nc1 10.1021/jm100835q
42606337 17939 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccc4s3)CC2)nc1 10.1021/jm100835q
CHEMBL1259242 17939 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccc4s3)CC2)nc1 10.1021/jm100835q
11741361 2830 None 36 Human Functional pEC50 = 6.6 6.6 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.9b00062
3924 2830 None 36 Human Functional pEC50 = 6.6 6.6 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.9b00062
CHEMBL230963 2830 None 36 Human Functional pEC50 = 6.6 6.6 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.9b00062
146025790 183102 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 424 7 1 3 4.8 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCSc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4793515 183102 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 424 7 1 3 4.8 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCSc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL5087427 217587 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None CCCCN1CCC(CCC(=O)c2ccc(N3CCN(CCCCc4c[nH]c5ccc(C#N)cc45)CC3)cc2)CC1 10.1016/j.ejmech.2021.114045
46227754 204124 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 393 5 3 3 3.1 O=C1NCCc2ccc3c(c21)CC(NCCCc1c[nH]c2ccc(F)cc12)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL606149 204124 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 393 5 3 3 3.1 O=C1NCCc2ccc3c(c21)CC(NCCCc1c[nH]c2ccc(F)cc12)CO3 10.1016/j.bmcl.2009.10.134
132256811 180049 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2Cl)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4746386 180049 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2Cl)CC1 10.1021/acs.jmedchem.0c00814
9865384 173599 None 32 Human Functional pEC50 = 7.6 7.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm9806906
9865384.0 173599 None 32 Human Functional pEC50 = 7.6 7.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm9806906
CHEMBL45305 173599 None 32 Human Functional pEC50 = 7.6 7.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm9806906
11175450 117011 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 347 9 3 2 4.6 c1ccc2c(CCCCNCCOc3cccc4[nH]ccc34)c[nH]c2c1 10.1021/jm0304010
CHEMBL338587 117011 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 347 9 3 2 4.6 c1ccc2c(CCCCNCCOc3cccc4[nH]ccc34)c[nH]c2c1 10.1021/jm0304010
11603514 71514 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926760 71514 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962492 71514 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 390 11 1 5 4.0 O=C1CSC(=O)N1CCCCCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
122183771 122306 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 426 7 2 3 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.5b00776
CHEMBL3597643 122306 None 0 Human Functional pEC50 = 6.6 6.6 -7 3
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 426 7 2 3 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.5b00776
132256730 183421 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4797282 183421 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
44461160 105484 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 429 4 0 7 1.4 O=C1c2ccccc2S(=O)(=O)N1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
CHEMBL311976 105484 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 429 4 0 7 1.4 O=C1c2ccccc2S(=O)(=O)N1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
168295269 192621 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assayAgonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay
ChEMBL 463 7 0 8 3.3 COc1cccc(N2CCN(CC3CCN(c4ncnc5cc(OC)c(OC)cc45)C3)CC2)c1 10.1016/j.ejmech.2022.114218
CHEMBL5209272 192621 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assayAgonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay
ChEMBL 463 7 0 8 3.3 COc1cccc(N2CCN(CC3CCN(c4ncnc5cc(OC)c(OC)cc45)C3)CC2)c1 10.1016/j.ejmech.2022.114218
15980810 202114 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 435 6 2 3 4.2 CC(C)N(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
CHEMBL592951 202114 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 435 6 2 3 4.2 CC(C)N(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
1220 187 None 44 Human Functional pEC50 = 7.6 7.6 -1 9
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm8007097
31 187 None 44 Human Functional pEC50 = 7.6 7.6 -1 9
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm8007097
7 187 None 44 Human Functional pEC50 = 7.6 7.6 -1 9
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm8007097
CHEMBL56 187 None 44 Human Functional pEC50 = 7.6 7.6 -1 9
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm8007097
CHEMBL5085893 217486 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6cccnc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
CHEMBL5094829 218005 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6cc[nH]c6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
46227757 203748 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 407 5 2 3 3.5 CN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
CHEMBL604063 203748 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 407 5 2 3 3.5 CN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
127049517 140290 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 465 9 1 5 4.3 CNC(=O)c1ccc(OC)c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3804943 140290 None 0 Human Functional pEC50 = 7.6 7.6 -2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 465 9 1 5 4.3 CNC(=O)c1ccc(OC)c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
127051038 140399 None 0 Human Functional pEC50 = 7.6 7.6 2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 421 8 1 4 4.1 NC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3806169 140399 None 0 Human Functional pEC50 = 7.6 7.6 2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 421 8 1 4 4.1 NC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
9950538 207316 None 0 Human Functional pEC50 = 7.6 7.6 -630 4
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
ChEMBL 355 3 1 4 4.0 CN1CCC[C@@H]1Cc1c[nH]c2ccc(-n3cnc4cc(C#N)ccc43)cc12 10.1016/0960-894X(95)00417-R
CHEMBL75642 207316 None 0 Human Functional pEC50 = 7.6 7.6 -630 4
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
ChEMBL 355 3 1 4 4.0 CN1CCC[C@@H]1Cc1c[nH]c2ccc(-n3cnc4cc(C#N)ccc43)cc12 10.1016/0960-894X(95)00417-R
49782156 17930 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 387 5 1 3 4.2 Cc1ccc(CNCC2(F)CCN(C(=O)C34CCCC(CCC3)C4)CC2)nc1 10.1021/jm100835q
CHEMBL1259210 17930 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 387 5 1 3 4.2 Cc1ccc(CNCC2(F)CCN(C(=O)C34CCCC(CCC3)C4)CC2)nc1 10.1021/jm100835q
137658832 159433 None 0 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 448 4 1 8 2.1 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4100152 159433 None 0 Human Functional pEC50 = 7.6 7.6 1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 448 4 1 8 2.1 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3OC(F)(F)O4)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
10503335 167958 None 0 Human Functional pEC50 = 6.6 6.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 441 6 1 5 4.1 O=C(c1ccc(Cl)c(Cl)c1)N1CC=C(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
CHEMBL43097 167958 None 0 Human Functional pEC50 = 6.6 6.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 441 6 1 5 4.1 O=C(c1ccc(Cl)c(Cl)c1)N1CC=C(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
5 139 None 45 Human Functional pEC50 = 7.6 7.6 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2015.05.042
5202 139 None 45 Human Functional pEC50 = 7.6 7.6 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2015.05.042
CHEMBL39 139 None 45 Human Functional pEC50 = 7.6 7.6 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2015.05.042
DB08839 139 None 45 Human Functional pEC50 = 7.6 7.6 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISAAgonist activity at human 5-HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 15 mins by ELISA
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2015.05.042
155533824 172001 None 0 Human Functional pEC50 = 7.6 7.6 25 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 238 2 0 2 2.7 CCc1cccc(N2CCN(C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4469777 172001 None 0 Human Functional pEC50 = 7.6 7.6 25 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 238 2 0 2 2.7 CCc1cccc(N2CCN(C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
49781265 103463 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 365 5 2 4 2.7 Cc1ccc(CNC[C@]2(O)C[C@@H]3CC[C@H](C2)N3C(=O)c2ccccc2)nc1 10.1021/jm100835q
CHEMBL3084757 103463 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 365 5 2 4 2.7 Cc1ccc(CNC[C@]2(O)C[C@@H]3CC[C@H](C2)N3C(=O)c2ccccc2)nc1 10.1021/jm100835q
132247309 179546 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 476 7 1 3 5.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(C(F)(F)F)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4740430 179546 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 476 7 1 3 5.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(C(F)(F)F)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL5088060 217625 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccccc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
46225166 201974 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 407 6 2 3 3.8 CCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NC3 10.1016/j.bmcl.2009.10.134
CHEMBL592029 201974 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 407 6 2 3 3.8 CCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NC3 10.1016/j.bmcl.2009.10.134
145964622 164441 None 0 Human Functional pEC50 = 7.6 7.6 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 452 9 1 6 4.3 O=C(NC1CC1)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4212622 164441 None 0 Human Functional pEC50 = 7.6 7.6 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 452 9 1 6 4.3 O=C(NC1CC1)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
172449599 195693 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 407 8 2 5 2.9 COc1cccc(N2CCN(CCCCNC(=O)c3n[nH]c4ccccc34)CC2)c1 10.1016/j.ejmech.2023.115285
CHEMBL5409227 195693 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 407 8 2 5 2.9 COc1cccc(N2CCN(CCCCNC(=O)c3n[nH]c4ccccc34)CC2)c1 10.1016/j.ejmech.2023.115285
1220 187 None 44 Human Functional pEC50 = 7.6 7.6 -1 9
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm061180b
31 187 None 44 Human Functional pEC50 = 7.6 7.6 -1 9
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm061180b
7 187 None 44 Human Functional pEC50 = 7.6 7.6 -1 9
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm061180b
CHEMBL56 187 None 44 Human Functional pEC50 = 7.6 7.6 -1 9
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm061180b
10742699 169318 None 0 Human Functional pEC50 = 7.6 7.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 461 6 1 5 4.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
CHEMBL440854 169318 None 0 Human Functional pEC50 = 7.6 7.6 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 461 6 1 5 4.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
CHEMBL5082360 217290 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None COc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccccc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
118626089 165568 None 3 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assayPartial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assay
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
CHEMBL4239823 165568 None 3 Human Functional pEC50 = 7.6 7.6 - 1
Partial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assayPartial agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in cAMP accumulation by chemiluminescence-based assay
ChEMBL 506 6 0 6 4.8 O=S(=O)(c1cncc2ccccc12)N1CCC[C@H]1CCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2018.01.002
172449599 195693 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 407 8 2 5 2.9 COc1cccc(N2CCN(CCCCNC(=O)c3n[nH]c4ccccc34)CC2)c1 10.1016/j.ejmech.2023.115285
CHEMBL5409227 195693 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 minsAgonist activity at human 5HT1A expressed in HEK293 cells assessed as inhibition of forskolin stimulated cAMP production preincubated for 10 mins followed by forskolin addition for 5 mins
ChEMBL 407 8 2 5 2.9 COc1cccc(N2CCN(CCCCNC(=O)c3n[nH]c4ccccc34)CC2)c1 10.1016/j.ejmech.2023.115285
137643395 158239 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 426 4 1 7 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3CCS4)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4087246 158239 None 0 Human Functional pEC50 = 7.5 7.5 -2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 426 4 1 7 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4c3CCS4)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
145961788 161665 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(N)c6c(nc5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4129051 161665 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 478 6 2 5 5.2 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(N)c6c(nc5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
132257264 180626 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 410 7 1 5 2.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cnccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4753414 180626 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 410 7 1 5 2.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cnccn2)CC1 10.1021/acs.jmedchem.9b00062
10695466 172817 None 0 Human Functional pEC50 = 7.5 7.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 464 8 1 4 4.8 CCN(CC)c1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C 10.1021/jm9806906
CHEMBL45048 172817 None 0 Human Functional pEC50 = 7.5 7.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 464 8 1 4 4.8 CCN(CC)c1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C 10.1021/jm9806906
46225310 202507 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 393 6 3 3 3.5 O=C1NCc2ccc3c(c21)CC(NCCCCc1c[nH]c2ccc(F)cc12)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL595622 202507 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 393 6 3 3 3.5 O=C1NCc2ccc3c(c21)CC(NCCCCc1c[nH]c2ccc(F)cc12)CO3 10.1016/j.bmcl.2009.10.134
242 470 None 70 Human Functional pEC50 = 6.5 6.5 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
34 470 None 70 Human Functional pEC50 = 6.5 6.5 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
60795 470 None 70 Human Functional pEC50 = 6.5 6.5 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
60795.0 470 None 70 Human Functional pEC50 = 6.5 6.5 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
CHEMBL1112 470 None 70 Human Functional pEC50 = 6.5 6.5 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
DB01238 470 None 70 Human Functional pEC50 = 6.5 6.5 -31 33
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2016.04.087
55191 99671 None 43 Human Functional pEC50 = 6.5 6.5 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 10.1021/jm0508641
55191.0 99671 None 43 Human Functional pEC50 = 6.5 6.5 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 10.1021/jm0508641
CHEMBL284092 99671 None 43 Human Functional pEC50 = 6.5 6.5 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 10.1021/jm0508641
DB12184 99671 None 43 Human Functional pEC50 = 6.5 6.5 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 10.1021/jm0508641
135399666 168866 None 4 Human Functional pEC50 = 5.5 5.5 -33 6
Agonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP productionAgonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP production
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL437314 168866 None 4 Human Functional pEC50 = 5.5 5.5 -33 6
Agonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP productionAgonistic activity at cloned human 5HT1A receptor expressed in CHO cells by inhibition of forskolin-induced cAMP production
ChEMBL 191 2 2 4 1.1 C[C@@H](N)Cn1ncc2ccc(O)cc21 10.1021/jm050663x
CHEMBL5084736 217421 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None C#CCN1CCC(CCC(=O)c2ccc(N3CCN(CCCCc4c[nH]c5ccc(C#N)cc45)CC3)cc2)CC1 10.1016/j.ejmech.2021.114045
CHEMBL5092455 217859 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccoc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
132247303 180365 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 451 8 2 4 3.2 NC(=O)c1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4750444 180365 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 451 8 2 4 3.2 NC(=O)c1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
44591281 180399 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 362 6 1 4 4.0 c1ccc2c(c1)CC(CCN1CCCC(c3ccnc(NC4CC4)n3)C1)C2 10.1016/j.bmcl.2008.12.087
CHEMBL475090 180399 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 362 6 1 4 4.0 c1ccc2c(c1)CC(CCN1CCCC(c3ccnc(NC4CC4)n3)C1)C2 10.1016/j.bmcl.2008.12.087
5 139 None 45 Human Functional pEC50 = 8.5 8.5 -33 26
Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2014.09.024
5202 139 None 45 Human Functional pEC50 = 8.5 8.5 -33 26
Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2014.09.024
CHEMBL39 139 None 45 Human Functional pEC50 = 8.5 8.5 -33 26
Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2014.09.024
DB08839 139 None 45 Human Functional pEC50 = 8.5 8.5 -33 26
Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2014.09.024
9906183 118167 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 345 8 2 3 4.3 c1cnc2c(OCCNCCCc3c[nH]c4ccccc34)cccc2c1 10.1021/jm0304010
CHEMBL340705 118167 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 345 8 2 3 4.3 c1cnc2c(OCCNCCCc3c[nH]c4ccccc34)cccc2c1 10.1021/jm0304010
10789419 172859 None 0 Human Functional pEC50 = 8.5 8.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 443 6 2 4 4.4 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cc[nH]n3)n2)CC1 10.1021/jm9806906
CHEMBL45101 172859 None 0 Human Functional pEC50 = 8.5 8.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 443 6 2 4 4.4 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cc[nH]n3)n2)CC1 10.1021/jm9806906
145988006 167217 None 0 Human Functional pEC50 = 8.5 8.5 14 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 553 8 0 9 2.9 CC(=O)O[C@H]1[C@H]2C[C@H]([C@@H]3C(=O)N(CCCCN4CCN(c5cccc6sccc56)CC4)C(=O)[C@H]23)[C@H]1OC(C)=O 10.1016/j.ejmech.2017.12.099
CHEMBL4290309 167217 None 0 Human Functional pEC50 = 8.5 8.5 14 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 553 8 0 9 2.9 CC(=O)O[C@H]1[C@H]2C[C@H]([C@@H]3C(=O)N(CCCCN4CCN(c5cccc6sccc56)CC4)C(=O)[C@H]23)[C@H]1OC(C)=O 10.1016/j.ejmech.2017.12.099
145990482 167079 None 0 Human Functional pEC50 = 8.5 8.5 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 436 6 0 6 3.0 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3scnc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4287752 167079 None 0 Human Functional pEC50 = 8.5 8.5 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 436 6 0 6 3.0 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3scnc23)CC1 10.1016/j.ejmech.2017.12.099
1220 187 None 44 Human Functional pEC50 = 8.5 8.5 -1 9
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2021.114045
31 187 None 44 Human Functional pEC50 = 8.5 8.5 -1 9
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2021.114045
7 187 None 44 Human Functional pEC50 = 8.5 8.5 -1 9
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2021.114045
CHEMBL56 187 None 44 Human Functional pEC50 = 8.5 8.5 -1 9
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.ejmech.2021.114045
162643405 181857 None 0 Human Functional pEC50 = 8.5 8.5 8 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 434 6 1 6 3.5 O=c1[nH]c(=O)n(CCCCN2CCN(c3cccc4sccc34)CC2)c2ccccc12 10.1016/j.ejmech.2020.112572
CHEMBL4777475 181857 None 0 Human Functional pEC50 = 8.5 8.5 8 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 434 6 1 6 3.5 O=c1[nH]c(=O)n(CCCCN2CCN(c3cccc4sccc34)CC2)c2ccccc12 10.1016/j.ejmech.2020.112572
5 139 None 45 Human Functional pEC50 = 8.5 8.5 -33 26
Agonist activity at 5-HT1A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT1A 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 = 8.5 8.5 -33 26
Agonist activity at 5-HT1A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT1A 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 = 8.5 8.5 -33 26
Agonist activity at 5-HT1A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT1A 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 = 8.5 8.5 -33 26
Agonist activity at 5-HT1A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT1A receptor (unknown origin) by calcium flux assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.3c00734
10647006 165548 None 0 Human Functional pEC50 = 8.5 8.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 445 6 1 4 4.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3ccco3)n2)CC1 10.1021/jm9806906
CHEMBL42393 165548 None 0 Human Functional pEC50 = 8.5 8.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 445 6 1 4 4.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3ccco3)n2)CC1 10.1021/jm9806906
132257058 181015 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 449 7 2 4 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3c2CCN3)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4757755 181015 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 449 7 2 4 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc3c2CCN3)CC1 10.1021/acs.jmedchem.0c00814
11518341 77076 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 464 10 1 5 3.4 CC(=O)Nc1cccc(N2CCN(CCCCN(C)S(=O)(=O)CC3CCCCC3)CC2)c1 10.1021/jm0508641
CHEMBL207220 77076 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 464 10 1 5 3.4 CC(=O)Nc1cccc(N2CCN(CCCCN(C)S(=O)(=O)CC3CCCCC3)CC2)c1 10.1021/jm0508641
145983928 166507 None 0 Human Functional pEC50 = 8.4 8.4 1 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4277101 166507 None 0 Human Functional pEC50 = 8.4 8.4 1 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
145992860 166968 None 0 Human Functional pEC50 = 8.4 8.4 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 437 6 0 6 2.2 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4285839 166968 None 0 Human Functional pEC50 = 8.4 8.4 2 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 437 6 0 6 2.2 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/j.ejmech.2017.12.099
10740939 122688 None 0 Human Functional pEC50 = 8.4 8.4 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 422 6 1 4 3.7 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL360319 122688 None 0 Human Functional pEC50 = 8.4 8.4 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 422 6 1 4 3.7 CN(C)c1cccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm9806906
10694239 173716 None 0 Human Functional pEC50 = 8.4 8.4 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 436 6 1 4 4.0 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1N(C)C 10.1021/jm9806906
CHEMBL45336 173716 None 0 Human Functional pEC50 = 8.4 8.4 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 436 6 1 4 4.0 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1N(C)C 10.1021/jm9806906
5 139 None 45 Human Functional pEC50 = 8.4 8.4 -33 26
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2012.12.016
5202 139 None 45 Human Functional pEC50 = 8.4 8.4 -33 26
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2012.12.016
CHEMBL39 139 None 45 Human Functional pEC50 = 8.4 8.4 -33 26
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2012.12.016
DB08839 139 None 45 Human Functional pEC50 = 8.4 8.4 -33 26
Agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2012.12.016
42606101 17882 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Br)s3)CC2)nc1 10.1021/jm100835q
CHEMBL1259072 17882 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Br)s3)CC2)nc1 10.1021/jm100835q
42605991 17907 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 4 3.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3Cl)CC2)nc1 10.1021/jm100835q
CHEMBL1259139 17907 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 4 3.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3Cl)CC2)nc1 10.1021/jm100835q
11464531 18738 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 428 6 1 7 2.8 Nn1c(CCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2ccccc2c1=O 10.1021/jm1002292
CHEMBL1277651 18738 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human cloned 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 428 6 1 7 2.8 Nn1c(CCCCN2CCN(c3ccc4ccccc4n3)CC2)nc2ccccc2c1=O 10.1021/jm1002292
137631570 156575 None 0 Human Functional pEC50 = 7.5 7.5 5 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 430 4 1 8 3.0 Cc1nc2n(c(=O)c1CCN1CCN(c3csc4ccsc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4067506 156575 None 0 Human Functional pEC50 = 7.5 7.5 5 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 430 4 1 8 3.0 Cc1nc2n(c(=O)c1CCN1CCN(c3csc4ccsc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
5 139 None 45 Human Functional pEC50 = 7.5 7.5 -33 26
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.0c00814
5202 139 None 45 Human Functional pEC50 = 7.5 7.5 -33 26
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.0c00814
CHEMBL39 139 None 45 Human Functional pEC50 = 7.5 7.5 -33 26
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.0c00814
DB08839 139 None 45 Human Functional pEC50 = 7.5 7.5 -33 26
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.0c00814
5 139 None 45 Human Functional pEC50 = 7.5 7.5 -33 26
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b00062
5202 139 None 45 Human Functional pEC50 = 7.5 7.5 -33 26
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b00062
CHEMBL39 139 None 45 Human Functional pEC50 = 7.5 7.5 -33 26
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b00062
DB08839 139 None 45 Human Functional pEC50 = 7.5 7.5 -33 26
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b00062
10646934 101154 None 0 Human Functional pEC50 = 7.5 7.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 443 6 1 5 4.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
CHEMBL295025 101154 None 0 Human Functional pEC50 = 7.5 7.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 443 6 1 5 4.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
137635433 156028 None 0 Human Functional pEC50 = 6.5 6.5 -125 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 439 4 1 8 2.5 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2(C)O 10.1016/j.bmc.2017.07.040
CHEMBL4061068 156028 None 0 Human Functional pEC50 = 6.5 6.5 -125 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 439 4 1 8 2.5 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2(C)O 10.1016/j.bmc.2017.07.040
127051340 140299 None 0 Human Functional pEC50 = 6.5 6.5 -10 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 453 8 1 4 4.5 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1F 10.1016/j.bmcl.2016.04.087
CHEMBL3805046 140299 None 0 Human Functional pEC50 = 6.5 6.5 -10 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 453 8 1 4 4.5 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1F 10.1016/j.bmcl.2016.04.087
11339067 87617 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 417 7 1 3 5.5 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3ncccc3c2C1 10.1016/j.bmcl.2007.03.049
CHEMBL233591 87617 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 417 7 1 3 5.5 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3ncccc3c2C1 10.1016/j.bmcl.2007.03.049
44593729 179486 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 363 7 2 4 4.2 CCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1 10.1016/j.bmcl.2008.12.087
CHEMBL473902 179486 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 363 7 2 4 4.2 CCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1 10.1016/j.bmcl.2008.12.087
11741361 2830 None 36 Human Functional pEC50 = 6.5 6.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.0c00814
3924 2830 None 36 Human Functional pEC50 = 6.5 6.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.0c00814
CHEMBL230963 2830 None 36 Human Functional pEC50 = 6.5 6.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.0c00814
127049522 140291 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 435 8 1 4 4.3 CNC(=O)c1ccccc1OCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2016.04.087
CHEMBL3804954 140291 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 435 8 1 4 4.3 CNC(=O)c1ccccc1OCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2016.04.087
23625384 86401 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 409 6 2 5 3.0 CNc1ccnc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm070714l
CHEMBL231373 86401 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 409 6 2 5 3.0 CNc1ccnc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm070714l
10576554 172856 None 0 Human Functional pEC50 = 6.5 6.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 475 7 1 5 4.6 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CF)(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
CHEMBL45094 172856 None 0 Human Functional pEC50 = 6.5 6.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 475 7 1 5 4.6 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CF)(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
130431325 172515 None 0 Human Functional pEC50 = 7.5 7.5 2 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 439 8 1 4 5.0 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4476699 172515 None 0 Human Functional pEC50 = 7.5 7.5 2 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 439 8 1 4 5.0 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL5077564 216994 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(CC6CCC6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
56850663 71528 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 375 7 1 5 2.1 O=C1C2CSCN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926748 71528 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 375 7 1 5 2.1 O=C1C2CSCN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962696 71528 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 375 7 1 5 2.1 O=C1C2CSCN2C(=O)N1CCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
1220 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
31 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
7 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
CHEMBL56 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.0c00814
1220 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.9b00062
31 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.9b00062
7 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.9b00062
CHEMBL56 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/acs.jmedchem.9b00062
44461162 208009 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 413 7 1 5 2.9 O=C(NCCCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL81095 208009 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 413 7 1 5 2.9 O=C(NCCCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
42606688 17860 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 5 2.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3cnn4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1259017 17860 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 5 2.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3cnn4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL5089999 217726 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCN3CCN(C4=CC5CC(CC6CCN(Cc7ccccc7)CC6)C(=O)C5C=C4)CC3)c2c1 10.1016/j.ejmech.2021.114045
132256796 182905 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 454 8 1 4 4.6 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4790662 182905 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 454 8 1 4 4.6 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
10093856 77117 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 424 10 1 5 2.5 CC(=O)Nc1cccc(N2CCN(CCCCN(C)S(=O)(=O)CC(C)C)CC2)c1 10.1021/jm0508641
CHEMBL207478 77117 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 424 10 1 5 2.5 CC(=O)Nc1cccc(N2CCN(CCCCN(C)S(=O)(=O)CC(C)C)CC2)c1 10.1021/jm0508641
52943589 17920 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 371 5 2 5 2.7 Cc1ccc(CNCC2(O)CC3CCC(C2)N3C(=O)c2ccsc2)nc1 10.1021/jm100835q
CHEMBL1259184 17920 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 371 5 2 5 2.7 Cc1ccc(CNCC2(O)CC3CCC(C2)N3C(=O)c2ccsc2)nc1 10.1021/jm100835q
1220 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm070714l
31 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm070714l
7 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm070714l
CHEMBL56 187 None 44 Human Functional pEC50 = 7.5 7.5 -1 9
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm070714l
16109511 84286 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 377 8 1 3 5.5 CCC1(C)Cc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
CHEMBL221131 84286 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 377 8 1 3 5.5 CCC1(C)Cc2cccc(OCCNCc3cccc(C4=CCCC4)c3)c2O1 10.1021/jm061180b
132256760 183350 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 437 8 2 4 4.1 CNc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4796345 183350 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 437 8 2 4 4.1 CNc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
137658253 159724 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 422 4 0 7 3.1 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2=O 10.1016/j.bmc.2017.07.040
CHEMBL4103509 159724 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 422 4 0 7 3.1 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2=O 10.1016/j.bmc.2017.07.040
5 139 None 45 Rat Functional pEC50 = 6.5 6.5 -19 26
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm800176x
5202 139 None 45 Rat Functional pEC50 = 6.5 6.5 -19 26
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm800176x
CHEMBL39 139 None 45 Rat Functional pEC50 = 6.5 6.5 -19 26
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm800176x
DB08839 139 None 45 Rat Functional pEC50 = 6.5 6.5 -19 26
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm800176x
24949693 182410 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
ChEMBL 370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 10.1021/jm800176x
CHEMBL478413 182410 None 0 Rat Functional pEC50 = 6.5 6.5 - 1
Agonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor in CRL:CD(SD)BR-COBS rat hippocampus assessed as increase in [35S]GTPgammaS binding
ChEMBL 370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 10.1021/jm800176x
CHEMBL5086277 217511 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6cccc(C(F)(F)F)c6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
208951 83077 None 29 Human Functional pEC50 = 6.5 6.5 -112 2
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 385 4 1 4 4.1 O=c1[nH]c2cccc(N3CCN(Cc4cccc(-c5ccccc5)c4)CC3)c2o1 10.1021/jm061180b
CHEMBL218166 83077 None 29 Human Functional pEC50 = 6.5 6.5 -112 2
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 385 4 1 4 4.1 O=c1[nH]c2cccc(N3CCN(Cc4cccc(-c5ccccc5)c4)CC3)c2o1 10.1021/jm061180b
44408882 75028 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 381 7 2 3 4.4 CC(C)CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL203282 75028 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 381 7 2 3 4.4 CC(C)CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
9799121 75539 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 363 7 2 3 4.4 CC(C)N1CC(CNCCCc2c[nH]c3ccccc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL204331 75539 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 363 7 2 3 4.4 CC(C)N1CC(CNCCCc2c[nH]c3ccccc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
10694238 101324 None 0 Human Functional pEC50 = 7.5 7.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 436 6 1 4 4.0 Cc1cc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc(N(C)C)c1 10.1021/jm9806906
CHEMBL296289 101324 None 0 Human Functional pEC50 = 7.5 7.5 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 436 6 1 4 4.0 Cc1cc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc(N(C)C)c1 10.1021/jm9806906
44408883 74735 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 321 5 2 3 3.2 CN1CC(CNCCc2c[nH]c3ccccc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL203067 74735 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 321 5 2 3 3.2 CN1CC(CNCCc2c[nH]c3ccccc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
9863750 83195 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 361 7 1 3 4.9 C1=C(c2cccc(CNCCOc3cccc4c3OC3(CC3)C4)c2)CCC1 10.1021/jm061180b
CHEMBL218313 83195 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 361 7 1 3 4.9 C1=C(c2cccc(CNCCOc3cccc4c3OC3(CC3)C4)c2)CCC1 10.1021/jm061180b
44537919 200592 None 0 Human Functional pEC50 = 6.5 6.5 1 3
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL574700 200592 None 0 Human Functional pEC50 = 6.5 6.5 1 3
Agonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
132256814 180624 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 454 8 1 4 4.6 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1021/acs.jmedchem.0c00814
CHEMBL4753394 180624 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 454 8 1 4 4.6 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)cc1 10.1021/acs.jmedchem.0c00814
11188024 145669 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4c(ccc5ncccc45)C3)c2c1 10.1016/j.bmcl.2007.03.049
CHEMBL391531 145669 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 375 5 2 3 4.4 Fc1ccc2[nH]cc(CCCNC3COc4c(ccc5ncccc45)C3)c2c1 10.1016/j.bmcl.2007.03.049
CHEMBL5076277 216914 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None O=C(CCC1CCN(Cc2ccccc2)CC1)c1ccc(N2CCN(CCCCc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.ejmech.2021.114045
44408853 141306 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 373 5 2 3 4.0 CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2cc(Cl)ccc21 10.1016/j.bmcl.2005.11.054
CHEMBL382857 141306 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 373 5 2 3 4.0 CN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2cc(Cl)ccc21 10.1016/j.bmcl.2005.11.054
46227762 202115 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 435 7 2 3 4.2 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
CHEMBL592953 202115 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 435 7 2 3 4.2 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
42606572 17859 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccc4o3)CC2)nc1 10.1021/jm100835q
CHEMBL1259016 17859 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccc4o3)CC2)nc1 10.1021/jm100835q
129186549 158952 None 0 Human Functional pEC50 = 7.5 7.5 -4 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 423 4 1 6 4.0 Cc1nc2n(c(=O)c1CCN1CCC(c3cccc4sccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4094926 158952 None 0 Human Functional pEC50 = 7.5 7.5 -4 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 423 4 1 6 4.0 Cc1nc2n(c(=O)c1CCN1CCC(c3cccc4sccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
56850924 71546 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 348 8 1 5 2.8 O=C1CSC(=O)N1CCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1926758 71546 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 348 8 1 5 2.8 O=C1CSC(=O)N1CCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
CHEMBL1962806 71546 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIAAgonist activity at human 5HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP production pretreated 20 mins before forskolin challenge measured after 2 hrs by RIA
ChEMBL 348 8 1 5 2.8 O=C1CSC(=O)N1CCCCCNCC1CCc2ccccc2O1 10.1021/jm2007886
127049847 140405 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 469 8 1 4 5.0 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1Cl 10.1016/j.bmcl.2016.04.087
CHEMBL3806224 140405 None 0 Human Functional pEC50 = 7.5 7.5 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 469 8 1 4 5.0 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1Cl 10.1016/j.bmcl.2016.04.087
145961458 161492 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4cccc5c(N)c6c(nc45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4126486 161492 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4cccc5c(N)c6c(nc45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
122183778 122312 None 0 Human Functional pEC50 = 6.5 6.5 -51 2
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 434 8 2 6 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cnc3ccccc3c2)CC1 10.1021/acs.jmedchem.5b00776
CHEMBL3597649 122312 None 0 Human Functional pEC50 = 6.5 6.5 -51 2
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 434 8 2 6 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cnc3ccccc3c2)CC1 10.1021/acs.jmedchem.5b00776
46230654 202894 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at 5HT1A receptor by GTPgammaS assayAgonist activity at 5HT1A receptor by GTPgammaS assay
ChEMBL 289 3 1 2 4.2 Fc1ccccc1Oc1cccc(F)c1C1CCNCC1 10.1016/j.bmcl.2009.12.023
CHEMBL598346 202894 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at 5HT1A receptor by GTPgammaS assayAgonist activity at 5HT1A receptor by GTPgammaS assay
ChEMBL 289 3 1 2 4.2 Fc1ccccc1Oc1cccc(F)c1C1CCNCC1 10.1016/j.bmcl.2009.12.023
46230654 202894 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
ChEMBL 289 3 1 2 4.2 Fc1ccccc1Oc1cccc(F)c1C1CCNCC1 10.1016/j.bmcl.2010.11.066
CHEMBL598346 202894 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
ChEMBL 289 3 1 2 4.2 Fc1ccccc1Oc1cccc(F)c1C1CCNCC1 10.1016/j.bmcl.2010.11.066
2965107 44967 None 5 Human Functional pEC50 = 4.5 4.5 - 1
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 314 5 3 2 2.7 O=C(O)C1CCCCC1C(=O)NCCc1c[nH]c2ccccc12 nan
CHEMBL1523325 44967 None 5 Human Functional pEC50 = 4.5 4.5 - 1
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 314 5 3 2 2.7 O=C(O)C1CCCCC1C(=O)NCCc1c[nH]c2ccccc12 nan
9881324 28380 None 3 Human Functional pEC50 = 7.5 7.5 1 4
Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.
ChEMBL 244 3 1 2 2.8 COc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm00101a032
CHEMBL137485 28380 None 3 Human Functional pEC50 = 7.5 7.5 1 4
Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.
ChEMBL 244 3 1 2 2.8 COc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm00101a032
11739995 18058 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 363 8 2 3 4.5 Fc1ccc2[nH]cc(CCCNCCOc3cccc4ncccc34)c2c1 10.1021/jm0304010
CHEMBL126536 18058 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 363 8 2 3 4.5 Fc1ccc2[nH]cc(CCCNCCOc3cccc4ncccc34)c2c1 10.1021/jm0304010
42606103 17901 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3C)CC2)nc1 10.1021/jm100835q
CHEMBL1259122 17901 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3sccc3C)CC2)nc1 10.1021/jm100835q
46225208 201924 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 433 6 2 3 4.3 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)C1CCC1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL591561 201924 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 433 6 2 3 4.3 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)C1CCC1)CO3 10.1016/j.bmcl.2009.10.134
130431296 174532 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 457 8 1 4 4.9 CCc1cccc(N2CCN(CC(F)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.9b00607
CHEMBL4553059 174532 None 0 Human Functional pEC50 = 6.5 6.5 1 2
Agonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5-HT1A receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 457 8 1 4 4.9 CCc1cccc(N2CCN(CC(F)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.9b00607
CHEMBL5076629 216941 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4cccc5c4C(=O)C(CC4CCN(Cc6ccccc6)CC4)C5)CC3)c2c1 10.1016/j.ejmech.2021.114045
15980808 202236 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 447 7 2 3 4.2 O=C1NCCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL593865 202236 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 447 7 2 3 4.2 O=C1NCCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
49782388 17870 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 495 5 1 3 3.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccc4[te]3)CC2)nc1 10.1021/jm100835q
CHEMBL1259036 17870 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 495 5 1 3 3.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccc4[te]3)CC2)nc1 10.1021/jm100835q
127048532 140319 None 0 Human Functional pEC50 = 6.4 6.4 3 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 453 8 1 4 4.5 CNC(=O)c1cc(F)cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805262 140319 None 0 Human Functional pEC50 = 6.4 6.4 3 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 453 8 1 4 4.5 CNC(=O)c1cc(F)cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
23625381 86308 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 430 6 1 4 3.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ncc(C(F)F)cn2)CC1 10.1021/jm070714l
CHEMBL231272 86308 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 430 6 1 4 3.9 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ncc(C(F)F)cn2)CC1 10.1021/jm070714l
17371 170370 None 9 Human Functional pEC50 = 5.4 5.4 - 1
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 234 5 1 1 3.2 CCN(CC)CCc1c[nH]c2cc(F)ccc12 10.1021/jm000339w
CHEMBL444612 170370 None 9 Human Functional pEC50 = 5.4 5.4 - 1
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 234 5 1 1 3.2 CCN(CC)CCc1c[nH]c2cc(F)ccc12 10.1021/jm000339w
162644356 181884 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 380 7 0 5 2.1 O=C(c1ccccc1)N(CCCN1CCN(c2ccccn2)CC1)C1COC1 10.1016/j.ejmech.2020.112214
CHEMBL4777749 181884 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 380 7 0 5 2.1 O=C(c1ccccc1)N(CCCN1CCN(c2ccccn2)CC1)C1COC1 10.1016/j.ejmech.2020.112214
2477 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
2477.0 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
36 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
437 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
CHEMBL49 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
DB00490 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
132247308 181867 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 451 8 2 4 3.2 NC(=O)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4777581 181867 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 451 8 2 4 3.2 NC(=O)c1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
132257275 180739 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 425 7 1 4 4.0 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4754941 180739 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 425 7 1 4 4.0 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
9952481 141444 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 393 4 2 4 4.3 COc1cccc2c1OC(CN1CC=C(c3c[nH]c4ccc(F)cc34)CC1)CN2 10.1016/j.bmcl.2005.11.054
CHEMBL383688 141444 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 393 4 2 4 4.3 COc1cccc2c1OC(CN1CC=C(c3c[nH]c4ccc(F)cc34)CC1)CN2 10.1016/j.bmcl.2005.11.054
11741361 2830 None 36 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/jm070714l
3924 2830 None 36 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/jm070714l
CHEMBL230963 2830 None 36 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/jm070714l
42606455 17897 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 403 5 1 5 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccsc4s3)CC2)nc1 10.1021/jm100835q
CHEMBL1259109 17897 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 403 5 1 5 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccsc4s3)CC2)nc1 10.1021/jm100835q
145969406 164924 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 498 7 0 6 4.7 CC(=O)c1c(OCCCN2CCN(c3ccccc3Br)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.bmc.2017.12.016
CHEMBL4218720 164924 None 0 Rat Functional pEC50 = 7.4 7.4 - 1
Agonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 498 7 0 6 4.7 CC(=O)c1c(OCCCN2CCN(c3ccccc3Br)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.bmc.2017.12.016
132247302 180567 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4752833 180567 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1 10.1021/acs.jmedchem.0c00814
10600032 172647 None 0 Human Functional pEC50 = 7.4 7.4 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 459 6 2 6 3.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(O)(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
CHEMBL44841 172647 None 0 Human Functional pEC50 = 7.4 7.4 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 459 6 2 6 3.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(O)(CNCc2cccc(-n3cccn3)n2)CC1 10.1021/jm9806906
44433258 89116 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Antagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as 5-HT-stimulated [35S]GTPgammaS bindingAntagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 302 7 3 3 3.2 OC(CCNC1CCCCC1)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2007.07.086
CHEMBL236518 89116 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Antagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as 5-HT-stimulated [35S]GTPgammaS bindingAntagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 302 7 3 3 3.2 OC(CCNC1CCCCC1)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2007.07.086
5 139 None 45 Human Functional pEC50 = 6.4 6.4 -33 26
Agonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assayAgonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
5202 139 None 45 Human Functional pEC50 = 6.4 6.4 -33 26
Agonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assayAgonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
CHEMBL39 139 None 45 Human Functional pEC50 = 6.4 6.4 -33 26
Agonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assayAgonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
DB08839 139 None 45 Human Functional pEC50 = 6.4 6.4 -33 26
Agonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assayAgonist activity at human 5-HT1A receptor expressed in U2OS cells assessed as beta-arrestin recruitment incubated for 5 hrs by Tango assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2022.114218
15980853 202523 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 411 5 3 3 3.3 O=C1NCCc2cc(F)c3c(c21)CC(NCCCc1c[nH]c2ccc(F)cc12)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL595744 202523 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 411 5 3 3 3.3 O=C1NCCc2cc(F)c3c(c21)CC(NCCCc1c[nH]c2ccc(F)cc12)CO3 10.1016/j.bmcl.2009.10.134
11313610 117918 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 333 8 3 2 4.3 c1ccc2c(CCCNCCOc3cccc4[nH]ccc34)c[nH]c2c1 10.1021/jm0304010
CHEMBL340301 117918 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 333 8 3 2 4.3 c1ccc2c(CCCNCCOc3cccc4[nH]ccc34)c[nH]c2c1 10.1021/jm0304010
162662080 181525 None 0 Human Functional pEC50 = 8.4 8.4 6 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 466 6 1 5 3.7 O=C1NCC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)c2cc(F)ccc21 10.1016/j.ejmech.2020.112572
CHEMBL4763837 181525 None 0 Human Functional pEC50 = 8.4 8.4 6 3
Agonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader methodAgonist activity at 5-HT1A receptor (unknown origin) preincubated for 60 mins followed by addition of Eu-cAMP and measured after 60 mins by plate reader method
ChEMBL 466 6 1 5 3.7 O=C1NCC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)c2cc(F)ccc21 10.1016/j.ejmech.2020.112572
127049864 140369 None 0 Human Functional pEC50 = 8.4 8.4 2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805860 140369 None 0 Human Functional pEC50 = 8.4 8.4 2 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cccc(OCCCCN2CCN(c3nsc4ccccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
129186554 157910 None 0 Human Functional pEC50 = 8.3 8.3 -3 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 408 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2 10.1016/j.bmc.2017.07.040
CHEMBL4083333 157910 None 0 Human Functional pEC50 = 8.3 8.3 -3 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 408 4 0 6 3.5 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2 10.1016/j.bmc.2017.07.040
9950482 117090 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 354 8 2 3 3.8 Fc1ccc2[nH]cc(CCCNCCOc3cccc4c3OCC4)c2c1 10.1021/jm0304010
CHEMBL338982 117090 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 354 8 2 3 3.8 Fc1ccc2[nH]cc(CCCNCCOc3cccc4c3OCC4)c2c1 10.1021/jm0304010
44591319 189821 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 8 2 5 3.4 COCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1 10.1016/j.bmcl.2008.12.087
CHEMBL515573 189821 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 8 2 5 3.4 COCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1 10.1016/j.bmcl.2008.12.087
132256734 179673 None 1 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 408 7 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4741857 179673 None 1 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 408 7 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL5087878 217614 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccccc4C(=O)CCC4CCN(Cc5ccccc5)CC4)CC3)c2c1 10.1016/j.ejmech.2021.114045
10692801 168011 None 0 Human Functional pEC50 = 6.4 6.4 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 407 6 1 3 4.2 CCc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm9806906
CHEMBL431332 168011 None 0 Human Functional pEC50 = 6.4 6.4 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 407 6 1 3 4.2 CCc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm9806906
2477 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2008.12.087
2477.0 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2008.12.087
36 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2008.12.087
437 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2008.12.087
CHEMBL49 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2008.12.087
DB00490 745 None 38 Human Functional pEC50 = 7.4 7.4 -2 20
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/j.bmcl.2008.12.087
11221557 18046 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 342 9 2 3 3.9 COc1ccccc1OCCNCCCc1c[nH]c2ccc(F)cc12 10.1021/jm0304010
CHEMBL126484 18046 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 342 9 2 3 3.9 COc1ccccc1OCCNCCCc1c[nH]c2ccc(F)cc12 10.1021/jm0304010
9953959 75312 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 421 5 1 4 4.7 CCN1CC(CN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)Oc2c(OC)cccc21 10.1016/j.bmcl.2005.11.054
CHEMBL203726 75312 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 421 5 1 4 4.7 CCN1CC(CN2CC=C(c3c[nH]c4ccc(F)cc34)CC2)Oc2c(OC)cccc21 10.1016/j.bmcl.2005.11.054
42606105 17900 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(C)s3)CC2)nc1 10.1021/jm100835q
CHEMBL1259121 17900 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 361 5 1 4 3.5 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(C)s3)CC2)nc1 10.1021/jm100835q
145976348 163836 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 443 8 1 7 3.2 CNC(=O)c1cncc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2018.01.038
CHEMBL4205326 163836 None 0 Human Functional pEC50 = 7.4 7.4 1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 443 8 1 7 3.2 CNC(=O)c1cncc(OCCCCN2CCN(c3nsc4cc(F)ccc34)CC2)c1 10.1016/j.bmcl.2018.01.038
23625534 151386 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 443 6 2 5 3.7 CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ncc1Cl 10.1021/jm070714l
CHEMBL396062 151386 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 443 6 2 5 3.7 CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ncc1Cl 10.1021/jm070714l
132257061 180133 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4747425 180133 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c00814
168295509 192623 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assay
ChEMBL 449 6 1 8 3.0 COc1cc2ncnc(N3CCC(CN4CCN(c5ccccc5O)CC4)C3)c2cc1OC 10.1016/j.ejmech.2022.114218
CHEMBL5209283 192623 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP production incubated for 40 mins by TR-FRET assay
ChEMBL 449 6 1 8 3.0 COc1cc2ncnc(N3CCC(CN4CCN(c5ccccc5O)CC4)C3)c2cc1OC 10.1016/j.ejmech.2022.114218
122183765 122300 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 452 8 1 5 4.2 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cnc3ccccc3c2)CC1 10.1021/acs.jmedchem.5b00776
CHEMBL3597637 122300 None 0 Human Functional pEC50 = 7.4 7.4 -1 3
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 452 8 1 5 4.2 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cnc3ccccc3c2)CC1 10.1021/acs.jmedchem.5b00776
5 139 None 45 Human Functional pEC50 = 7.4 7.4 -33 26
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(95)00417-R
5202 139 None 45 Human Functional pEC50 = 7.4 7.4 -33 26
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(95)00417-R
CHEMBL39 139 None 45 Human Functional pEC50 = 7.4 7.4 -33 26
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(95)00417-R
DB08839 139 None 45 Human Functional pEC50 = 7.4 7.4 -33 26
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/0960-894X(95)00417-R
132247307 180516 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 481 8 2 4 4.6 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4752177 180516 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 481 8 2 4 4.6 CC(=O)Nc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
46225263 202160 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 483 6 2 3 4.6 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)C(=O)c1ccccc1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL593281 202160 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 483 6 2 3 4.6 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)C(=O)c1ccccc1)CO3 10.1016/j.bmcl.2009.10.134
11313754 16854 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 338 10 2 3 4.2 COc1ccccc1OCCNCCCCc1c[nH]c2ccccc12 10.1021/jm0304010
CHEMBL124818 16854 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 338 10 2 3 4.2 COc1ccccc1OCCNCCCCc1c[nH]c2ccccc12 10.1021/jm0304010
53248258 62057 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 441 8 1 5 4.2 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm200288r
CHEMBL1774538 62057 None 0 Human Functional pEC50 = 6.4 6.4 -1 3
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 441 8 1 5 4.2 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm200288r
23626164 86400 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 410 6 1 5 3.0 COc1ccnc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm070714l
CHEMBL231372 86400 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 410 6 1 5 3.0 COc1ccnc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm070714l
24944943 102565 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 381 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCNCCOc1cccc2ccccc12 10.1021/jm400766k
CHEMBL2431038 102565 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 381 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCNCCOc1cccc2ccccc12 10.1021/jm400766k
CHEMBL3040400 102565 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 381 9 1 4 3.0 O=C1C2CCCN2C(=O)N1CCCCNCCOc1cccc2ccccc12 10.1021/jm400766k
164619127 185631 None 0 Human Functional pEC50 = 7.3 7.3 -8 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185631 None 0 Human Functional pEC50 = 7.3 7.3 -8 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
132256759 179694 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 409 7 1 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccnc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4742122 179694 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 409 7 1 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccnc2)CC1 10.1021/acs.jmedchem.9b00062
164619127 185631 None 0 Human Functional pEC50 = 7.3 7.3 -8 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 185631 None 0 Human Functional pEC50 = 7.3 7.3 -8 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
137660385 159181 None 0 Human Functional pEC50 = 6.4 6.4 -22 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nccc4sccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4097395 159181 None 0 Human Functional pEC50 = 6.4 6.4 -22 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3nccc4sccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
162648066 179949 None 0 Human Functional pEC50 = 6.3 6.3 1 3
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 433 8 0 3 5.1 CCCN(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)C(=O)c1ccccc1 10.1016/j.ejmech.2020.112214
CHEMBL4745192 179949 None 0 Human Functional pEC50 = 6.3 6.3 1 3
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 433 8 0 3 5.1 CCCN(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)C(=O)c1ccccc1 10.1016/j.ejmech.2020.112214
11394411 17863 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 364 8 2 4 3.9 Fc1ccc2[nH]cc(CCCNCCOc3cccc4nccnc34)c2c1 10.1021/jm0304010
CHEMBL125902 17863 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 364 8 2 4 3.9 Fc1ccc2[nH]cc(CCCNCCOc3cccc4nccnc34)c2c1 10.1021/jm0304010
42605992 17906 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 4 3.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)s3)CC2)nc1 10.1021/jm100835q
CHEMBL1259138 17906 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 4 3.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)s3)CC2)nc1 10.1021/jm100835q
162652689 180571 None 0 Human Functional pEC50 = 7.3 7.3 11 3
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 433 7 0 3 5.1 CC(C)N(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)C(=O)c1ccccc1 10.1016/j.ejmech.2020.112214
CHEMBL4752859 180571 None 0 Human Functional pEC50 = 7.3 7.3 11 3
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 433 7 0 3 5.1 CC(C)N(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)C(=O)c1ccccc1 10.1016/j.ejmech.2020.112214
16109484 84388 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 365 9 1 3 5.6 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCCC2)c1 10.1021/jm061180b
CHEMBL221743 84388 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 365 9 1 3 5.6 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCCC2)c1 10.1021/jm061180b
132256713 182576 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 407 7 1 3 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCCc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4786537 182576 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 407 7 1 3 4.0 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCCc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
11722647 207880 None 0 Human Functional pEC50 = 6.3 6.3 -41 4
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
ChEMBL 305 4 1 4 3.0 CN(C)CCc1c[nH]c2ccc(-n3cnc4cccnc43)cc12 10.1016/0960-894X(95)00417-R
CHEMBL80189 207880 None 0 Human Functional pEC50 = 6.3 6.3 -41 4
Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pigCompound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
ChEMBL 305 4 1 4 3.0 CN(C)CCc1c[nH]c2ccc(-n3cnc4cccnc43)cc12 10.1016/0960-894X(95)00417-R
164937988 195320 None 4 Human Functional pEC50 = 5.3 5.3 -169 5
Agonist activity at 5-HT1A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT1A receptor (unknown origin) by calcium flux assay
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
CHEMBL5400876 195320 None 4 Human Functional pEC50 = 5.3 5.3 -169 5
Agonist activity at 5-HT1A receptor (unknown origin) by calcium flux assayAgonist activity at 5-HT1A receptor (unknown origin) by calcium flux assay
ChEMBL 338 5 0 5 3.4 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1021/acs.jmedchem.3c00734
127051040 140366 None 0 Human Functional pEC50 = 6.3 6.3 -28 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 491 12 1 4 5.9 CCCCCNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805826 140366 None 0 Human Functional pEC50 = 6.3 6.3 -28 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 491 12 1 4 5.9 CCCCCNC(=O)c1cccc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL5078629 217061 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccoc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
5487088 208305 None 32 Rat Functional pEC50 = 7.3 7.3 -19 2
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 351 5 2 5 3.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(Nc3ncccc3[N+](=O)[O-])cc12 10.1021/jm00042a003
CHEMBL83597 208305 None 32 Rat Functional pEC50 = 7.3 7.3 -19 2
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 351 5 2 5 3.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(Nc3ncccc3[N+](=O)[O-])cc12 10.1021/jm00042a003
52945241 17933 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 385 5 1 3 3.6 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC3C5)C4)CC2)nc1 10.1021/jm100835q
CHEMBL1259223 17933 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 385 5 1 3 3.6 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC3C5)C4)CC2)nc1 10.1021/jm100835q
132256759 179694 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 409 7 1 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccnc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4742122 179694 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 409 7 1 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccnc2)CC1 10.1021/acs.jmedchem.9b00062
44290346 177480 None 0 Human Functional pEC50 = 7.3 7.3 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 436 6 1 4 4.0 Cc1ccc(N(C)C)nc1CNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/jm9806906
CHEMBL46379 177480 None 0 Human Functional pEC50 = 7.3 7.3 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 436 6 1 4 4.0 Cc1ccc(N(C)C)nc1CNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/jm9806906
145986552 166838 None 0 Human Functional pEC50 = 7.3 7.3 11 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 453 6 0 5 4.8 O=C1c2ccc(Cl)cc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4283369 166838 None 0 Human Functional pEC50 = 7.3 7.3 11 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 453 6 0 5 4.8 O=C1c2ccc(Cl)cc2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
132257112 183470 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4797752 183470 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.0c00814
168281650 191311 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assay
ChEMBL 467 6 0 7 3.9 COc1cc2ncnc(N3CCC(CN4CCN(c5ccc(Cl)cc5)CC4)C3)c2cc1OC 10.1016/j.ejmech.2022.114218
CHEMBL5189417 191311 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as stimulation of ERK1/2 phosphorylation incubated for 15 mins by Alpha LISA assay
ChEMBL 467 6 0 7 3.9 COc1cc2ncnc(N3CCC(CN4CCN(c5ccc(Cl)cc5)CC4)C3)c2cc1OC 10.1016/j.ejmech.2022.114218
155535272 172134 None 0 Human Functional pEC50 = 7.3 7.3 4 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 280 5 0 2 3.8 CCCCN1CCN(c2cccc(CC)c2Cl)CC1 10.1021/acs.jmedchem.6b00860
CHEMBL4471669 172134 None 0 Human Functional pEC50 = 7.3 7.3 4 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 280 5 0 2 3.8 CCCCN1CCN(c2cccc(CC)c2Cl)CC1 10.1021/acs.jmedchem.6b00860
52946036 17934 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 433 5 1 3 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(Cl)(C5)C3)C4)CC2)nc1 10.1021/jm100835q
CHEMBL1259224 17934 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 433 5 1 3 4.4 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(Cl)(C5)C3)C4)CC2)nc1 10.1021/jm100835q
137659145 159530 None 0 Human Functional pEC50 = 6.3 6.3 -58 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 443 4 0 7 3.6 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2Cl 10.1016/j.bmc.2017.07.040
CHEMBL4101115 159530 None 0 Human Functional pEC50 = 6.3 6.3 -58 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 443 4 0 7 3.6 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2Cl 10.1016/j.bmc.2017.07.040
46224739 201569 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 447 8 2 3 4.6 O=C1NCc2ccc3c(c21)CC(N(CCCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL589141 201569 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 447 8 2 3 4.6 O=C1NCc2ccc3c(c21)CC(N(CCCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL5088366 217644 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(CC6CCCC6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
10813865 178126 None 0 Human Functional pEC50 = 8.3 8.3 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 460 6 1 5 5.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3nccs3)n2)CC1 10.1021/jm9806906
CHEMBL46467 178126 None 0 Human Functional pEC50 = 8.3 8.3 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 460 6 1 5 5.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3nccs3)n2)CC1 10.1021/jm9806906
127049866 140358 None 1 Human Functional pEC50 = 8.3 8.3 17 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 423 8 1 5 4.2 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4sccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3805704 140358 None 1 Human Functional pEC50 = 8.3 8.3 17 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 423 8 1 5 4.2 CNC(=O)c1cccc(OCCCCN2CCN(c3cccc4sccc34)CC2)c1 10.1016/j.bmcl.2016.04.087
10765698 165339 None 0 Human Functional pEC50 = 8.3 8.3 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 443 6 1 4 5.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3ccco3)n2)CC1 10.1021/jm9806906
CHEMBL42294 165339 None 0 Human Functional pEC50 = 8.3 8.3 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 443 6 1 4 5.3 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3ccco3)n2)CC1 10.1021/jm9806906
10091417 208014 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 384 6 0 5 3.4 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL543377 208014 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 384 6 0 5 3.4 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL81118 208014 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 384 6 0 5 3.4 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
5 139 None 45 Human Functional pEC50 = 8.2 8.2 -33 26
Agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric methodAgonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
5202 139 None 45 Human Functional pEC50 = 8.2 8.2 -33 26
Agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric methodAgonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
CHEMBL39 139 None 45 Human Functional pEC50 = 8.2 8.2 -33 26
Agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric methodAgonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
DB08839 139 None 45 Human Functional pEC50 = 8.2 8.2 -33 26
Agonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric methodAgonist activity at human 5-HT1AR expressed in CHO-K1 cells assessed as increase in calcium flux by fluorimetric method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2018.01.002
10047814 104920 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 421 6 0 6 2.7 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
CHEMBL311015 104920 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 421 6 0 6 2.7 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
10764513 101239 None 0 Human Functional pEC50 = 8.2 8.2 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 418 6 1 4 3.8 Cc1ccc(C(=O)N2CCC(F)(CNCc3cccc(N(C)C)n3)CC2)cc1Cl 10.1021/jm9806906
CHEMBL295662 101239 None 0 Human Functional pEC50 = 8.2 8.2 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 418 6 1 4 3.8 Cc1ccc(C(=O)N2CCC(F)(CNCc3cccc(N(C)C)n3)CC2)cc1Cl 10.1021/jm9806906
10575934 166237 None 0 Human Functional pEC50 = 8.2 8.2 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 459 6 1 4 5.8 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cccs3)n2)CC1 10.1021/jm9806906
CHEMBL42618 166237 None 0 Human Functional pEC50 = 8.2 8.2 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 459 6 1 4 5.8 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(-c3cccs3)n2)CC1 10.1021/jm9806906
145992523 167109 None 0 Human Functional pEC50 = 8.2 8.2 5 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 453 6 0 5 4.8 O=C1c2cccc(Cl)c2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4288388 167109 None 0 Human Functional pEC50 = 8.2 8.2 5 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 453 6 0 5 4.8 O=C1c2cccc(Cl)c2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
5 139 None 45 Human Functional pEC50 = 8.2 8.2 -33 26
Agonist activity at human 5HT1A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT1A 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 = 8.2 8.2 -33 26
Agonist activity at human 5HT1A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT1A 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 = 8.2 8.2 -33 26
Agonist activity at human 5HT1A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT1A 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 = 8.2 8.2 -33 26
Agonist activity at human 5HT1A receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assayAgonist activity at human 5HT1A 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
1220 187 None 44 Human Functional pEC50 = 8.2 8.2 -1 9
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm000339w
31 187 None 44 Human Functional pEC50 = 8.2 8.2 -1 9
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm000339w
7 187 None 44 Human Functional pEC50 = 8.2 8.2 -1 9
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm000339w
CHEMBL56 187 None 44 Human Functional pEC50 = 8.2 8.2 -1 9
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm000339w
9887537 84379 None 31 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm061180b
CHEMBL221692 84379 None 31 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm061180b
CHEMBL4751170 84379 None 31 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm061180b
156021805 178260 None 0 Human Functional pEC50 = 8.2 8.2 24 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 432 6 0 8 3.2 N#Cc1ccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc2c1 10.1016/j.bmcl.2020.127027
CHEMBL4648979 178260 None 0 Human Functional pEC50 = 8.2 8.2 24 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 432 6 0 8 3.2 N#Cc1ccn2c(=O)n(CCCCN3CCN(c4cccc5sccc45)CC3)nc2c1 10.1016/j.bmcl.2020.127027
9999722 164277 None 0 Human Functional pEC50 = 7.3 7.3 -112 2
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 50-550Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 50-550
ChEMBL 378 6 2 4 2.4 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(c4ccccc4)CC3)cc12 10.1016/0960-894X(95)00091-7
CHEMBL421064 164277 None 0 Human Functional pEC50 = 7.3 7.3 -112 2
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 50-550Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 50-550
ChEMBL 378 6 2 4 2.4 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(c4ccccc4)CC3)cc12 10.1016/0960-894X(95)00091-7
42606335 17925 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 411 6 1 5 3.8 COc1c(C(=O)N2CCC(F)(CNCc3ccc(C)cn3)CC2)csc1Cl 10.1021/jm100835q
CHEMBL1259198 17925 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 411 6 1 5 3.8 COc1c(C(=O)N2CCC(F)(CNCc3ccc(C)cn3)CC2)csc1Cl 10.1021/jm100835q
5 139 None 45 Human Functional pEC50 = 7.3 7.3 -33 26
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b00062
5202 139 None 45 Human Functional pEC50 = 7.3 7.3 -33 26
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b00062
CHEMBL39 139 None 45 Human Functional pEC50 = 7.3 7.3 -33 26
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b00062
DB08839 139 None 45 Human Functional pEC50 = 7.3 7.3 -33 26
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.9b00062
44591317 180756 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 8 3 5 3.2 OCCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1 10.1016/j.bmcl.2008.12.087
CHEMBL475502 180756 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 379 8 3 5 3.2 OCCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1 10.1016/j.bmcl.2008.12.087
164619170 185707 None 0 Human Functional pEC50 = 7.3 7.3 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185707 None 0 Human Functional pEC50 = 7.3 7.3 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
6088 119906 None 24 Human Functional pEC50 = 5.3 5.3 -100 2
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 174 3 2 1 1.9 CNCCc1c[nH]c2ccccc12 nan
CHEMBL348588 119906 None 24 Human Functional pEC50 = 5.3 5.3 -100 2
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 174 3 2 1 1.9 CNCCc1c[nH]c2ccccc12 nan
145962091 161428 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 464 5 2 5 4.8 N#Cc1ccc2[nH]cc(CCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4125732 161428 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 464 5 2 5 4.8 N#Cc1ccc2[nH]cc(CCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
49781928 17919 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 391 5 1 3 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc4ccccc4c3)CC2)nc1 10.1021/jm100835q
CHEMBL1259181 17919 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 391 5 1 3 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc4ccccc4c3)CC2)nc1 10.1021/jm100835q
11515921 76573 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 355 6 3 4 3.3 COc1cccc2c1OC(CNCCc1c[nH]c3ccc(F)cc13)CN2 10.1016/j.bmcl.2005.11.054
CHEMBL206130 76573 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 355 6 3 4 3.3 COc1cccc2c1OC(CNCCc1c[nH]c3ccc(F)cc13)CN2 10.1016/j.bmcl.2005.11.054
164619170 185707 None 0 Human Functional pEC50 = 7.3 7.3 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185707 None 0 Human Functional pEC50 = 7.3 7.3 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
10015045 13657 None 0 Rat Functional pEC50 = 5.3 5.3 -91 3
Ability to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptorAbility to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptor
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00004a011
CHEMBL119455 13657 None 0 Rat Functional pEC50 = 5.3 5.3 -91 3
Ability to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptorAbility to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptor
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00004a011
CHEMBL5069928 216711 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)CC(CC4CCN(Cc6ccccc6)CC4)C5=O)CC3)c2c1 10.1016/j.ejmech.2021.114045
132257112 183470 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4797752 183470 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.0c00814
132256800 182900 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 478 7 1 4 4.8 CC1(C)Cc2cccc(OCCNCC3(F)CCN(C(=O)c4ccc(F)c(Cl)c4)CC3)c2O1 10.1021/acs.jmedchem.0c00814
CHEMBL4790600 182900 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 478 7 1 4 4.8 CC1(C)Cc2cccc(OCCNCC3(F)CCN(C(=O)c4ccc(F)c(Cl)c4)CC3)c2O1 10.1021/acs.jmedchem.0c00814
15980809 202302 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 447 6 2 3 4.4 O=C1NCCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)C1CCC1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL594357 202302 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 447 6 2 3 4.4 O=C1NCCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)C1CCC1)CO3 10.1016/j.bmcl.2009.10.134
42606106 17911 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 393 6 1 5 3.9 CSc1ccc(C(=O)N2CCC(F)(CNCc3ccc(C)cn3)CC2)s1 10.1021/jm100835q
CHEMBL1259153 17911 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 393 6 1 5 3.9 CSc1ccc(C(=O)N2CCC(F)(CNCc3ccc(C)cn3)CC2)s1 10.1021/jm100835q
162654486 180718 None 0 Human Functional pEC50 = 7.3 7.3 125 3
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 366 8 0 4 3.1 CCCN(CCCN1CCN(c2ccccn2)CC1)C(=O)c1ccccc1 10.1016/j.ejmech.2020.112214
CHEMBL4754651 180718 None 0 Human Functional pEC50 = 7.3 7.3 125 3
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 366 8 0 4 3.1 CCCN(CCCN1CCN(c2ccccn2)CC1)C(=O)c1ccccc1 10.1016/j.ejmech.2020.112214
132256715 179515 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 408 7 2 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4740097 179515 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 408 7 2 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL5072034 216761 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6cccnc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
132256811 180049 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2Cl)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4746386 180049 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2Cl)CC1 10.1021/acs.jmedchem.0c00814
3082625 194840 None 4 Rat Functional pEC50 = 7.3 7.3 - 1
Ability to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptorAbility to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptor
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00004a011
CHEMBL53510 194840 None 4 Rat Functional pEC50 = 7.3 7.3 - 1
Ability to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptorAbility to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptor
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00004a011
46180192 204533 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 291 3 0 2 4.0 C=CCOc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm9015763
CHEMBL608728 204533 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 291 3 0 2 4.0 C=CCOc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm9015763
155529450 171540 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 495 8 0 5 4.2 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2019.126667
CHEMBL4463030 171540 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 495 8 0 5 4.2 O=C1c2ccccc2S(=O)(=O)N1CCCCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2019.126667
11164569 118246 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 370 8 2 3 4.8 Fc1cc(OCCNCCCc2c[nH]c3ccc(F)cc23)c2occc2c1 10.1021/jm0304010
CHEMBL340895 118246 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 370 8 2 3 4.8 Fc1cc(OCCNCCCc2c[nH]c3ccc(F)cc23)c2occc2c1 10.1021/jm0304010
132256806 180111 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 438 8 1 4 4.1 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)cc1 10.1021/acs.jmedchem.0c00814
CHEMBL4747083 180111 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 438 8 1 4 4.1 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)cc1 10.1021/acs.jmedchem.0c00814
145963420 161583 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4ccc5c(N)c6c(nc5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4127877 161583 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4ccc5c(N)c6c(nc5c4)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL5071558 216749 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)C(=O)C(CC4CCN(Cc6ccccc6)CC4)C5)CC3)c2c1 10.1016/j.ejmech.2021.114045
CHEMBL5082250 217283 None 2 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccccc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
164628178 186453 None 0 Human Functional pEC50 = 7.2 7.2 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186453 None 0 Human Functional pEC50 = 7.2 7.2 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
5 139 None 45 Human Functional pEC50 = 7.2 7.2 -33 26
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.0c00814
5202 139 None 45 Human Functional pEC50 = 7.2 7.2 -33 26
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.0c00814
CHEMBL39 139 None 45 Human Functional pEC50 = 7.2 7.2 -33 26
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.0c00814
DB08839 139 None 45 Human Functional pEC50 = 7.2 7.2 -33 26
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.0c00814
164628178 186453 None 0 Human Functional pEC50 = 7.2 7.2 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 186453 None 0 Human Functional pEC50 = 7.2 7.2 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
162677207 183664 None 0 Human Functional pEC50 = 6.2 6.2 3 3
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 447 7 0 4 4.0 O=C(c1ccccc1)N(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1COC1 10.1016/j.ejmech.2020.112214
CHEMBL4800286 183664 None 0 Human Functional pEC50 = 6.2 6.2 3 3
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 447 7 0 4 4.0 O=C(c1ccccc1)N(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1COC1 10.1016/j.ejmech.2020.112214
42606456 17902 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 437 5 1 5 5.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3sc4sccc4c3Cl)CC2)nc1 10.1021/jm100835q
CHEMBL1259123 17902 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 437 5 1 5 5.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3sc4sccc4c3Cl)CC2)nc1 10.1021/jm100835q
72699716 115253 None 0 Human Functional pEC50 = 6.2 6.2 -3 3
Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay
ChEMBL 343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344459 115253 None 0 Human Functional pEC50 = 6.2 6.2 -3 3
Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay
ChEMBL 343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
172456322 196371 None 0 Rat Functional pEC50 = 8.2 8.2 1905 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 603 9 0 6 5.4 COc1ccccc1N1CCN(CCCCN2C(=O)C3C(C2=O)C2(C)C(=O)C3(C)C(c3ccccc3)=C2c2ccccc2)CC1 10.1016/j.bmc.2023.117518
CHEMBL5422403 196371 None 0 Rat Functional pEC50 = 8.2 8.2 1905 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 603 9 0 6 5.4 COc1ccccc1N1CCN(CCCCN2C(=O)C3C(C2=O)C2(C)C(=O)C3(C)C(c3ccccc3)=C2c2ccccc2)CC1 10.1016/j.bmc.2023.117518
1220 187 None 44 Human Functional pEC50 = 8.2 8.2 -1 9
Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmcl.2019.126667
31 187 None 44 Human Functional pEC50 = 8.2 8.2 -1 9
Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmcl.2019.126667
7 187 None 44 Human Functional pEC50 = 8.2 8.2 -1 9
Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmcl.2019.126667
CHEMBL56 187 None 44 Human Functional pEC50 = 8.2 8.2 -1 9
Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assayAgonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/j.bmcl.2019.126667
127048539 140350 None 0 Human Functional pEC50 = 8.2 8.2 7 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 441 8 1 5 4.4 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
CHEMBL3805649 140350 None 0 Human Functional pEC50 = 8.2 8.2 7 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 441 8 1 5 4.4 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
132247303 180365 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 451 8 2 4 3.2 NC(=O)c1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4750444 180365 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 451 8 2 4 3.2 NC(=O)c1ccccc1OCCNCC1(F)CCN(C(=O)c2ccc(F)c(Cl)c2)CC1 10.1021/acs.jmedchem.0c00814
10405775 104964 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL311275 104964 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL543139 104964 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1 10.1016/s0960-894x(98)00406-5
145989451 167391 None 0 Human Functional pEC50 = 8.2 8.2 -3 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 459 6 0 6 2.7 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3c2OC(F)(F)O3)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4293718 167391 None 0 Human Functional pEC50 = 8.2 8.2 -3 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 459 6 0 6 2.7 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3c2OC(F)(F)O3)CC1 10.1016/j.ejmech.2017.12.099
145978208 163633 None 0 Human Functional pEC50 = 8.2 8.2 10 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 451 9 1 7 3.6 O=C(NC1CC1)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4202871 163633 None 0 Human Functional pEC50 = 8.2 8.2 10 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 451 9 1 7 3.6 O=C(NC1CC1)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
16109486 137444 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 351 7 1 4 4.2 C1=C(c2cccc(CNCCOc3cccc4c3OCCO4)c2)CCC1 10.1021/jm061180b
CHEMBL375297 137444 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 351 7 1 4 4.2 C1=C(c2cccc(CNCCOc3cccc4c3OCCO4)c2)CCC1 10.1021/jm061180b
49780603 17912 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 391 5 2 4 2.9 Cc1ccc(CNCC2(O)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
CHEMBL1259155 17912 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 391 5 2 4 2.9 Cc1ccc(CNCC2(O)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
132256800 182900 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 478 7 1 4 4.8 CC1(C)Cc2cccc(OCCNCC3(F)CCN(C(=O)c4ccc(F)c(Cl)c4)CC3)c2O1 10.1021/acs.jmedchem.0c00814
CHEMBL4790600 182900 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 478 7 1 4 4.8 CC1(C)Cc2cccc(OCCNCC3(F)CCN(C(=O)c4ccc(F)c(Cl)c4)CC3)c2O1 10.1021/acs.jmedchem.0c00814
1 1650 None 7 Human Functional pEC50 = 8.2 8.2 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cellsCompound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells
ChEMBL 415 6 2 6 1.5 OC[C@H]1COc2c(O1)cccc2N1CCN(CC1)CCNC(=O)c1ccc(cc1)F 10.1016/s0960-894x(98)00406-5
57347 1650 None 7 Human Functional pEC50 = 8.2 8.2 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cellsCompound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells
ChEMBL 415 6 2 6 1.5 OC[C@H]1COc2c(O1)cccc2N1CCN(CC1)CCNC(=O)c1ccc(cc1)F 10.1016/s0960-894x(98)00406-5
CHEMBL1742477 1650 None 7 Human Functional pEC50 = 8.2 8.2 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cellsCompound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells
ChEMBL 415 6 2 6 1.5 OC[C@H]1COc2c(O1)cccc2N1CCN(CC1)CCNC(=O)c1ccc(cc1)F 10.1016/s0960-894x(98)00406-5
10670050 169361 None 0 Human Functional pEC50 = 8.2 8.2 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 424 6 2 4 4.2 CNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
CHEMBL44118 169361 None 0 Human Functional pEC50 = 8.2 8.2 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 424 6 2 4 4.2 CNc1cccc(CNCC2(F)CCN(C(=O)c3ccc(Cl)c(Cl)c3)CC2)n1 10.1021/jm9806906
10405775 104964 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL311275 104964 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL543139 104964 None 0 Human Functional pEC50 = 8.2 8.2 - 1
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
ChEMBL 352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1 10.1016/s0960-894x(98)00406-5
145990794 166896 None 0 Human Functional pEC50 = 8.2 8.2 -1 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4284346 166896 None 0 Human Functional pEC50 = 8.2 8.2 -1 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
10047196 140055 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 410 10 2 5 2.1 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)CC(C)C)CC2)c1 10.1021/jm0508641
CHEMBL379984 140055 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 410 10 2 5 2.1 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)CC(C)C)CC2)c1 10.1021/jm0508641
11741361 2830 None 36 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.0c00814
3924 2830 None 36 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.0c00814
CHEMBL230963 2830 None 36 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.0c00814
11741361 2830 None 36 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.9b00062
3924 2830 None 36 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.9b00062
CHEMBL230963 2830 None 36 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 394 5 1 4 3.3 Cc1cnc(nc1)CNCC1(F)CCN(CC1)C(=O)c1ccc(c(c1)Cl)F 10.1021/acs.jmedchem.9b00062
9862968 18003 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 344 8 2 2 4.9 c1ccc2c(OCCNCCCc3c[nH]c4ccccc34)cccc2c1 10.1021/jm0304010
CHEMBL126253 18003 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 344 8 2 2 4.9 c1ccc2c(OCCNCCCc3c[nH]c4ccccc34)cccc2c1 10.1021/jm0304010
53248210 62051 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 455 9 1 6 3.7 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm200288r
CHEMBL1774532 62051 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 455 9 1 6 3.7 COc1ccc2oc(C(=O)NCCC(F)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm200288r
172452097 195742 None 0 Rat Functional pEC50 = 6.2 6.2 40 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 607 8 0 5 6.1 CC12C(=O)C(C)(C(c3ccccc3)=C1c1ccccc1)C1C(=O)N(CCCCN3CCN(c4cccc(Cl)c4)CC3)C(=O)C12 10.1016/j.bmc.2023.117518
CHEMBL5409943 195742 None 0 Rat Functional pEC50 = 6.2 6.2 40 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 607 8 0 5 6.1 CC12C(=O)C(C)(C(c3ccccc3)=C1c1ccccc1)C1C(=O)N(CCCCN3CCN(c4cccc(Cl)c4)CC3)C(=O)C12 10.1016/j.bmc.2023.117518
52947712 17852 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 415 5 2 4 3.1 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(O)(C5)C3)C4)CC2)nc1 10.1021/jm100835q
CHEMBL1258996 17852 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 415 5 2 4 3.1 Cc1ccc(CNCC2(F)CCN(C(=O)C34CC5CC(CC(O)(C5)C3)C4)CC2)nc1 10.1021/jm100835q
137651544 157566 None 0 Human Functional pEC50 = 6.2 6.2 -17 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 409 4 0 7 2.9 Cc1nc2n(c(=O)c1CCN1CCN(c3nccc4sccc34)CC1)CCCC2 10.1016/j.bmc.2017.07.040
CHEMBL4079365 157566 None 0 Human Functional pEC50 = 6.2 6.2 -17 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 409 4 0 7 2.9 Cc1nc2n(c(=O)c1CCN1CCN(c3nccc4sccc34)CC1)CCCC2 10.1016/j.bmc.2017.07.040
132256806 180111 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 438 8 1 4 4.1 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)cc1 10.1021/acs.jmedchem.0c00814
CHEMBL4747083 180111 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 438 8 1 4 4.1 COc1ccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)cc1 10.1021/acs.jmedchem.0c00814
CHEMBL5071820 216757 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccccc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
16092107 202389 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 379 5 3 3 3.1 O=C1NCc2ccc3c(c21)CC(NCCCc1c[nH]c2ccc(F)cc12)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL594829 202389 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 379 5 3 3 3.1 O=C1NCc2ccc3c(c21)CC(NCCCc1c[nH]c2ccc(F)cc12)CO3 10.1016/j.bmcl.2009.10.134
42606336 17149 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 455 6 1 5 4.0 COc1c(C(=O)N2CCC(F)(CNCc3ccc(C)cn3)CC2)csc1Br 10.1021/jm100835q
CHEMBL1255610 17149 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 455 6 1 5 4.0 COc1c(C(=O)N2CCC(F)(CNCc3ccc(C)cn3)CC2)csc1Br 10.1021/jm100835q
145960493 161654 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
CHEMBL4128838 161654 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 492 6 2 6 4.8 N#Cc1ccc2[nH]cc(C(=O)CCCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1 10.1016/j.bmc.2018.04.037
11339067 87617 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 417 7 1 3 5.5 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3ncccc3c2C1 10.1016/j.bmcl.2007.03.049
CHEMBL233591 87617 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor expressed in CHO membrane assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 417 7 1 3 5.5 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3ncccc3c2C1 10.1016/j.bmcl.2007.03.049
42606458 17889 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 483 5 1 6 3.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3sc(Br)c4c3OCCO4)CC2)nc1 10.1021/jm100835q
CHEMBL1259090 17889 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 483 5 1 6 3.7 Cc1ccc(CNCC2(F)CCN(C(=O)c3sc(Br)c4c3OCCO4)CC2)nc1 10.1021/jm100835q
132256734 179673 None 1 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 408 7 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4741857 179673 None 1 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 408 7 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2)CC1 10.1021/acs.jmedchem.0c00814
5022 1651 None 58 Human Functional pEC50 = 6.2 6.2 6 9
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1021/jm070714l
6918248 1651 None 58 Human Functional pEC50 = 6.2 6.2 6 9
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1021/jm070714l
6918248.0 1651 None 58 Human Functional pEC50 = 6.2 6.2 6 9
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1021/jm070714l
8182 1651 None 58 Human Functional pEC50 = 6.2 6.2 6 9
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1021/jm070714l
CHEMBL231068 1651 None 58 Human Functional pEC50 = 6.2 6.2 6 9
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1021/jm070714l
DB04908 1651 None 58 Human Functional pEC50 = 6.2 6.2 6 9
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1021/jm070714l
145973003 164629 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Antagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAntagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 450 8 0 7 3.9 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2C(C)=O)CC1 10.1016/j.bmc.2017.12.016
CHEMBL4215022 164629 None 0 Rat Functional pEC50 = 6.2 6.2 - 1
Antagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assayAntagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
ChEMBL 450 8 0 7 3.9 COc1ccccc1N1CCN(CCCOc2ccc3c(C)cc(=O)oc3c2C(C)=O)CC1 10.1016/j.bmc.2017.12.016
44461160 105484 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 429 4 0 7 1.4 O=C1c2ccccc2S(=O)(=O)N1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
CHEMBL311976 105484 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 429 4 0 7 1.4 O=C1c2ccccc2S(=O)(=O)N1CCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
132247302 180567 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4752833 180567 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 442 7 1 3 4.7 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1 10.1021/acs.jmedchem.0c00814
44591318 179584 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 393 9 2 5 3.8 COCCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1 10.1016/j.bmcl.2008.12.087
CHEMBL474090 179584 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 393 9 2 5 3.8 COCCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1 10.1016/j.bmcl.2008.12.087
CHEMBL5072039 216762 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(CC6CCCCC6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
CHEMBL5082836 217315 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccccc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
CHEMBL5091978 217827 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)C/C(=C\C4CCN(Cc6ccccc6)CC4)C5=O)CC3)c2c1 10.1016/j.ejmech.2021.114045
132257069 181162 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 425 7 1 4 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCSc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4759629 181162 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 425 7 1 4 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCSc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL5088143 217631 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccsc6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
16109482 142006 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 367 9 1 4 5.4 CC(C)Oc1ccccc1OCCNCc1cccc(-c2ccsc2)c1 10.1021/jm061180b
CHEMBL386988 142006 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 367 9 1 4 5.4 CC(C)Oc1ccccc1OCCNCc1cccc(-c2ccsc2)c1 10.1021/jm061180b
42 2063 None 41 Human Functional pEC50 = 7.2 7.2 -4 10
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cellsCompound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/s0960-894x(98)00406-5
56971 2063 None 41 Human Functional pEC50 = 7.2 7.2 -4 10
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cellsCompound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/s0960-894x(98)00406-5
CHEMBL8412 2063 None 41 Human Functional pEC50 = 7.2 7.2 -4 10
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cellsCompound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1016/s0960-894x(98)00406-5
137640522 157180 None 0 Human Functional pEC50 = 6.2 6.2 -87 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 427 4 0 7 3.3 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2F 10.1016/j.bmc.2017.07.040
CHEMBL4074373 157180 None 0 Human Functional pEC50 = 6.2 6.2 -87 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 427 4 0 7 3.3 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2F 10.1016/j.bmc.2017.07.040
6090 34576 None 10 Human Functional pEC50 = 6.2 6.2 - 1
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 216 5 1 1 3.1 CCN(CC)CCc1c[nH]c2ccccc12 10.1021/jm000339w
CHEMBL142936 34576 None 10 Human Functional pEC50 = 6.2 6.2 - 1
EC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorEC50 for inhibition of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 216 5 1 1 3.1 CCN(CC)CCc1c[nH]c2ccccc12 10.1021/jm000339w
5 139 None 45 Human Functional pEC50 = 7.2 7.2 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2017.05.047
5202 139 None 45 Human Functional pEC50 = 7.2 7.2 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2017.05.047
CHEMBL39 139 None 45 Human Functional pEC50 = 7.2 7.2 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2017.05.047
DB08839 139 None 45 Human Functional pEC50 = 7.2 7.2 -33 26
Agonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assayAgonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as increase in calcium mobilization measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2017.05.047
10024776 166175 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 413 5 1 3 4.3 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(Cl)cn2)CC1 10.1021/jm070714l
CHEMBL425833 166175 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 413 5 1 3 4.3 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCc2ccc(Cl)cn2)CC1 10.1021/jm070714l
16109496 84174 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 351 9 1 3 5.2 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCC2)c1 10.1021/jm061180b
CHEMBL220809 84174 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 351 9 1 3 5.2 CC(C)Oc1ccccc1OCCNCc1cccc(C2=CCCC2)c1 10.1021/jm061180b
138692460 179501 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4739908 179501 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 426 7 1 3 4.2 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(F)c2)CC1 10.1021/acs.jmedchem.0c00814
137656381 159853 None 0 Human Functional pEC50 = 7.2 7.2 33 2
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4scnc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4105102 159853 None 0 Human Functional pEC50 = 7.2 7.2 33 2
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4scnc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
156015516 177668 None 0 Human Functional pEC50 = 8.2 8.2 14 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 485 6 0 7 4.1 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Br)cccn12 10.1016/j.bmcl.2020.127027
CHEMBL4640409 177668 None 0 Human Functional pEC50 = 8.2 8.2 14 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 485 6 0 7 4.1 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2c(Br)cccn12 10.1016/j.bmcl.2020.127027
2810280 182882 None 2 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 476 8 1 3 5.2 O=C(CN1CCN(CCCc2c[nH]c3ccc(F)cc23)CC1)N(c1ccccc1)C1CCCCC1 10.1016/j.ejmech.2020.112214
CHEMBL4790303 182882 None 2 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5H1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL 476 8 1 3 5.2 O=C(CN1CCN(CCCc2c[nH]c3ccc(F)cc23)CC1)N(c1ccccc1)C1CCCCC1 10.1016/j.ejmech.2020.112214
2810280 182882 None 2 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at recombinant 5HT1A receptor (unknown origin) expressed in CHO cell membrane assessed as [35S]GTPgammaS binding by liquid scintillation counting methodAgonist activity at recombinant 5HT1A receptor (unknown origin) expressed in CHO cell membrane assessed as [35S]GTPgammaS binding by liquid scintillation counting method
ChEMBL 476 8 1 3 5.2 O=C(CN1CCN(CCCc2c[nH]c3ccc(F)cc23)CC1)N(c1ccccc1)C1CCCCC1 10.1016/j.ejmech.2020.112214
CHEMBL4790303 182882 None 2 Human Functional pEC50 = 8.2 8.2 - 1
Agonist activity at recombinant 5HT1A receptor (unknown origin) expressed in CHO cell membrane assessed as [35S]GTPgammaS binding by liquid scintillation counting methodAgonist activity at recombinant 5HT1A receptor (unknown origin) expressed in CHO cell membrane assessed as [35S]GTPgammaS binding by liquid scintillation counting method
ChEMBL 476 8 1 3 5.2 O=C(CN1CCN(CCCc2c[nH]c3ccc(F)cc23)CC1)N(c1ccccc1)C1CCCCC1 10.1016/j.ejmech.2020.112214
10025854 101590 None 0 Human Functional pEC50 = 8.2 8.2 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 432 6 1 4 4.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(N3CCC3)n2)CC1 10.1021/jm9806906
CHEMBL298260 101590 None 0 Human Functional pEC50 = 8.2 8.2 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 432 6 1 4 4.2 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(CNCc2cccc(N3CCC3)n2)CC1 10.1021/jm9806906
129186544 161168 None 0 Human Functional pEC50 = 8.2 8.2 -2 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 444 4 0 6 4.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2(F)F 10.1016/j.bmc.2017.07.040
CHEMBL4087132 161168 None 0 Human Functional pEC50 = 8.2 8.2 -2 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 444 4 0 6 4.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2(F)F 10.1016/j.bmc.2017.07.040
CHEMBL4116744 161168 None 0 Human Functional pEC50 = 8.2 8.2 -2 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 444 4 0 6 4.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2(F)F 10.1016/j.bmc.2017.07.040
3251 4072 None 43 Human Functional pEC50 = 8.2 8.2 -3 4
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm0304010
5684 4072 None 43 Human Functional pEC50 = 8.2 8.2 -3 4
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm0304010
80 4072 None 43 Human Functional pEC50 = 8.2 8.2 -3 4
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm0304010
CHEMBL31354 4072 None 43 Human Functional pEC50 = 8.2 8.2 -3 4
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm0304010
129186534 159790 None 0 Human Functional pEC50 = 8.1 8.1 -2 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 426 4 0 6 3.9 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2F 10.1016/j.bmc.2017.07.040
CHEMBL4104261 159790 None 0 Human Functional pEC50 = 8.1 8.1 -2 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 426 4 0 6 3.9 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2F 10.1016/j.bmc.2017.07.040
127049515 140372 None 0 Human Functional pEC50 = 8.1 8.1 5 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 453 8 1 4 4.5 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
CHEMBL3805884 140372 None 0 Human Functional pEC50 = 8.1 8.1 5 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 453 8 1 4 4.5 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
10091417 208014 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 384 6 0 5 3.4 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL543377 208014 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 384 6 0 5 3.4 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL81118 208014 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)Compound was tested for its potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 2)
ChEMBL 384 6 0 5 3.4 O=C(CCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1016/s0960-894x(98)00406-5
145993493 167453 None 0 Human Functional pEC50 = 8.1 8.1 3 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 439 6 0 5 4.5 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4294617 167453 None 0 Human Functional pEC50 = 8.1 8.1 3 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 439 6 0 5 4.5 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
124 2981 None 32 Human Functional pEC50 = 7.2 7.2 -12 24
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2981 None 32 Human Functional pEC50 = 7.2 7.2 -12 24
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2981 None 32 Human Functional pEC50 = 7.2 7.2 -12 24
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636.0 2981 None 32 Human Functional pEC50 = 7.2 7.2 -12 24
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2981 None 32 Human Functional pEC50 = 7.2 7.2 -12 24
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2981 None 32 Human Functional pEC50 = 7.2 7.2 -12 24
PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]PUBCHEM_BIOASSAY: Dose Response assay for agonists of 5-Hydroxytryptamine (Serotonin) Receptor Subtype 1A (5HT1A). (Class of assay: confirmatory) [Related pubchem assays: 567, 574 ]
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
138692457 182539 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 438 8 1 4 4.1 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
CHEMBL4786067 182539 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 438 8 1 4 4.1 COc1cccc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)c1 10.1021/acs.jmedchem.0c00814
172469973 197043 None 0 Rat Functional pEC50 = 6.2 6.2 72 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 574 8 0 6 4.8 CC12C(=O)C(C)(C(c3ccccc3)=C1c1ccccc1)C1C(=O)N(CCCCN3CCN(c4ccccn4)CC3)C(=O)C12 10.1016/j.bmc.2023.117518
CHEMBL5437394 197043 None 0 Rat Functional pEC50 = 6.2 6.2 72 2
Agonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysisAgonist activity at Sprague-Dawley rat hippocampal membrane 5-HT1A receptor assessed as stimulation of [35S]GTPgammaS binding measured after 90 mins by scintillation counter analysis
ChEMBL 574 8 0 6 4.8 CC12C(=O)C(C)(C(c3ccccc3)=C1c1ccccc1)C1C(=O)N(CCCCN3CCN(c4ccccn4)CC3)C(=O)C12 10.1016/j.bmc.2023.117518
53248158 62008 None 0 Human Functional pEC50 = 7.1 7.1 7 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 462 9 1 5 4.0 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm200288r
CHEMBL1774383 62008 None 0 Human Functional pEC50 = 7.1 7.1 7 2
Agonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at 5HT1A receptor assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 462 9 1 5 4.0 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm200288r
2477 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
2477.0 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
36 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
437 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
CHEMBL49 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
DB00490 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.0c00814
2477 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.9b00062
2477.0 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.9b00062
36 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.9b00062
437 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.9b00062
CHEMBL49 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.9b00062
DB00490 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/acs.jmedchem.9b00062
132247309 179546 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 476 7 1 3 5.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(C(F)(F)F)c2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4740430 179546 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
ChEMBL 476 7 1 3 5.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2cccc(C(F)(F)F)c2)CC1 10.1021/acs.jmedchem.0c00814
127051041 140307 None 0 Human Functional pEC50 = 7.1 7.1 -7 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 449 8 1 4 4.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1C 10.1016/j.bmcl.2016.04.087
CHEMBL3805120 140307 None 0 Human Functional pEC50 = 7.1 7.1 -7 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 449 8 1 4 4.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1C 10.1016/j.bmcl.2016.04.087
132256715 179515 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 408 7 2 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4740097 179515 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 408 7 2 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCNc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
71574210 86317 None 0 Human Functional pEC50 = 5.1 5.1 -2 2
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312934 86317 None 0 Human Functional pEC50 = 5.1 5.1 -2 2
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 478 7 1 5 4.0 O=S(=O)(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
46225165 201973 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 393 5 2 3 3.4 CN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NC3 10.1016/j.bmcl.2009.10.134
CHEMBL592028 201973 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 393 5 2 3 3.4 CN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NC3 10.1016/j.bmcl.2009.10.134
24944944 102566 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 331 9 1 4 1.9 O=C1C2CCCN2C(=O)N1CCCCNCCOc1ccccc1 10.1021/jm400766k
CHEMBL2431146 102566 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 331 9 1 4 1.9 O=C1C2CCCN2C(=O)N1CCCCNCCOc1ccccc1 10.1021/jm400766k
CHEMBL3040401 102566 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 331 9 1 4 1.9 O=C1C2CCCN2C(=O)N1CCCCNCCOc1ccccc1 10.1021/jm400766k
129186541 161300 None 0 Human Functional pEC50 = 7.1 7.1 -14 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 407 4 0 5 4.5 Cc1nc2n(c(=O)c1CCN1CCC(c3cccc4sccc34)CC1)CCCC2 10.1016/j.bmc.2017.07.040
CHEMBL4078409 161300 None 0 Human Functional pEC50 = 7.1 7.1 -14 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 407 4 0 5 4.5 Cc1nc2n(c(=O)c1CCN1CCC(c3cccc4sccc34)CC1)CCCC2 10.1016/j.bmc.2017.07.040
CHEMBL4117823 161300 None 0 Human Functional pEC50 = 7.1 7.1 -14 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 407 4 0 5 4.5 Cc1nc2n(c(=O)c1CCN1CCC(c3cccc4sccc34)CC1)CCCC2 10.1016/j.bmc.2017.07.040
130431277 170035 None 0 Human Functional pEC50 = 7.1 7.1 -4 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4441358 170035 None 0 Human Functional pEC50 = 7.1 7.1 -4 2
Agonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5-HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl 10.1021/acs.jmedchem.6b00860
53319432 57157 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
ChEMBL 325 4 1 3 4.2 Fc1cccc(Cl)c1Oc1cccc(F)c1O[C@@H]1CCNC1 10.1016/j.bmcl.2010.11.066
CHEMBL1645617 57157 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5HT1A receptor by GTPgammaS binding assayAgonist activity at 5HT1A receptor by GTPgammaS binding assay
ChEMBL 325 4 1 3 4.2 Fc1cccc(Cl)c1Oc1cccc(F)c1O[C@@H]1CCNC1 10.1016/j.bmcl.2010.11.066
6918388 84173 None 24 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 348 5 1 3 4.4 Fc1ccc(-c2cncc(CNC[C@H]3CCc4ccccc4O3)c2)cc1 10.1021/jm061180b
CHEMBL220808 84173 None 24 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 348 5 1 3 4.4 Fc1ccc(-c2cncc(CNC[C@H]3CCc4ccccc4O3)c2)cc1 10.1021/jm061180b
137646568 158041 None 0 Human Functional pEC50 = 6.1 6.1 -120 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 423 4 0 8 2.5 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2=O 10.1016/j.bmc.2017.07.040
CHEMBL4084663 158041 None 0 Human Functional pEC50 = 6.1 6.1 -120 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 423 4 0 8 2.5 Cc1nc2n(c(=O)c1CCN1CCN(c3nsc4ccccc34)CC1)CCCC2=O 10.1016/j.bmc.2017.07.040
44593729 179486 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 363 7 2 4 4.2 CCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1 10.1016/j.bmcl.2008.12.087
CHEMBL473902 179486 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by FLIPRAgonist activity at human 5HT1A receptor expressed in CHO cells by FLIPR
ChEMBL 363 7 2 4 4.2 CCCNc1nccc(C2CCCN(CCc3c[nH]c4ccccc34)C2)n1 10.1016/j.bmcl.2008.12.087
213 3853 None 34 Human Functional pEC50 = 6.1 6.1 -33 21
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1016/j.bmcl.2020.127027
2717 3853 None 34 Human Functional pEC50 = 6.1 6.1 -33 21
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1016/j.bmcl.2020.127027
5533 3853 None 34 Human Functional pEC50 = 6.1 6.1 -33 21
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1016/j.bmcl.2020.127027
5533.0 3853 None 34 Human Functional pEC50 = 6.1 6.1 -33 21
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1016/j.bmcl.2020.127027
CHEMBL621 3853 None 34 Human Functional pEC50 = 6.1 6.1 -33 21
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1016/j.bmcl.2020.127027
DB00656 3853 None 34 Human Functional pEC50 = 6.1 6.1 -33 21
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1016/j.bmcl.2020.127027
132256764 180698 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 406 7 1 2 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCCc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4754363 180698 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 406 7 1 2 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCCc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
10453264 86125 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 394 5 1 4 3.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nn1 10.1021/jm070714l
CHEMBL230961 86125 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 394 5 1 4 3.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nn1 10.1021/jm070714l
1220 187 None 44 Human Functional pEC50 = 8.1 8.1 -1 9
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm400766k
31 187 None 44 Human Functional pEC50 = 8.1 8.1 -1 9
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm400766k
7 187 None 44 Human Functional pEC50 = 8.1 8.1 -1 9
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm400766k
CHEMBL56 187 None 44 Human Functional pEC50 = 8.1 8.1 -1 9
Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIAAgonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm400766k
132256734 179673 None 1 Human Functional pEC50 = 8.1 8.1 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 408 7 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2)CC1 10.1021/acs.jmedchem.0c00814
CHEMBL4741857 179673 None 1 Human Functional pEC50 = 8.1 8.1 - 1
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 408 7 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2)CC1 10.1021/acs.jmedchem.0c00814
132256734 179673 None 1 Human Functional pEC50 = 8.1 8.1 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 408 7 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4741857 179673 None 1 Human Functional pEC50 = 8.1 8.1 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 408 7 1 3 4.1 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
127048540 140292 None 0 Human Functional pEC50 = 8.1 8.1 3 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 465 8 1 6 3.5 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4c3OC(F)(F)O4)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
CHEMBL3804965 140292 None 0 Human Functional pEC50 = 8.1 8.1 3 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 465 8 1 6 3.5 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4c3OC(F)(F)O4)CC2)ccc1F 10.1016/j.bmcl.2016.04.087
10550911 178992 None 0 Human Functional pEC50 = 8.1 8.1 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 436 7 2 4 4.3 CCNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C 10.1021/jm9806906
CHEMBL46984 178992 None 0 Human Functional pEC50 = 8.1 8.1 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 436 7 2 4 4.3 CCNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ccc1C 10.1021/jm9806906
CHEMBL5087461 217590 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None C=CCN1CCC(CCC(=O)c2ccc(N3CCN(CCCCc4c[nH]c5ccc(C#N)cc45)CC3)cc2)CC1 10.1016/j.ejmech.2021.114045
49780600 17903 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 407 5 0 3 4.3 Cc1ccc(CN(C)CC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
CHEMBL1259124 17903 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 407 5 0 3 4.3 Cc1ccc(CN(C)CC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
5 139 None 45 Human Functional pEC50 = 8.1 8.1 -33 26
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
5202 139 None 45 Human Functional pEC50 = 8.1 8.1 -33 26
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
CHEMBL39 139 None 45 Human Functional pEC50 = 8.1 8.1 -33 26
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
DB08839 139 None 45 Human Functional pEC50 = 8.1 8.1 -33 26
Binding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-SBinding affinity against human 5-hydroxytryptamine 1A receptors HEK 293 cell membranes using [35S]GTP gamma-S
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
145988497 167287 None 0 Human Functional pEC50 = 8.1 8.1 -7 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 411 6 0 5 3.6 O=C1C2CCCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4291387 167287 None 0 Human Functional pEC50 = 8.1 8.1 -7 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 411 6 0 5 3.6 O=C1C2CCCC2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
132256735 180616 None 13 Human Functional pEC50 = 8.1 8.1 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 409 7 1 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4753328 180616 None 13 Human Functional pEC50 = 8.1 8.1 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 409 7 1 4 3.5 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
10695395 171747 None 0 Human Functional pEC50 = 8.1 8.1 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 462 6 1 5 4.8 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cnco3)n2)CC1 10.1021/jm9806906
CHEMBL44659 171747 None 0 Human Functional pEC50 = 8.1 8.1 - 1
In vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptorIn vitro effective concentration required to inhibit forskolin-stimulated cAMP levels in HA7 cells expressing human 5-HT1A receptor
ChEMBL 462 6 1 5 4.8 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCc2cccc(-c3cnco3)n2)CC1 10.1021/jm9806906
2477 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm0508641
2477.0 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm0508641
36 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm0508641
437 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm0508641
CHEMBL49 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm0508641
DB00490 745 None 38 Human Functional pEC50 = 7.1 7.1 -2 20
Activity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assayActivity against 5HT1A receptor by Gi-[35S]GTP-gamma-S binding assay
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm0508641
44373641 120303 None 0 Human Functional pEC50 = 7.1 7.1 -354 2
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 85-370Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 85-370
ChEMBL 408 7 2 5 2.4 COc1cccc(N2CCN(C(=O)COc3ccc4[nH]cc(CCN)c4c3)CC2)c1 10.1016/0960-894X(95)00091-7
CHEMBL352234 120303 None 0 Human Functional pEC50 = 7.1 7.1 -354 2
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 85-370Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 85-370
ChEMBL 408 7 2 5 2.4 COc1cccc(N2CCN(C(=O)COc3ccc4[nH]cc(CCN)c4c3)CC2)c1 10.1016/0960-894X(95)00091-7
23625533 149551 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 423 6 2 5 3.4 CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ncc1C 10.1021/jm070714l
CHEMBL394606 149551 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 423 6 2 5 3.4 CNc1nc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)ncc1C 10.1021/jm070714l
132256764 180698 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 406 7 1 2 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCCc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4754363 180698 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay
ChEMBL 406 7 1 2 4.6 O=C(c1ccc(F)c(Cl)c1)N1CCC(F)(CNCCCc2ccccc2)CC1 10.1021/acs.jmedchem.9b00062
72699817 115252 None 0 Human Functional pEC50 = 6.1 6.1 -1 3
Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay
ChEMBL 343 4 1 4 4.5 CCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344458 115252 None 0 Human Functional pEC50 = 6.1 6.1 -1 3
Agonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) after 20 mins by [35S]GTP-gammaS binding assay
ChEMBL 343 4 1 4 4.5 CCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
44433303 145261 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Antagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as 5-HT-stimulated [35S]GTPgammaS bindingAntagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 354 7 3 3 3.9 OC(CCNC12CC3CC(CC(C3)C1)C2)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2007.07.086
CHEMBL391230 145261 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Antagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as 5-HT-stimulated [35S]GTPgammaS bindingAntagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 354 7 3 3 3.9 OC(CCNC12CC3CC(CC(C3)C1)C2)COc1cccc2[nH]ccc12 10.1016/j.bmcl.2007.07.086
46180398 202714 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 291 0 0 2 3.8 C[C@@H]1Cc2ccc3c(c2O1)-c1cccc2c1[C@@H](C3)N(C)CC2 10.1021/jm9015763
CHEMBL597094 202714 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 291 0 0 2 3.8 C[C@@H]1Cc2ccc3c(c2O1)-c1cccc2c1[C@@H](C3)N(C)CC2 10.1021/jm9015763
42606457 17888 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 401 5 1 4 4.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3scc4c3CCCC4)CC2)nc1 10.1021/jm100835q
CHEMBL1259089 17888 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 401 5 1 4 4.1 Cc1ccc(CNCC2(F)CCN(C(=O)c3scc4c3CCCC4)CC2)nc1 10.1021/jm100835q
172463952 196538 None 0 Human Functional pEC50 = 7.1 7.1 -4 4
Partial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 196538 None 0 Human Functional pEC50 = 7.1 7.1 -4 4
Partial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
71574302 86298 None 0 Human Functional pEC50 = 6.1 6.1 4 2
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
CHEMBL2312637 86298 None 0 Human Functional pEC50 = 6.1 6.1 4 2
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 492 8 1 5 4.4 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2cccnc2c1 10.1016/j.ejmech.2012.11.042
172463952 196538 None 0 Human Functional pEC50 = 7.1 7.1 -4 4
Partial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5426242 196538 None 0 Human Functional pEC50 = 7.1 7.1 -4 4
Partial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 418 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2ccc(=O)[nH]c2c1)CC3 10.1021/acs.jmedchem.3c00098
172450959 195711 None 0 Human Functional pEC50 = 7.1 7.1 -22 4
Partial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 195711 None 0 Human Functional pEC50 = 7.1 7.1 -22 4
Partial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
45483459 201301 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
ChEMBL 271 3 1 2 4.1 Fc1cccc(C2CCNCC2)c1Oc1ccccc1 10.1016/j.bmcl.2009.10.014
CHEMBL583751 201301 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Partial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assayPartial agonist activity at human 5HT1A expressed in HEK293 cells by FLIPR assay
ChEMBL 271 3 1 2 4.1 Fc1cccc(C2CCNCC2)c1Oc1ccccc1 10.1016/j.bmcl.2009.10.014
5492087 208468 None 3 Rat Functional pEC50 = 6.1 6.1 -95 2
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 337 4 2 5 3.6 CN1CCC(c2c[nH]c3ccc(Nc4ncccc4[N+](=O)[O-])cc23)C1 10.1021/jm00042a003
CHEMBL84942 208468 None 3 Rat Functional pEC50 = 6.1 6.1 -95 2
Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptorInhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
ChEMBL 337 4 2 5 3.6 CN1CCC(c2c[nH]c3ccc(Nc4ncccc4[N+](=O)[O-])cc23)C1 10.1021/jm00042a003
44134038 202722 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5HT1A receptor by GTPgammaS assayAgonist activity at 5HT1A receptor by GTPgammaS assay
ChEMBL 306 3 1 3 4.1 Fc1cccc(Cl)c1Oc1ncccc1C1CCNCC1 10.1016/j.bmcl.2009.12.023
CHEMBL597134 202722 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5HT1A receptor by GTPgammaS assayAgonist activity at 5HT1A receptor by GTPgammaS assay
ChEMBL 306 3 1 3 4.1 Fc1cccc(Cl)c1Oc1ncccc1C1CCNCC1 10.1016/j.bmcl.2009.12.023
23625705 149789 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 423 6 1 5 3.1 CN(C)c1ccnc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm070714l
CHEMBL394778 149789 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 423 6 1 5 3.1 CN(C)c1ccnc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)n1 10.1021/jm070714l
172450959 195711 None 0 Human Functional pEC50 = 7.1 7.1 -22 4
Partial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
CHEMBL5409419 195711 None 0 Human Functional pEC50 = 7.1 7.1 -22 4
Partial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assayPartial agonist activity at 5-HT1A receptor (unknown origin) expressed in HEK293T co-expressing G-alphai assessed as increase in cAMP accumulation incubated for 5 mins by BRET assay
ChEMBL 420 7 1 5 4.5 COc1cccc2c3c(oc12)CN(CCCCOc1ccc2c(c1)NC(=O)CC2)CC3 10.1021/acs.jmedchem.3c00098
129186558 158638 None 0 Human Functional pEC50 = 6.1 6.1 -13 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3cncc4sccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4091554 158638 None 0 Human Functional pEC50 = 6.1 6.1 -13 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 425 4 1 8 2.4 Cc1nc2n(c(=O)c1CCN1CCN(c3cncc4sccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
86280005 122298 None 0 Human Functional pEC50 = 8.1 8.1 1 3
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 438 7 1 4 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1 10.1021/acs.jmedchem.5b00776
CHEMBL3597635 122298 None 0 Human Functional pEC50 = 8.1 8.1 1 3
Agonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assayAgonist activity at 5HT1A receptor (unknown origin) by [35S]GTPgammaS binding assay
ChEMBL 438 7 1 4 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1 10.1021/acs.jmedchem.5b00776
CHEMBL5079986 217146 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None CCN1CCC(CCC(=O)c2ccc(N3CCN(CCCCc4c[nH]c5ccc(C#N)cc45)CC3)cc2)CC1 10.1016/j.ejmech.2021.114045
46227770 202384 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 421 6 2 3 3.9 CCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
CHEMBL594788 202384 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 421 6 2 3 3.9 CCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2ccc3c(c2C1)C(=O)NCC3 10.1016/j.bmcl.2009.10.134
145964299 164227 None 0 Human Functional pEC50 = 8.1 8.1 1 6
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 426 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4210030 164227 None 0 Human Functional pEC50 = 8.1 8.1 1 6
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 426 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL5089691 217712 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(CC6CC6)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
132257275 180739 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 425 7 1 4 4.0 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
CHEMBL4754941 180739 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 425 7 1 4 4.0 O=C(c1ccc(Cl)c(Cl)c1)N1CCC(F)(CNCCOc2ccccn2)CC1 10.1021/acs.jmedchem.9b00062
156010883 177249 None 0 Human Functional pEC50 = 8.0 8.0 14 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 441 6 0 7 4.0 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccc(Cl)cn12 10.1016/j.bmcl.2020.127027
CHEMBL4633978 177249 None 0 Human Functional pEC50 = 8.0 8.0 14 3
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 441 6 0 7 4.0 O=c1n(CCCCN2CCN(c3cccc4sccc34)CC2)nc2ccc(Cl)cn12 10.1016/j.bmcl.2020.127027
156018685 177972 None 0 Human Functional pEC50 = 8.0 8.0 -1 6
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 432 6 0 8 3.2 N#Cc1ccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n2c1 10.1016/j.bmcl.2020.127027
CHEMBL4644391 177972 None 0 Human Functional pEC50 = 8.0 8.0 -1 6
Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assayAgonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay
ChEMBL 432 6 0 8 3.2 N#Cc1ccc2nn(CCCCN3CCN(c4cccc5sccc45)CC3)c(=O)n2c1 10.1016/j.bmcl.2020.127027
91884611 159660 None 0 Human Functional pEC50 = 8.0 8.0 -3 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 424 4 1 7 3.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
CHEMBL4102670 159660 None 0 Human Functional pEC50 = 8.0 8.0 -3 6
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 424 4 1 7 3.0 Cc1nc2n(c(=O)c1CCN1CCN(c3cccc4sccc34)CC1)CCCC2O 10.1016/j.bmc.2017.07.040
44408942 76762 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 353 6 2 3 3.7 CCN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
CHEMBL206644 76762 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 353 6 2 3 3.7 CCN1CC(CNCCc2c[nH]c3ccc(F)cc23)Oc2ccccc21 10.1016/j.bmcl.2005.11.054
145989181 167324 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2ccc3ccsc3c2)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4292250 167324 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
Agonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assayAgonist activity at 5-HT1A receptor (unknown origin) after 60 mins by Ultra lance cAMP assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2ccc3ccsc3c2)CC1 10.1016/j.ejmech.2017.12.099
42606577 17869 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 5 2.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccn4n3)CC2)nc1 10.1021/jm100835q
CHEMBL1259035 17869 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 381 5 1 5 2.8 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc4ccccn4n3)CC2)nc1 10.1021/jm100835q
11430856 78050 None 28 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 450 10 2 5 3.0 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)CC3CCCCC3)CC2)c1 10.1021/jm070714l
CHEMBL209821 78050 None 28 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 450 10 2 5 3.0 CC(=O)Nc1cccc(N2CCN(CCCCNS(=O)(=O)CC3CCCCC3)CC2)c1 10.1021/jm070714l
145960544 161736 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 520 7 2 5 5.6 CC(=O)Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(C#N)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
CHEMBL4130176 161736 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay
ChEMBL 520 7 2 5 5.6 CC(=O)Nc1c2c(nc3cccc(N4CCN(CCCCc5c[nH]c6ccc(C#N)cc56)CC4)c13)CCCC2 10.1016/j.bmc.2018.04.037
44408890 140253 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 307 5 3 3 3.2 c1ccc2c(c1)NCC(CNCCc1c[nH]c3ccccc13)O2 10.1016/j.bmcl.2005.11.054
CHEMBL380342 140253 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Intrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptorIntrinsic activity assessed by stimulation of [35S]GTP-gamma-S binding in CHO cells expressing 5HT1A receptor
ChEMBL 307 5 3 3 3.2 c1ccc2c(c1)NCC(CNCCc1c[nH]c3ccccc13)O2 10.1016/j.bmcl.2005.11.054
132256728 180072 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 424 7 1 5 3.2 Cc1cnc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/acs.jmedchem.9b00062
CHEMBL4746734 180072 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assayBiased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay
ChEMBL 424 7 1 5 3.2 Cc1cnc(OCCNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/acs.jmedchem.9b00062
10048222 54013 None 0 Human Functional pEC50 = 7.0 7.0 -33 2
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1A receptor in HeLa cells; value ranges from 95-320Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1A receptor in HeLa cells; value ranges from 95-320
ChEMBL 428 6 2 4 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(c4cccc5ccccc45)CC3)cc12 10.1016/0960-894X(95)00091-7
CHEMBL160581 54013 None 0 Human Functional pEC50 = 7.0 7.0 -33 2
Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1A receptor in HeLa cells; value ranges from 95-320Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1A receptor in HeLa cells; value ranges from 95-320
ChEMBL 428 6 2 4 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(c4cccc5ccccc45)CC3)cc12 10.1016/0960-894X(95)00091-7
164623991 185643 None 0 Human Functional pEC50 = 7.0 7.0 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 185643 None 0 Human Functional pEC50 = 7.0 7.0 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164623991 185643 None 0 Human Functional pEC50 = 7.0 7.0 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 185643 None 0 Human Functional pEC50 = 7.0 7.0 -15 3
Partial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at 5HT1A receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
127049848 140384 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 449 8 1 4 4.6 CNC(=O)c1cc(C)cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
CHEMBL3806047 140384 None 0 Human Functional pEC50 = 7.0 7.0 -1 3
Agonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assayAgonistic activity at human 5-HT1A receptor measured after 60 mins by Ultra Lance cAMP assay
ChEMBL 449 8 1 4 4.6 CNC(=O)c1cc(C)cc(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmcl.2016.04.087
54296648 78799 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 312 8 2 2 3.9 Fc1ccc2[nH]cc(CCCNCCOc3ccccc3)c2c1 10.1021/jm0304010
CHEMBL2112644 78799 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
ChEMBL 312 8 2 2 3.9 Fc1ccc2[nH]cc(CCCNCCOc3ccccc3)c2c1 10.1021/jm0304010
5 139 None 45 Human Functional pEC50 = 7.0 7.0 -33 26
Agonist activity at human 5-HT1A 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-HT1A 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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2018.04.059
5202 139 None 45 Human Functional pEC50 = 7.0 7.0 -33 26
Agonist activity at human 5-HT1A 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-HT1A 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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2018.04.059
CHEMBL39 139 None 45 Human Functional pEC50 = 7.0 7.0 -33 26
Agonist activity at human 5-HT1A 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-HT1A 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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2018.04.059
DB08839 139 None 45 Human Functional pEC50 = 7.0 7.0 -33 26
Agonist activity at human 5-HT1A 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-HT1A 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 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmcl.2018.04.059
42606334 17915 None 0 Human Functional pEC50 = 7 7.0 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 377 6 1 5 3.2 COc1cscc1C(=O)N1CCC(F)(CNCc2ccc(C)cn2)CC1 10.1021/jm100835q
CHEMBL1259165 17915 None 0 Human Functional pEC50 = 7 7.0 - 1
Intrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS bindingIntrinsic activity at human 5-HT1A receptor expressed in CHO cells assessed as increase of serotonin-induced [35S]GTPgammaS binding
ChEMBL 377 6 1 5 3.2 COc1cscc1C(=O)N1CCC(F)(CNCc2ccc(C)cn2)CC1 10.1021/jm100835q
CHEMBL5093872 217941 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assayAgonist activity at human 5-HT1A receptor expressed in HEK293 cells incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay
ChEMBL None None None N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc(C(=O)CCC5CCN(Cc6ccccc6F)CC5)cc4)CC3)c2c1 10.1016/j.ejmech.2021.114045
11774457 66809 None 0 Rat Functional pED50 = 8.3 8.3 - 1
Effective dose against 5-HT1a receptorEffective dose against 5-HT1a receptor
ChEMBL 419 8 3 4 2.5 NC(=O)c1ccc(N2CCN(CCCCc3c[nH]c4ccc(C(N)=O)cc34)CC2)cc1 10.1021/jm040792y
CHEMBL185938 66809 None 0 Rat Functional pED50 = 8.3 8.3 - 1
Effective dose against 5-HT1a receptorEffective dose against 5-HT1a receptor
ChEMBL 419 8 3 4 2.5 NC(=O)c1ccc(N2CCN(CCCCc3c[nH]c4ccc(C(N)=O)cc34)CC2)cc1 10.1021/jm040792y
4223 3992 None 57 Human Functional pIC50 = 9.7 9.7 7 17
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/acs.jmedchem.7b01788
6918314 3992 None 57 Human Functional pIC50 = 9.7 9.7 7 17
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/acs.jmedchem.7b01788
6918314.0 3992 None 57 Human Functional pIC50 = 9.7 9.7 7 17
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/acs.jmedchem.7b01788
7427 3992 None 57 Human Functional pIC50 = 9.7 9.7 7 17
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/acs.jmedchem.7b01788
CHEMBL439849 3992 None 57 Human Functional pIC50 = 9.7 9.7 7 17
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/acs.jmedchem.7b01788
DB06684 3992 None 57 Human Functional pIC50 = 9.7 9.7 7 17
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/acs.jmedchem.7b01788
11249411 67416 None 0 Human Functional pIC50 = 9.2 9.2 1 3
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 402 6 1 5 3.9 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)OCO5)CC3)c2c1 10.1021/acs.jmedchem.7b01788
CHEMBL188799 67416 None 0 Human Functional pIC50 = 9.2 9.2 1 3
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 402 6 1 5 3.9 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)OCO5)CC3)c2c1 10.1021/acs.jmedchem.7b01788
11362047 67564 None 0 Human Functional pIC50 = 9 9.0 1 3
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 416 6 1 5 4.0 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)OCCO5)CC3)c2c1 10.1021/acs.jmedchem.7b01788
CHEMBL189709 67564 None 0 Human Functional pIC50 = 9 9.0 1 3
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 416 6 1 5 4.0 N#Cc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)OCCO5)CC3)c2c1 10.1021/acs.jmedchem.7b01788
12004200 8572 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 467 4 0 6 4.9 COc1cc(N2CCN(C3CCN(c4cccc5c(C)ccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1094558 8572 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 467 4 0 6 4.9 COc1cc(N2CCN(C3CCN(c4cccc5c(C)ccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
12004226 8786 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 531 4 0 6 5.3 COc1cc(N2CCN(C3CCN(c4cc(Br)cc5cccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1096529 8786 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 531 4 0 6 5.3 COc1cc(N2CCN(C3CCN(c4cc(Br)cc5cccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
44593712 184949 None 0 Human Functional pIC50 = 6 6.0 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 446 7 2 4 4.1 N#Cc1ccc2[nH]cc(CCCN(C3CCC3)C3COc4c(F)ccc(C(N)=O)c4C3)c2c1 10.1021/jm8007097
CHEMBL485228 184949 None 0 Human Functional pIC50 = 6 6.0 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 446 7 2 4 4.1 N#Cc1ccc2[nH]cc(CCCN(C3CCC3)C3COc4c(F)ccc(C(N)=O)c4C3)c2c1 10.1021/jm8007097
44192200 197845 None 1 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 451 3 0 7 3.9 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C#N)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL551964 197845 None 1 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 451 3 0 7 3.9 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C#N)ccc4n2)CC1)O3 10.1021/jm900374r
10111229 5070 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 394 5 1 4 4.2 Fc1ccc2[nH]cc(C3=CCN(CCOc4cccc5c4OCCO5)CC3)c2c1 10.1016/s0960-894x(01)00746-6
CHEMBL105390 5070 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 394 5 1 4 4.2 Fc1ccc2[nH]cc(C3=CCN(CCOc4cccc5c4OCCO5)CC3)c2c1 10.1016/s0960-894x(01)00746-6
11164569 118246 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 370 8 2 3 4.8 Fc1cc(OCCNCCCc2c[nH]c3ccc(F)cc23)c2occc2c1 10.1021/jm0304010
CHEMBL340895 118246 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 370 8 2 3 4.8 Fc1cc(OCCNCCCc2c[nH]c3ccc(F)cc23)c2occc2c1 10.1021/jm0304010
3251 4072 None 43 Human Functional pIC50 = 8.0 8.0 -3 4
Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.8b01096
5684 4072 None 43 Human Functional pIC50 = 8.0 8.0 -3 4
Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.8b01096
80 4072 None 43 Human Functional pIC50 = 8.0 8.0 -3 4
Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.8b01096
CHEMBL31354 4072 None 43 Human Functional pIC50 = 8.0 8.0 -3 4
Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.8b01096
9975609 164251 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonism at the 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism at the 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 357 5 2 2 4.8 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3[nH]ccc23)C1 10.1016/s0960-894x(01)00746-6
CHEMBL421027 164251 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonism at the 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism at the 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 357 5 2 2 4.8 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3[nH]ccc23)C1 10.1016/s0960-894x(01)00746-6
9929572 4811 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 376 5 1 4 4.1 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3c2OCCO3)C1 10.1016/s0960-894x(01)00746-6
CHEMBL104144 4811 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 376 5 1 4 4.1 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3c2OCCO3)C1 10.1016/s0960-894x(01)00746-6
44220114 197711 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 440 3 0 6 4.4 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4ccccc4n2)C[C@H]1C)O3 10.1021/jm900374r
CHEMBL551107 197711 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 440 3 0 6 4.4 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4ccccc4n2)C[C@H]1C)O3 10.1021/jm900374r
145946265 167612 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
CHEMBL4203310 167612 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
CHEMBL4299892 167612 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 396 10 0 4 3.9 Cc1cc(C)c(OCCOCCN2CCN(CCc3ccccc3)CC2)c(C)c1 10.1016/j.bmcl.2018.04.059
9820163 4841 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 358 5 2 3 4.2 C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3[nH]ccc23)C1 10.1016/s0960-894x(01)00746-6
CHEMBL104229 4841 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 358 5 2 3 4.2 C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3[nH]ccc23)C1 10.1016/s0960-894x(01)00746-6
10362715 16610 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 386 8 2 3 4.4 Fc1cc2c(c(OCCNCCCc3c[nH]c4ccc(F)cc34)c1)OCCC2 10.1021/jm0304010
CHEMBL124069 16610 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 386 8 2 3 4.4 Fc1cc2c(c(OCCNCCCc3c[nH]c4ccc(F)cc34)c1)OCCC2 10.1021/jm0304010
25139055 184488 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 455 7 2 3 4.9 NC(=O)c1ccc(Cl)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL484572 184488 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 455 7 2 3 4.9 NC(=O)c1ccc(Cl)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
11751072 78043 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 441 9 2 3 4.6 CCCN(CCCCc1c[nH]c2ccc(F)cc12)C1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm060218h
CHEMBL209784 78043 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 441 9 2 3 4.6 CCCN(CCCCc1c[nH]c2ccc(F)cc12)C1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm060218h
44365679 41198 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assay
ChEMBL 437 4 1 6 4.6 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1csc4ccccc14)C3)CO2 10.1016/j.bmcl.2003.10.024
CHEMBL148860 41198 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assay
ChEMBL 437 4 1 6 4.6 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1csc4ccccc14)C3)CO2 10.1016/j.bmcl.2003.10.024
11662592 72368 None 0 Human Functional pIC50 = 5.9 5.9 -15 2
Displacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptorDisplacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198463 72368 None 0 Human Functional pIC50 = 5.9 5.9 -15 2
Displacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptorDisplacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
11845645 79554 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 413 7 2 3 3.8 CCN(CCCc1c[nH]c2ccc(F)cc12)[C@H]1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm060218h
CHEMBL211393 79554 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 413 7 2 3 3.8 CCN(CCCc1c[nH]c2ccc(F)cc12)[C@H]1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm060218h
9798864 168654 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 358 7 2 3 3.6 Fc1cc2c(c(OCCNCCc3c[nH]c4ccc(F)cc34)c1)OCC2 10.1021/jm0304010
CHEMBL435612 168654 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 358 7 2 3 3.6 Fc1cc2c(c(OCCNCCc3c[nH]c4ccc(F)cc34)c1)OCC2 10.1021/jm0304010
1220 187 None 44 Rat Functional pIC50 = 7.9 7.9 1 9
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
31 187 None 44 Rat Functional pIC50 = 7.9 7.9 1 9
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
7 187 None 44 Rat Functional pIC50 = 7.9 7.9 1 9
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
CHEMBL56 187 None 44 Rat Functional pIC50 = 7.9 7.9 1 9
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
9998826 120541 None 0 Rat Functional pIC50 = 7.9 7.9 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
CHEMBL354210 120541 None 0 Rat Functional pIC50 = 7.9 7.9 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
10474964 130539 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 130539 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 130539 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
44365728 120955 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assay
ChEMBL 382 4 1 6 2.7 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1ccccn1)C3)CO2 10.1016/j.bmcl.2003.10.024
CHEMBL355953 120955 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assay
ChEMBL 382 4 1 6 2.7 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1ccccn1)C3)CO2 10.1016/j.bmcl.2003.10.024
12004255 8961 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 539 4 0 6 5.7 COc1cc(N2CCN(C3CCN(c4ccc(F)c5cc(C(F)(F)F)cnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1098133 8961 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 539 4 0 6 5.7 COc1cc(N2CCN(C3CCN(c4ccc(F)c5cc(C(F)(F)F)cnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
10474964 130539 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 130539 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 130539 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
10046389 61436 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
CHEMBL177031 61436 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
44219922 197666 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 504 3 0 6 4.8 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(Br)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL550700 197666 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 504 3 0 6 4.8 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(Br)ccc4n2)CC1)O3 10.1021/jm900374r
11303781 117337 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 388 8 2 4 3.8 Fc1cc(OCCNCCCc2c[nH]c3ccc(F)cc23)c2c(c1)OCCO2 10.1021/jm0304010
CHEMBL339490 117337 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 388 8 2 4 3.8 Fc1cc(OCCNCCCc2c[nH]c3ccc(F)cc23)c2c(c1)OCCO2 10.1021/jm0304010
10158434 26138 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 409 5 2 4 4.8 OC(CCN1CCN(c2cccc3[nH]ccc23)CC1)c1csc2ccc(F)cc12 10.1021/jm0111200
CHEMBL135623 26138 None 0 Rat Functional pIC50 = 7.8 7.8 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 409 5 2 4 4.8 OC(CCN1CCN(c2cccc3[nH]ccc23)CC1)c1csc2ccc(F)cc12 10.1021/jm0111200
126 4070 None 6 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 395 6 1 4 3.5 COc1ccccc1N1CCN(CC1)C[C@@H](C(=O)NC(C)(C)C)c1ccccc1 10.1016/j.bmcl.2018.04.059
6604840 4070 None 6 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 395 6 1 4 3.5 COc1ccccc1N1CCN(CC1)C[C@@H](C(=O)NC(C)(C)C)c1ccccc1 10.1016/j.bmcl.2018.04.059
CHEMBL38288 4070 None 6 Human Functional pIC50 = 7.8 7.8 1 2
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 395 6 1 4 3.5 COc1ccccc1N1CCN(CC1)C[C@@H](C(=O)NC(C)(C)C)c1ccccc1 10.1016/j.bmcl.2018.04.059
44219923 198436 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 4 1 7 3.2 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C(N)=O)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL559778 198436 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 4 1 7 3.2 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C(N)=O)ccc4n2)CC1)O3 10.1021/jm900374r
44593715 185078 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 411 4 3 3 3.2 NC(=O)c1ccc(F)c2c1C[C@@H](NCC1CCc3[nH]c4ccc(F)cc4c3C1)CO2 10.1021/jm8007097
CHEMBL485407 185078 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 411 4 3 3 3.2 NC(=O)c1ccc(F)c2c1C[C@@H](NCC1CCc3[nH]c4ccc(F)cc4c3C1)CO2 10.1021/jm8007097
46180399 204655 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma binding
ChEMBL 291 0 0 2 3.8 C[C@H]1Cc2ccc3c(c2O1)-c1cccc2c1[C@@H](C3)N(C)CC2 10.1021/jm9015763
CHEMBL609611 204655 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma binding
ChEMBL 291 0 0 2 3.8 C[C@H]1Cc2ccc3c(c2O1)-c1cccc2c1[C@@H](C3)N(C)CC2 10.1021/jm9015763
9846057 165609 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 403 5 1 5 4.7 OC(CCN1CCN(c2cccc3cccnc23)CC1)c1csc2ccccc12 10.1021/jm0111200
CHEMBL424083 165609 None 0 Rat Functional pIC50 = 7.7 7.7 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 403 5 1 5 4.7 OC(CCN1CCN(c2cccc3cccnc23)CC1)c1csc2ccccc12 10.1021/jm0111200
145961441 161456 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 502 8 0 6 5.6 CC(=O)c1c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.ejmech.2017.05.047
CHEMBL4126092 161456 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 502 8 0 6 5.6 CC(=O)c1c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.ejmech.2017.05.047
44220115 198476 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 465 3 0 7 4.3 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C#N)ccc4n2)C[C@H]1C)O3 10.1021/jm900374r
CHEMBL560170 198476 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 465 3 0 7 4.3 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C#N)ccc4n2)C[C@H]1C)O3 10.1021/jm900374r
44593716 185183 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 6 2 3 4.4 CCCN(CC1CCc2[nH]c3ccc(F)cc3c2C1)[C@H]1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm8007097
CHEMBL485579 185183 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 6 2 3 4.4 CCCN(CC1CCc2[nH]c3ccc(F)cc3c2C1)[C@H]1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm8007097
9842337 169515 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonism at the 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism at the 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 370 5 1 4 4.3 C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3ncccc23)C1 10.1016/s0960-894x(01)00746-6
CHEMBL442391 169515 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonism at the 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism at the 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 370 5 1 4 4.3 C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3ncccc23)C1 10.1016/s0960-894x(01)00746-6
25139058 184497 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 421 7 2 3 4.2 NC(=O)c1cccc2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL484580 184497 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 421 7 2 3 4.2 NC(=O)c1cccc2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL484747 184497 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 421 7 2 3 4.2 NC(=O)c1cccc2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
44220113 199211 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 440 3 0 6 4.4 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4ccccc4n2)C[C@@H]1C)O3 10.1021/jm900374r
CHEMBL565234 199211 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 440 3 0 6 4.4 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4ccccc4n2)C[C@@H]1C)O3 10.1021/jm900374r
145960744 161697 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 438 7 0 6 4.0 CC(=O)c1c(OCCCN2CCN(c3ccccc3F)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.ejmech.2017.05.047
CHEMBL4129562 161697 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 438 7 0 6 4.0 CC(=O)c1c(OCCCN2CCN(c3ccccc3F)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.ejmech.2017.05.047
44593712 184949 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 446 7 2 4 4.1 N#Cc1ccc2[nH]cc(CCCN(C3CCC3)C3COc4c(F)ccc(C(N)=O)c4C3)c2c1 10.1021/jm8007097
CHEMBL485228 184949 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 446 7 2 4 4.1 N#Cc1ccc2[nH]cc(CCCN(C3CCC3)C3COc4c(F)ccc(C(N)=O)c4C3)c2c1 10.1021/jm8007097
127034967 136575 None 0 Human Functional pIC50 = 5.7 5.7 -19 3
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay
ChEMBL 260 5 2 4 1.6 CB1C=Cc2c(cccc2OCC(O)CN(C)C)N1 10.1021/acs.jmedchem.5b01088
CHEMBL3736156 136575 None 0 Human Functional pIC50 = 5.7 5.7 -19 3
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay
ChEMBL 260 5 2 4 1.6 CB1C=Cc2c(cccc2OCC(O)CN(C)C)N1 10.1021/acs.jmedchem.5b01088
12004142 8773 None 1 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 471 4 0 6 4.7 COc1cc(N2CCN(C3CCN(c4ccc(F)c5cccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1096476 8773 None 1 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 471 4 0 6 4.7 COc1cc(N2CCN(C3CCN(c4ccc(F)c5cccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
12004223 8863 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 499 4 0 6 5.3 COc1cc(N2CCN(C3CCN(c4ccc(F)c5c(C)cc(C)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1097181 8863 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 499 4 0 6 5.3 COc1cc(N2CCN(C3CCN(c4ccc(F)c5c(C)cc(C)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
3251 4072 None 43 Human Functional pIC50 = 8.6 8.6 -3 4
Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2020.112709
5684 4072 None 43 Human Functional pIC50 = 8.6 8.6 -3 4
Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2020.112709
80 4072 None 43 Human Functional pIC50 = 8.6 8.6 -3 4
Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2020.112709
CHEMBL31354 4072 None 43 Human Functional pIC50 = 8.6 8.6 -3 4
Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2020.112709
12004280 8962 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 489 4 0 6 4.9 COc1cc(N2CCN(C3CCN(c4ccc(F)c5cc(F)cnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1098134 8962 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 489 4 0 6 4.9 COc1cc(N2CCN(C3CCN(c4ccc(F)c5cc(F)cnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
11293572 140206 None 3 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL380095 140206 None 3 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
46225309 202596 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 454 8 2 4 4.3 N#Cc1ccc2[nH]cc(CCCCN(CC3CC3)C3COc4ccc5c(c4C3)C(=O)NC5)c2c1 10.1016/j.bmcl.2009.10.134
CHEMBL596297 202596 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 454 8 2 4 4.3 N#Cc1ccc2[nH]cc(CCCCN(CC3CC3)C3COc4ccc5c(c4C3)C(=O)NC5)c2c1 10.1016/j.bmcl.2009.10.134
25139065 184480 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 9 1 4 4.5 NC(=O)c1ccc(F)c2c1CC(N(CCCCn1ccc3cccc(F)c31)CC1CC1)CO2 10.1021/jm8007097
CHEMBL484537 184480 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 9 1 4 4.5 NC(=O)c1ccc(F)c2c1CC(N(CCCCn1ccc3cccc(F)c31)CC1CC1)CO2 10.1021/jm8007097
44593714 185221 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 457 7 2 3 4.5 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3c(F)cc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL485625 185221 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 457 7 2 3 4.5 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3c(F)cc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
11484260 116985 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 328 8 2 3 3.5 COc1ccc(F)cc1OCCNCCc1c[nH]c2ccccc12 10.1021/jm0304010
CHEMBL338482 116985 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 328 8 2 3 3.5 COc1ccc(F)cc1OCCNCCc1c[nH]c2ccccc12 10.1021/jm0304010
44365671 38930 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assay
ChEMBL 431 4 1 5 4.5 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1ccc4ccccc4c1)C3)CO2 10.1016/j.bmcl.2003.10.024
CHEMBL146751 38930 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assay
ChEMBL 431 4 1 5 4.5 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1ccc4ccccc4c1)C3)CO2 10.1016/j.bmcl.2003.10.024
44365672 43961 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assay
ChEMBL 381 4 1 5 3.4 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1ccccc1)C3)CO2 10.1016/j.bmcl.2003.10.024
CHEMBL151266 43961 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by forskolin stimulated cAMP assay
ChEMBL 381 4 1 5 3.4 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1ccccc1)C3)CO2 10.1016/j.bmcl.2003.10.024
9864676 127875 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 380 6 0 3 4.5 O=C(CCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL366388 127875 None 0 Rat Functional pIC50 = 6.7 6.7 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 380 6 0 3 4.5 O=C(CCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
44219921 197593 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 444 3 0 6 4.2 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(F)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL550169 197593 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 444 3 0 6 4.2 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(F)ccc4n2)CC1)O3 10.1021/jm900374r
9929572 4811 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 376 5 1 4 4.1 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3c2OCCO3)C1 10.1016/s0960-894x(01)00746-6
CHEMBL104144 4811 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 376 5 1 4 4.1 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3c2OCCO3)C1 10.1016/s0960-894x(01)00746-6
46225207 204358 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 433 7 2 3 4.2 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL607419 204358 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 433 7 2 3 4.2 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
11845636 79455 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 408 7 1 3 5.1 COc1cccc2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm060218h
CHEMBL211363 79455 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 408 7 1 3 5.1 COc1cccc2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm060218h
145963270 161673 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 464 9 0 7 4.3 COc1cccc(N2CCN(CCCCOc3ccc4c(C)cc(=O)oc4c3C(C)=O)CC2)c1 10.1016/j.ejmech.2017.05.047
CHEMBL4129173 161673 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 464 9 0 7 4.3 COc1cccc(N2CCN(CCCCOc3ccc4c(C)cc(=O)oc4c3C(C)=O)CC2)c1 10.1016/j.ejmech.2017.05.047
12004224 8790 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 521 4 0 6 5.6 COc1cc(N2CCN(C3CCN(c4cccc5ccc(C(F)(F)F)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1096540 8790 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 521 4 0 6 5.6 COc1cc(N2CCN(C3CCN(c4cccc5ccc(C(F)(F)F)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
11272673 69419 None 0 Human Functional pIC50 = 7.6 7.6 - 1
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 503 7 0 8 3.6 C[C@H](CN(C(=O)c1ccc([N+](=O)[O-])cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
CHEMBL193206 69419 None 0 Human Functional pIC50 = 7.6 7.6 - 1
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 503 7 0 8 3.6 C[C@H](CN(C(=O)c1ccc([N+](=O)[O-])cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
11339973 80241 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 453 8 2 3 4.7 NC(=O)c1ccc(F)c2c1CC(N(CCCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm060218h
CHEMBL213673 80241 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 453 8 2 3 4.7 NC(=O)c1ccc(F)c2c1CC(N(CCCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm060218h
164622805 185969 None 0 Human Functional pIC50 = 6.6 6.6 -21 6
Antagonist activity at 5-HT1A receptor (unknown origin)Antagonist activity at 5-HT1A receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
CHEMBL4867978 185969 None 0 Human Functional pIC50 = 6.6 6.6 -21 6
Antagonist activity at 5-HT1A receptor (unknown origin)Antagonist activity at 5-HT1A receptor (unknown origin)
ChEMBL 467 9 0 6 4.5 Fc1ccc2c(C3CCN(CCCOc4ccc(CCN5CCOCC5)cc4)CC3)noc2c1 10.1016/j.bmcl.2021.127909
44365672 43961 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assay
ChEMBL 381 4 1 5 3.4 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1ccccc1)C3)CO2 10.1016/j.bmcl.2003.10.024
CHEMBL151266 43961 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assay
ChEMBL 381 4 1 5 3.4 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1ccccc1)C3)CO2 10.1016/j.bmcl.2003.10.024
10116877 135279 None 7 Human Functional pIC50 = 7.6 7.6 - 1
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 483 6 0 7 3.6 C[C@H](CN(C(=O)c1ccc(C#N)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
CHEMBL372205 135279 None 7 Human Functional pIC50 = 7.6 7.6 - 1
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 483 6 0 7 3.6 C[C@H](CN(C(=O)c1ccc(C#N)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
25139217 185097 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 7 2 3 4.6 CNC(=O)c1ccc(F)c2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL485434 185097 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 7 2 3 4.6 CNC(=O)c1ccc(F)c2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
11845822 77599 None 5 Human Functional pIC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm060218h
CHEMBL208773 77599 None 5 Human Functional pIC50 = 7.6 7.6 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm060218h
145961730 161561 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 452 8 0 6 4.4 CC(=O)c1c(OCCCCN2CCN(c3ccccc3F)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.ejmech.2017.05.047
CHEMBL4127564 161561 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 452 8 0 6 4.4 CC(=O)c1c(OCCCCN2CCN(c3ccccc3F)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.ejmech.2017.05.047
145947560 167809 None 0 Human Functional pIC50 = 6.5 6.5 2 4
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 344 6 0 3 4.2 Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2018.04.059
CHEMBL4212812 167809 None 0 Human Functional pIC50 = 6.5 6.5 2 4
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 344 6 0 3 4.2 Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2018.04.059
CHEMBL4302457 167809 None 0 Human Functional pIC50 = 6.5 6.5 2 4
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 344 6 0 3 4.2 Cc1cc(OCCCN2CCN(c3ccccc3)CC2)ccc1Cl 10.1016/j.bmcl.2018.04.059
44219920 198116 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 471 4 0 8 4.0 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc([N+](=O)[O-])ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL556474 198116 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 471 4 0 8 4.0 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc([N+](=O)[O-])ccc4n2)CC1)O3 10.1021/jm900374r
11316467 122703 None 0 Human Functional pIC50 = 8.5 8.5 1 2
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 434 7 2 4 4.3 NC(=O)c1cc2cc(N3CCN(CCCCc4c[nH]c5ccc(F)cc45)CC3)ccc2o1 10.1021/acs.jmedchem.7b01788
CHEMBL360390 122703 None 0 Human Functional pIC50 = 8.5 8.5 1 2
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 434 7 2 4 4.3 NC(=O)c1cc2cc(N3CCN(CCCCc4c[nH]c5ccc(F)cc45)CC3)ccc2o1 10.1021/acs.jmedchem.7b01788
71449095 78823 None 0 Rat Functional pIC50 = 8.4 8.4 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 421 5 1 5 4.8 OC(CCN1CCN(c2ccc3ccccc3n2)CC1)c1csc2ccc(F)cc12 10.1021/jm0111200
CHEMBL2112696 78823 None 0 Rat Functional pIC50 = 8.4 8.4 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 421 5 1 5 4.8 OC(CCN1CCN(c2ccc3ccccc3n2)CC1)c1csc2ccc(F)cc12 10.1021/jm0111200
16091081 8606 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 453 4 0 6 4.6 COc1cc(N2CCN(C3CCN(c4cccc5cccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1094872 8606 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 453 4 0 6 4.6 COc1cc(N2CCN(C3CCN(c4cccc5cccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
12004116 8571 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 521 4 0 6 5.6 COc1cc(N2CCN(C3CCN(c4cccc5cc(C(F)(F)F)cnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1094557 8571 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 521 4 0 6 5.6 COc1cc(N2CCN(C3CCN(c4cccc5cc(C(F)(F)F)cnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
12004253 8744 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 551 5 0 7 5.6 COc1cc(N2CCN(C3CCN(c4cccc5c(OC)cc(C(F)(F)F)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1096156 8744 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 551 5 0 7 5.6 COc1cc(N2CCN(C3CCN(c4cccc5c(OC)cc(C(F)(F)F)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
10180988 116687 None 0 Rat Functional pIC50 = 7.5 7.5 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 428 5 1 6 4.1 OC(CCN1CCN(c2cccc3c2OCCO3)CC1)c1csc2ccc(F)cc12 10.1021/jm0111200
CHEMBL336842 116687 None 0 Rat Functional pIC50 = 7.5 7.5 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 428 5 1 6 4.1 OC(CCN1CCN(c2cccc3c2OCCO3)CC1)c1csc2ccc(F)cc12 10.1021/jm0111200
10159609 23646 None 0 Rat Functional pIC50 = 7.5 7.5 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 391 5 2 4 4.6 OC(CCN1CCN(c2cccc3[nH]ccc23)CC1)c1csc2ccccc12 10.1021/jm0111200
CHEMBL133476 23646 None 0 Rat Functional pIC50 = 7.5 7.5 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 391 5 2 4 4.6 OC(CCN1CCN(c2cccc3[nH]ccc23)CC1)c1csc2ccccc12 10.1021/jm0111200
44354158 21576 None 0 Rat Functional pIC50 = 7.5 7.5 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 405 5 2 5 4.4 OC(CCN1CCN(C2C=Cc3ccccc3N2)CC1)c1csc2ccccc12 10.1021/jm0111200
CHEMBL131691 21576 None 0 Rat Functional pIC50 = 7.5 7.5 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 405 5 2 5 4.4 OC(CCN1CCN(C2C=Cc3ccccc3N2)CC1)c1csc2ccccc12 10.1021/jm0111200
11568826 132866 None 0 Human Functional pIC50 = 6.5 6.5 -9 2
Displacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptorDisplacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL370110 132866 None 0 Human Functional pIC50 = 6.5 6.5 -9 2
Displacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptorDisplacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
11444410 168569 None 0 Human Functional pIC50 = 7.5 7.5 - 1
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 526 6 0 6 4.7 C[C@H](CN(C(=O)c1ccc(C(F)(F)F)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
CHEMBL435111 168569 None 0 Human Functional pIC50 = 7.5 7.5 - 1
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 526 6 0 6 4.7 C[C@H](CN(C(=O)c1ccc(C(F)(F)F)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
46225207 204358 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 433 7 2 3 4.2 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
CHEMBL607419 204358 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 433 7 2 3 4.2 O=C1NCc2ccc3c(c21)CC(N(CCCc1c[nH]c2ccc(F)cc12)CC1CC1)CO3 10.1016/j.bmcl.2009.10.134
46180192 204533 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma binding
ChEMBL 291 3 0 2 4.0 C=CCOc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm9015763
CHEMBL608728 204533 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma binding
ChEMBL 291 3 0 2 4.0 C=CCOc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm9015763
46180194 204620 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma binding
ChEMBL 291 0 0 2 3.8 CC1Cc2ccc3c(c2O1)-c1cccc2c1[C@@H](C3)N(C)CC2 10.1021/jm9015763
CHEMBL609317 204620 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Agonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma bindingAgonist activity at 5HT1A receptor expressed in CHO cells assessed as inhibition of 5-HT-stimulated [35S]GTPgamma binding
ChEMBL 291 0 0 2 3.8 CC1Cc2ccc3c(c2O1)-c1cccc2c1[C@@H](C3)N(C)CC2 10.1021/jm9015763
9975609 164251 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 357 5 2 2 4.8 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3[nH]ccc23)C1 10.1016/s0960-894x(01)00746-6
CHEMBL421027 164251 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 357 5 2 2 4.8 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3[nH]ccc23)C1 10.1016/s0960-894x(01)00746-6
11261072 133642 None 0 Human Functional pIC50 = 7.5 7.5 - 1
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 492 6 0 6 4.4 C[C@H](CN(C(=O)c1ccc(Cl)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
CHEMBL371149 133642 None 0 Human Functional pIC50 = 7.5 7.5 - 1
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 492 6 0 6 4.4 C[C@H](CN(C(=O)c1ccc(Cl)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
12004114 8787 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 471 4 0 6 4.7 COc1cc(N2CCN(C3CCN(c4c(F)ccc5cccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1096530 8787 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 471 4 0 6 4.7 COc1cc(N2CCN(C3CCN(c4c(F)ccc5cccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
25140362 184328 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 8 2 3 4.6 CC(CCc1c[nH]c2ccc(F)cc12)N(CC1CC1)C1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm8007097
CHEMBL483370 184328 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 8 2 3 4.6 CC(CCc1c[nH]c2ccc(F)cc12)N(CC1CC1)C1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm8007097
44365679 41198 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assay
ChEMBL 437 4 1 6 4.6 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1csc4ccccc14)C3)CO2 10.1016/j.bmcl.2003.10.024
CHEMBL148860 41198 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assay
ChEMBL 437 4 1 6 4.6 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1csc4ccccc14)C3)CO2 10.1016/j.bmcl.2003.10.024
11394095 16814 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 354 7 2 3 3.8 Fc1cc2c(c(OCCNCCc3c[nH]c4ccccc34)c1)OCCC2 10.1021/jm0304010
CHEMBL124638 16814 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorEffective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 354 7 2 3 3.8 Fc1cc2c(c(OCCNCCc3c[nH]c4ccccc34)c1)OCCC2 10.1021/jm0304010
9998826 120541 None 0 Rat Functional pIC50 = 7.4 7.4 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
CHEMBL354210 120541 None 0 Rat Functional pIC50 = 7.4 7.4 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
11123104 165534 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 442 5 1 6 4.4 OC(CCN1CCN(c2cccc3c2OCCCO3)CC1)c1csc2ccc(F)cc12 10.1021/jm0111200
CHEMBL423896 165534 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 442 5 1 6 4.4 OC(CCN1CCN(c2cccc3c2OCCCO3)CC1)c1csc2ccc(F)cc12 10.1021/jm0111200
25139652 191693 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 9 1 4 4.5 NC(=O)c1ccc(F)c2c1CC(N(CCCCn1ccc3ccc(F)cc31)CC1CC1)CO2 10.1021/jm8007097
CHEMBL519514 191693 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 9 1 4 4.5 NC(=O)c1ccc(F)c2c1CC(N(CCCCn1ccc3ccc(F)cc31)CC1CC1)CO2 10.1021/jm8007097
145946714 167657 None 0 Human Functional pIC50 = 6.4 6.4 -4 4
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4213352 167657 None 0 Human Functional pIC50 = 6.4 6.4 -4 4
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4300399 167657 None 0 Human Functional pIC50 = 6.4 6.4 -4 4
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2cc(C)cc(C)c2C)CC1 10.1016/j.bmcl.2018.04.059
145962266 161735 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 459 8 0 7 4.2 CC(=O)c1c(OCCCCN2CCN(c3ccccc3C#N)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.ejmech.2017.05.047
CHEMBL4130132 161735 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 459 8 0 7 4.2 CC(=O)c1c(OCCCCN2CCN(c3ccccc3C#N)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.ejmech.2017.05.047
10046389 61436 None 0 Rat Functional pIC50 = 7.4 7.4 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
CHEMBL177031 61436 None 0 Rat Functional pIC50 = 7.4 7.4 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
9820163 4841 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 358 5 2 3 4.2 C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3[nH]ccc23)C1 10.1016/s0960-894x(01)00746-6
CHEMBL104229 4841 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 358 5 2 3 4.2 C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3[nH]ccc23)C1 10.1016/s0960-894x(01)00746-6
11260140 185063 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 479 8 2 3 5.1 O=C(NC1CC1)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL485385 185063 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 479 8 2 3 5.1 O=C(NC1CC1)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
2303 3187 None 44 Human Functional pIC50 = 5.4 5.4 -346 20
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
4946 3187 None 44 Human Functional pIC50 = 5.4 5.4 -346 20
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
564 3187 None 44 Human Functional pIC50 = 5.4 5.4 -346 20
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
63 3187 None 44 Human Functional pIC50 = 5.4 5.4 -346 20
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
91536 3187 None 44 Human Functional pIC50 = 5.4 5.4 -346 20
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
CHEMBL27 3187 None 44 Human Functional pIC50 = 5.4 5.4 -346 20
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
CHEMBL452861 3187 None 44 Human Functional pIC50 = 5.4 5.4 -346 20
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
DB00571 3187 None 44 Human Functional pIC50 = 5.4 5.4 -346 20
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as seretonin-induced cAMP level by HTRF assay
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/acs.jmedchem.5b01088
11293380 67415 None 0 Human Functional pIC50 = 8.4 8.4 1 2
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 395 6 1 4 4.2 Fc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)OCO5)CC3)c2c1 10.1021/acs.jmedchem.7b01788
CHEMBL188798 67415 None 0 Human Functional pIC50 = 8.4 8.4 1 2
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 395 6 1 4 4.2 Fc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)OCO5)CC3)c2c1 10.1021/acs.jmedchem.7b01788
3251 4072 None 43 Human Functional pIC50 = 8.4 8.4 -3 4
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm8007097
5684 4072 None 43 Human Functional pIC50 = 8.4 8.4 -3 4
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm8007097
80 4072 None 43 Human Functional pIC50 = 8.4 8.4 -3 4
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm8007097
CHEMBL31354 4072 None 43 Human Functional pIC50 = 8.4 8.4 -3 4
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm8007097
11261072 133642 None 0 Human Functional pIC50 = 8.4 8.4 - 1
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 492 6 0 6 4.4 C[C@H](CN(C(=O)c1ccc(Cl)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
CHEMBL371149 133642 None 0 Human Functional pIC50 = 8.4 8.4 - 1
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 492 6 0 6 4.4 C[C@H](CN(C(=O)c1ccc(Cl)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
11272673 69419 None 0 Human Functional pIC50 = 8.4 8.4 - 1
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 503 7 0 8 3.6 C[C@H](CN(C(=O)c1ccc([N+](=O)[O-])cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
CHEMBL193206 69419 None 0 Human Functional pIC50 = 8.4 8.4 - 1
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 503 7 0 8 3.6 C[C@H](CN(C(=O)c1ccc([N+](=O)[O-])cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
4431 2729 None 18 Human Functional pIC50 = 8.3 8.3 2884 2
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.bmcl.2018.04.059
73 2729 None 18 Human Functional pIC50 = 8.3 8.3 2884 2
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.bmcl.2018.04.059
CHEMBL8618 2729 None 18 Human Functional pIC50 = 8.3 8.3 2884 2
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.bmcl.2018.04.059
12004201 8743 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 481 4 0 6 5.2 COc1cc(N2CCN(C3CCN(c4cccc5c(C)cc(C)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1096155 8743 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 481 4 0 6 5.2 COc1cc(N2CCN(C3CCN(c4cccc5c(C)cc(C)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
3251 4072 None 43 Human Functional pIC50 = 8.3 8.3 -3 4
Antagonist activity against human recombinant 5-HT1A receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT1A receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2014.12.045
5684 4072 None 43 Human Functional pIC50 = 8.3 8.3 -3 4
Antagonist activity against human recombinant 5-HT1A receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT1A receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2014.12.045
80 4072 None 43 Human Functional pIC50 = 8.3 8.3 -3 4
Antagonist activity against human recombinant 5-HT1A receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT1A receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2014.12.045
CHEMBL31354 4072 None 43 Human Functional pIC50 = 8.3 8.3 -3 4
Antagonist activity against human recombinant 5-HT1A receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting methodAntagonist activity against human recombinant 5-HT1A receptor expressed in CHOK1 cells assessed as reduction in serotonin-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2014.12.045
11248217 122769 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 425 6 1 4 4.7 Clc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)OCCO5)CC3)c2c1 10.1021/acs.jmedchem.7b01788
CHEMBL360407 122769 None 0 Human Functional pIC50 = 7.4 7.4 1 2
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 425 6 1 4 4.7 Clc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)OCCO5)CC3)c2c1 10.1021/acs.jmedchem.7b01788
11845815 166452 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 427 8 2 3 4.2 CCCN(CCCc1c[nH]c2ccc(F)cc12)[C@H]1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm8007097
CHEMBL427411 166452 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 427 8 2 3 4.2 CCCN(CCCc1c[nH]c2ccc(F)cc12)[C@H]1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm8007097
25139643 184498 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 451 8 2 4 4.2 COc1ccc2[nH]cc(CCCN(C3CCC3)C3COc4c(F)ccc(C(N)=O)c4C3)c2c1 10.1021/jm8007097
CHEMBL484581 184498 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 451 8 2 4 4.2 COc1ccc2[nH]cc(CCCN(C3CCC3)C3COc4c(F)ccc(C(N)=O)c4C3)c2c1 10.1021/jm8007097
10116877 135279 None 7 Human Functional pIC50 = 7.4 7.4 - 1
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 483 6 0 7 3.6 C[C@H](CN(C(=O)c1ccc(C#N)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
CHEMBL372205 135279 None 7 Human Functional pIC50 = 7.4 7.4 - 1
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 483 6 0 7 3.6 C[C@H](CN(C(=O)c1ccc(C#N)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
25140055 185073 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 8 1 4 4.7 NC(=O)c1ccc(F)c2c1CC(N(CCCCn1ccc3ccc(F)cc31)C1CCC1)CO2 10.1021/jm8007097
CHEMBL485398 185073 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 8 1 4 4.7 NC(=O)c1ccc(F)c2c1CC(N(CCCCn1ccc3ccc(F)cc31)C1CCC1)CO2 10.1021/jm8007097
44593715 185078 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 411 4 3 3 3.2 NC(=O)c1ccc(F)c2c1C[C@@H](NCC1CCc3[nH]c4ccc(F)cc4c3C1)CO2 10.1021/jm8007097
CHEMBL485407 185078 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 411 4 3 3 3.2 NC(=O)c1ccc(F)c2c1C[C@@H](NCC1CCc3[nH]c4ccc(F)cc4c3C1)CO2 10.1021/jm8007097
86342156 149686 None 0 Human Functional pIC50 = 7.3 7.3 -33 4
Antagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assayAntagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay
ChEMBL 438 6 1 6 4.4 O=C(N[C@H]1CC[C@H](CCN2CCN(c3nsc4ccccc34)CC2)CC1)c1ccco1 10.1016/j.ejmech.2016.07.038
CHEMBL3946995 149686 None 0 Human Functional pIC50 = 7.3 7.3 -33 4
Antagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assayAntagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay
ChEMBL 438 6 1 6 4.4 O=C(N[C@H]1CC[C@H](CCN2CCN(c3nsc4ccccc34)CC2)CC1)c1ccco1 10.1016/j.ejmech.2016.07.038
12004227 8774 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 471 4 0 6 4.7 COc1cc(N2CCN(C3CCN(c4cc(F)cc5cccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1096477 8774 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 471 4 0 6 4.7 COc1cc(N2CCN(C3CCN(c4cc(F)cc5cccnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
12004197 8819 None 1 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 467 4 0 6 4.9 COc1cc(N2CCN(C3CCN(c4cccc5ccc(C)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1096802 8819 None 1 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 467 4 0 6 4.9 COc1cc(N2CCN(C3CCN(c4cccc5ccc(C)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
11845822 77599 None 5 Human Functional pIC50 = 7.3 7.3 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL208773 77599 None 5 Human Functional pIC50 = 7.3 7.3 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
145963224 161593 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 450 8 0 7 3.9 COc1cccc(N2CCN(CCCOc3ccc4c(C)cc(=O)oc4c3C(C)=O)CC2)c1 10.1016/j.ejmech.2017.05.047
CHEMBL4128053 161593 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 450 8 0 7 3.9 COc1cccc(N2CCN(CCCOc3ccc4c(C)cc(=O)oc4c3C(C)=O)CC2)c1 10.1016/j.ejmech.2017.05.047
44220112 197651 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 426 3 0 6 4.1 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4ccccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL550576 197651 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 426 3 0 6 4.1 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4ccccc4n2)CC1)O3 10.1021/jm900374r
11845636 79455 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 408 7 1 3 5.1 COc1cccc2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL211363 79455 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 408 7 1 3 5.1 COc1cccc2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
11751188 66966 None 0 Human Functional pIC50 = 8.3 8.3 1 3
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 409 6 1 4 4.2 Fc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)OCCO5)CC3)c2c1 10.1021/acs.jmedchem.7b01788
CHEMBL186655 66966 None 0 Human Functional pIC50 = 8.3 8.3 1 3
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 409 6 1 4 4.2 Fc1ccc2[nH]cc(CCCCN3CCN(c4ccc5c(c4)OCCO5)CC3)c2c1 10.1021/acs.jmedchem.7b01788
4431 2729 None 18 Human Functional pIC50 = 8.3 8.3 2884 2
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.ejmech.2017.05.047
73 2729 None 18 Human Functional pIC50 = 8.3 8.3 2884 2
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.ejmech.2017.05.047
CHEMBL8618 2729 None 18 Human Functional pIC50 = 8.3 8.3 2884 2
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1016/j.ejmech.2017.05.047
46238348 9019 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 471 4 0 6 4.7 COc1cc(N2CCN(C3CCN(c4cccc5cc(F)cnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1098483 9019 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 471 4 0 6 4.7 COc1cc(N2CCN(C3CCN(c4cccc5cc(F)cnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
12004199 8570 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 467 4 0 6 4.9 COc1cc(N2CCN(C3CCN(c4cccc5cc(C)cnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1094556 8570 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 467 4 0 6 4.9 COc1cc(N2CCN(C3CCN(c4cccc5cc(C)cnc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
11374428 141736 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 453 9 2 3 4.6 NC(=O)c1ccc(F)c2c1CC(N(CCCCc1c[nH]c3ccc(F)cc13)CC1CC1)CO2 10.1021/jm060218h
CHEMBL385353 141736 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 453 9 2 3 4.6 NC(=O)c1ccc(F)c2c1CC(N(CCCCc1c[nH]c3ccc(F)cc13)CC1CC1)CO2 10.1021/jm060218h
11270594 192442 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3cc(F)ccc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL520661 192442 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3cc(F)ccc13)C1CCC1)CO2 10.1021/jm8007097
2477 745 None 38 Rat Functional pIC50 = 7.3 7.3 1 20
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
2477.0 745 None 38 Rat Functional pIC50 = 7.3 7.3 1 20
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
36 745 None 38 Rat Functional pIC50 = 7.3 7.3 1 20
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
437 745 None 38 Rat Functional pIC50 = 7.3 7.3 1 20
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
CHEMBL49 745 None 38 Rat Functional pIC50 = 7.3 7.3 1 20
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
DB00490 745 None 38 Rat Functional pIC50 = 7.3 7.3 1 20
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
10474964 130539 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 130539 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 130539 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
44335519 107564 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 369 5 1 3 4.9 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3ncccc23)C1 10.1016/s0960-894x(01)00746-6
CHEMBL318604 107564 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 369 5 1 3 4.9 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3ncccc23)C1 10.1016/s0960-894x(01)00746-6
25138913 192709 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 451 8 2 4 4.2 COc1cccc2c(CCCN(C3CCC3)C3COc4c(F)ccc(C(N)=O)c4C3)c[nH]c12 10.1021/jm8007097
CHEMBL521510 192709 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 451 8 2 4 4.2 COc1cccc2c(CCCN(C3CCC3)C3COc4c(F)ccc(C(N)=O)c4C3)c[nH]c12 10.1021/jm8007097
10319395 115514 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 410 5 1 6 3.9 OC(CCN1CCN(c2cccc3c2OCCO3)CC1)c1csc2ccccc12 10.1021/jm0111200
CHEMBL335082 115514 None 0 Rat Functional pIC50 = 7.3 7.3 - 1
Inhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranesInhibition of (+)-8-OH-DPAT stimulated [35S]GTP-gamma-S, binding to 5-hydroxytryptamine 1A receptor in hippocampal membranes
ChEMBL 410 5 1 6 3.9 OC(CCN1CCN(c2cccc3c2OCCO3)CC1)c1csc2ccccc12 10.1021/jm0111200
9866320 198770 None 5 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 411 3 1 4 5.0 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CC=C(c2c[nH]c4ccccc24)CC1)O3 10.1021/jm900374r
CHEMBL562248 198770 None 5 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 411 3 1 4 5.0 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CC=C(c2c[nH]c4ccccc24)CC1)O3 10.1021/jm900374r
145947937 167825 None 0 Human Functional pIC50 = 7.3 7.3 1 4
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4207653 167825 None 0 Human Functional pIC50 = 7.3 7.3 1 4
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4302655 167825 None 0 Human Functional pIC50 = 7.3 7.3 1 4
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 398 9 0 5 3.8 COc1ccccc1N1CCN(CCOCCOc2c(C)cc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
135339817 181590 None 0 Human Functional pIC50 = 7.3 7.3 -8 5
Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
CHEMBL4764679 181590 None 0 Human Functional pIC50 = 7.3 7.3 -8 5
Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assayAntagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay
ChEMBL 437 6 0 5 4.2 CN1CCc2ccc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)cc2C1=O 10.1016/j.ejmech.2020.112709
44220315 199067 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 465 3 0 7 4.3 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCCN(c2ccc4cc(C#N)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL564148 199067 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 465 3 0 7 4.3 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCCN(c2ccc4cc(C#N)ccc4n2)CC1)O3 10.1021/jm900374r
129103318 167410 None 0 Human Functional pIC50 = 6.2 6.2 -64 6
Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 167410 None 0 Human Functional pIC50 = 6.2 6.2 -64 6
Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assayAntagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
44220111 197710 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 510 4 0 7 5.0 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(OC(F)(F)F)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL551105 197710 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 510 4 0 7 5.0 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(OC(F)(F)F)ccc4n2)CC1)O3 10.1021/jm900374r
145946733 167679 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 368 7 0 4 4.2 COc1ccc(N2CCN(CCCOc3c(C)cc(C)cc3C)CC2)cc1 10.1016/j.bmcl.2018.04.059
CHEMBL4205526 167679 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 368 7 0 4 4.2 COc1ccc(N2CCN(CCCOc3c(C)cc(C)cc3C)CC2)cc1 10.1016/j.bmcl.2018.04.059
CHEMBL4300710 167679 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 368 7 0 4 4.2 COc1ccc(N2CCN(CCCOc3c(C)cc(C)cc3C)CC2)cc1 10.1016/j.bmcl.2018.04.059
11444410 168569 None 0 Human Functional pIC50 = 8.2 8.2 - 1
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 526 6 0 6 4.7 C[C@H](CN(C(=O)c1ccc(C(F)(F)F)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
CHEMBL435111 168569 None 0 Human Functional pIC50 = 8.2 8.2 - 1
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 526 6 0 6 4.7 C[C@H](CN(C(=O)c1ccc(C(F)(F)F)cc1)c1ccccn1)N1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm049493z
3251 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Antagonist activity at 5-HT1A receptor (unknown origin) by calcium flux assayAntagonist activity at 5-HT1A receptor (unknown origin) by calcium flux assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.3c00734
5684 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Antagonist activity at 5-HT1A receptor (unknown origin) by calcium flux assayAntagonist activity at 5-HT1A receptor (unknown origin) by calcium flux assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.3c00734
80 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Antagonist activity at 5-HT1A receptor (unknown origin) by calcium flux assayAntagonist activity at 5-HT1A receptor (unknown origin) by calcium flux assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.3c00734
CHEMBL31354 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Antagonist activity at 5-HT1A receptor (unknown origin) by calcium flux assayAntagonist activity at 5-HT1A receptor (unknown origin) by calcium flux assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.3c00734
11293572 140206 None 3 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm060218h
CHEMBL380095 140206 None 3 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm060218h
44593717 175094 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 465 6 2 3 4.4 NC(=O)c1ccc(F)c2c1C[C@@H](N(CC1CC1)CC1CCc3[nH]c4ccc(F)cc4c3C1)CO2 10.1021/jm8007097
CHEMBL456657 175094 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 465 6 2 3 4.4 NC(=O)c1ccc(F)c2c1C[C@@H](N(CC1CC1)CC1CCc3[nH]c4ccc(F)cc4c3C1)CO2 10.1021/jm8007097
25138907 175592 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 441 8 2 3 4.5 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2c(F)ccc(C(=O)NC)c2C1 10.1021/jm8007097
CHEMBL457750 175592 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 441 8 2 3 4.5 CCCN(CCCc1c[nH]c2ccc(F)cc12)C1COc2c(F)ccc(C(=O)NC)c2C1 10.1021/jm8007097
46225309 202596 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 454 8 2 4 4.3 N#Cc1ccc2[nH]cc(CCCCN(CC3CC3)C3COc4ccc5c(c4C3)C(=O)NC5)c2c1 10.1016/j.bmcl.2009.10.134
CHEMBL596297 202596 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activityAgonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
ChEMBL 454 8 2 4 4.3 N#Cc1ccc2[nH]cc(CCCCN(CC3CC3)C3COc4ccc5c(c4C3)C(=O)NC5)c2c1 10.1016/j.bmcl.2009.10.134
25139058 184497 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 421 7 2 3 4.2 NC(=O)c1cccc2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL484580 184497 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 421 7 2 3 4.2 NC(=O)c1cccc2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL484747 184497 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 421 7 2 3 4.2 NC(=O)c1cccc2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
11845817 166383 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 439 8 2 3 4.2 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)CC1CC1)CO2 10.1021/jm060218h
CHEMBL427051 166383 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 439 8 2 3 4.2 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)CC1CC1)CO2 10.1021/jm060218h
11246169 116997 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 386 8 3 3 4.4 Fc1ccc2[nH]cc(CCCNCCOc3cc(Cl)cc4[nH]cnc34)c2c1 10.1021/jm0304010
CHEMBL338520 116997 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 386 8 3 3 4.4 Fc1ccc2[nH]cc(CCCNCCOc3cc(Cl)cc4[nH]cnc34)c2c1 10.1021/jm0304010
44335674 109776 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 396 5 1 4 4.3 Fc1ccc2c(C3CCN(CCOc4cccc5c4OCCO5)CC3)c[nH]c2c1 10.1016/s0960-894x(01)00746-6
CHEMBL322915 109776 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 396 5 1 4 4.3 Fc1ccc2c(C3CCN(CCOc4cccc5c4OCCO5)CC3)c[nH]c2c1 10.1016/s0960-894x(01)00746-6
11846005 78163 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 399 6 2 3 3.4 CCN(CCc1c[nH]c2ccc(F)cc12)C1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm060218h
CHEMBL210348 78163 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 399 6 2 3 3.4 CCN(CCc1c[nH]c2ccc(F)cc12)C1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm060218h
11177435 80227 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 413 7 2 3 3.8 CCCN(CCc1c[nH]c2ccc(F)cc12)C1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm060218h
CHEMBL213639 80227 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 413 7 2 3 3.8 CCCN(CCc1c[nH]c2ccc(F)cc12)C1COc2c(F)ccc(C(N)=O)c2C1 10.1021/jm060218h
10111229 5070 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 394 5 1 4 4.2 Fc1ccc2[nH]cc(C3=CCN(CCOc4cccc5c4OCCO5)CC3)c2c1 10.1016/s0960-894x(01)00746-6
CHEMBL105390 5070 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,Antagonism of 5-hydroxytryptamine 1A receptor was determined in vitro using a [35S]GTP-gamma-S,
ChEMBL 394 5 1 4 4.2 Fc1ccc2[nH]cc(C3=CCN(CCOc4cccc5c4OCCO5)CC3)c2c1 10.1016/s0960-894x(01)00746-6
44335519 107564 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 369 5 1 3 4.9 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3ncccc23)C1 10.1016/s0960-894x(01)00746-6
CHEMBL318604 107564 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 369 5 1 3 4.9 C1=C(c2c[nH]c3ccccc23)CCN(CCOc2cccc3ncccc23)C1 10.1016/s0960-894x(01)00746-6
12004254 8887 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 539 4 0 6 5.7 COc1cc(N2CCN(C3CCN(c4ccc(F)c5ccc(C(F)(F)F)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1097484 8887 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 539 4 0 6 5.7 COc1cc(N2CCN(C3CCN(c4ccc(F)c5ccc(C(F)(F)F)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
3251 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm060218h
5684 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm060218h
80 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm060218h
CHEMBL31354 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm060218h
3251 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1000908
5684 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1000908
80 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1000908
CHEMBL31354 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1000908
3251 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm049493z
5684 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm049493z
80 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm049493z
CHEMBL31354 4072 None 43 Human Functional pIC50 = 8.2 8.2 -3 4
In vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptorIn vitro antagonism of 8-OH-DPAT inhibition of forskolin-induced cAMP production in CHO cells expressing 5-HT1A receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm049493z
145946966 167697 None 0 Human Functional pIC50 = 8.1 8.1 2 3
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 354 7 0 4 3.9 COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4209888 167697 None 0 Human Functional pIC50 = 8.1 8.1 2 3
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 354 7 0 4 3.9 COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
CHEMBL4300899 167697 None 0 Human Functional pIC50 = 8.1 8.1 2 3
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 354 7 0 4 3.9 COc1ccccc1N1CCN(CCCOc2ccc(C)cc2C)CC1 10.1016/j.bmcl.2018.04.059
11845819 78046 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 439 8 2 3 4.2 NC(=O)c1ccc(F)c2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)CC1CC1)CO2 10.1021/jm060218h
CHEMBL209802 78046 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 439 8 2 3 4.2 NC(=O)c1ccc(F)c2c1C[C@@H](N(CCCc1c[nH]c3ccc(F)cc13)CC1CC1)CO2 10.1021/jm060218h
44220314 197735 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 440 3 0 6 4.4 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCCN(c2ccc4ccccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL551304 197735 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 440 3 0 6 4.4 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCCN(c2ccc4ccccc4n2)CC1)O3 10.1021/jm900374r
44220316 197826 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 458 3 0 6 4.6 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCCN(c2ccc4cc(F)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL551909 197826 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 458 3 0 6 4.6 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCCN(c2ccc4cc(F)ccc4n2)CC1)O3 10.1021/jm900374r
4106 2502 None 21 Human Functional pIC50 = 7.2 7.2 -186 7
Antagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assayAntagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2016.07.038
5358812 2502 None 21 Human Functional pIC50 = 7.2 7.2 -186 7
Antagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assayAntagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2016.07.038
89 2502 None 21 Human Functional pIC50 = 7.2 7.2 -186 7
Antagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assayAntagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2016.07.038
CHEMBL93240 2502 None 21 Human Functional pIC50 = 7.2 7.2 -186 7
Antagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assayAntagonistic activity at 5-HT1A receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 assessed as inhibition of serotonin-induced calcium flux by Fluo-4 based FLIPR assay
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1016/j.ejmech.2016.07.038
25138912 184350 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 455 7 2 3 4.9 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(Cl)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL483573 184350 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 455 7 2 3 4.9 NC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(Cl)cc13)C1CCC1)CO2 10.1021/jm8007097
10046389 61436 None 0 Rat Functional pIC50 = 7.1 7.1 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
CHEMBL177031 61436 None 0 Rat Functional pIC50 = 7.1 7.1 - 1
Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampusInhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
25139366 175594 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 441 8 2 3 4.5 CCCN(CCCc1c[nH]c2ccc(F)cc12)[C@H]1COc2c(F)ccc(C(=O)NC)c2C1 10.1021/jm8007097
CHEMBL457751 175594 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 441 8 2 3 4.5 CCCN(CCCc1c[nH]c2ccc(F)cc12)[C@H]1COc2c(F)ccc(C(=O)NC)c2C1 10.1021/jm8007097
44269674 39314 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
In vitro Inhibitory activity tested at 5-hydroxytryptamine 1A receptor binding site in ratIn vitro Inhibitory activity tested at 5-hydroxytryptamine 1A receptor binding site in rat
ChEMBL 261 5 1 2 3.6 CCCN(CCC)[C@H]1Cc2c(O)cccc2C[C@H]1C 10.1021/jm00401a012
CHEMBL14708 39314 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
In vitro Inhibitory activity tested at 5-hydroxytryptamine 1A receptor binding site in ratIn vitro Inhibitory activity tested at 5-hydroxytryptamine 1A receptor binding site in rat
ChEMBL 261 5 1 2 3.6 CCCN(CCC)[C@H]1Cc2c(O)cccc2C[C@H]1C 10.1021/jm00401a012
CHEMBL544668 39314 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
In vitro Inhibitory activity tested at 5-hydroxytryptamine 1A receptor binding site in ratIn vitro Inhibitory activity tested at 5-hydroxytryptamine 1A receptor binding site in rat
ChEMBL 261 5 1 2 3.6 CCCN(CCC)[C@H]1Cc2c(O)cccc2C[C@H]1C 10.1021/jm00401a012
9890484 198412 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 460 3 0 6 4.7 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(Cl)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL559579 198412 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 460 3 0 6 4.7 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(Cl)ccc4n2)CC1)O3 10.1021/jm900374r
10090661 118232 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 372 7 2 3 4.0 Fc1cc2c(c(OCCNCCc3c[nH]c4ccc(F)cc34)c1)OCCC2 10.1021/jm0304010
CHEMBL340873 118232 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptorInhibition concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing 5-hydroxytryptamine 1A receptor
ChEMBL 372 7 2 3 4.0 Fc1cc2c(c(OCCNCCc3c[nH]c4ccc(F)cc34)c1)OCCC2 10.1021/jm0304010
11773729 125498 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 391 6 1 4 4.1 c1ccc2c(CCCCN3CCN(c4ccc5c(c4)OCCO5)CC3)c[nH]c2c1 10.1021/acs.jmedchem.7b01788
CHEMBL364610 125498 None 0 Human Functional pIC50 = 8.1 8.1 1 2
Agonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting methodAgonist activity at human 5HT1A expressed in CHO cell membranes assessed as increase in [35S]-GTPgammaS binding after 30 mins by liquid scintillation counting method
ChEMBL 391 6 1 4 4.1 c1ccc2c(CCCCN3CCN(c4ccc5c(c4)OCCO5)CC3)c[nH]c2c1 10.1021/acs.jmedchem.7b01788
3251 4072 None 43 Human Functional pIC50 = 8.1 8.1 -3 4
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm049493z
5684 4072 None 43 Human Functional pIC50 = 8.1 8.1 -3 4
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm049493z
80 4072 None 43 Human Functional pIC50 = 8.1 8.1 -3 4
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm049493z
CHEMBL31354 4072 None 43 Human Functional pIC50 = 8.1 8.1 -3 4
In vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cellsIn vitro inhibition of 8-OH-DPAT-induced [35S]GTP-gamma-S, binding to 5-HT1A receptor/G protein complex in CHO cells
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm049493z
11202474 184737 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 481 9 2 3 5.4 CCCNC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL484947 184737 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 481 9 2 3 5.4 CCCNC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
25140648 185095 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 7 2 3 4.6 CNC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL485433 185095 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 453 7 2 3 4.6 CNC(=O)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
12004141 8798 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 569 5 0 7 5.7 COc1cc(N2CCN(C3CCN(c4ccc(F)c5c(OC)cc(C(F)(F)F)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
CHEMBL1096671 8798 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP levelAntagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level
ChEMBL 569 5 0 7 5.7 COc1cc(N2CCN(C3CCN(c4ccc(F)c5c(OC)cc(C(F)(F)F)nc45)CC3)CC2)c2ncccc2c1 10.1021/jm1000908
44365671 38930 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assay
ChEMBL 431 4 1 5 4.5 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1ccc4ccccc4c1)C3)CO2 10.1016/j.bmcl.2003.10.024
CHEMBL146751 38930 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Agonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assayAgonistic activity of compound towards 5-hydroxytryptamine 1A receptor was evaluated by [35S]GTP-gamma-S, stimulated cAMP assay
ChEMBL 431 4 1 5 4.5 COc1cccc2c1O[C@@H](CN1[C@H]3CC[C@@H]1C[C@@](O)(c1ccc4ccccc4c1)C3)CO2 10.1016/j.bmcl.2003.10.024
9842337 169515 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 370 5 1 4 4.3 C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3ncccc23)C1 10.1016/s0960-894x(01)00746-6
CHEMBL442391 169515 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 370 5 1 4 4.3 C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3ncccc23)C1 10.1016/s0960-894x(01)00746-6
11477432 191803 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 493 8 2 3 5.5 O=C(NC1CCC1)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
CHEMBL519679 191803 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Activity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS bindingActivity at human cloned 5HT1A receptor expressed in CHO cells assessed as blockade of 5-HT-stimulated [35S]GTPgammaS binding
ChEMBL 493 8 2 3 5.5 O=C(NC1CCC1)c1ccc(F)c2c1CC(N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm8007097
44335674 109776 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 396 5 1 4 4.3 Fc1ccc2c(C3CCN(CCOc4cccc5c4OCCO5)CC3)c[nH]c2c1 10.1016/s0960-894x(01)00746-6
CHEMBL322915 109776 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonism of 5-hydroxytryptamine 1A receptor determined in vitroAntagonism of 5-hydroxytryptamine 1A receptor determined in vitro
ChEMBL 396 5 1 4 4.3 Fc1ccc2c(C3CCN(CCOc4cccc5c4OCCO5)CC3)c[nH]c2c1 10.1016/s0960-894x(01)00746-6
11845824 77600 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1C[C@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm060218h
CHEMBL208774 77600 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 439 7 2 3 4.3 NC(=O)c1ccc(F)c2c1C[C@H](N(CCCc1c[nH]c3ccc(F)cc13)C1CCC1)CO2 10.1021/jm060218h
9842682 107588 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonism at the 5-hydroxytryptamine 1A receptor in vitroAntagonism at the 5-hydroxytryptamine 1A receptor in vitro
ChEMBL 377 5 1 5 3.5 C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3c2OCCO3)C1 10.1016/s0960-894x(01)00746-6
CHEMBL318738 107588 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonism at the 5-hydroxytryptamine 1A receptor in vitroAntagonism at the 5-hydroxytryptamine 1A receptor in vitro
ChEMBL 377 5 1 5 3.5 C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3c2OCCO3)C1 10.1016/s0960-894x(01)00746-6
11418868 139441 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 425 7 2 3 3.8 NC(=O)c1ccc(F)c2c1CC(N(CCc1c[nH]c3ccc(F)cc13)CC1CC1)CO2 10.1021/jm060218h
CHEMBL379298 139441 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Agonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP productionAgonist activity at human 5HT1A receptor expressed in CHO cells by inhibition of 8-OH-DPAT-induced decrease in forskolin-stimulated cAMP production
ChEMBL 425 7 2 3 3.8 NC(=O)c1ccc(F)c2c1CC(N(CCc1c[nH]c3ccc(F)cc13)CC1CC1)CO2 10.1021/jm060218h
145961144 161678 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 445 7 0 7 3.8 CC(=O)c1c(OCCCN2CCN(c3ccccc3C#N)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.ejmech.2017.05.047
CHEMBL4129293 161678 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assayAntagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay
ChEMBL 445 7 0 7 3.8 CC(=O)c1c(OCCCN2CCN(c3ccccc3C#N)CC2)ccc2c(C)cc(=O)oc12 10.1016/j.ejmech.2017.05.047
10344103 105677 None 0 Rat Functional pKd = 10.1 10.1 - 0
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)
ChEMBL 457 6 0 7 2.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
CHEMBL312339 105677 None 0 Rat Functional pKd = 10.1 10.1 - 0
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)
ChEMBL 457 6 0 7 2.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
9848499 207758 None 22 Rat Functional pKd = 10.1 10.1 - 0
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)
ChEMBL 491 6 0 7 2.9 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cc(Cl)cc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
CHEMBL79261 207758 None 22 Rat Functional pKd = 10.1 10.1 - 0
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)
ChEMBL 491 6 0 7 2.9 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cc(Cl)cc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
11655728 16651 None 7 Human Functional pKd = 9.7 9.7 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241913 16651 None 7 Human Functional pKd = 9.7 9.7 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
3251 4072 None 43 Rat Functional pKd = 9.7 9.7 3 4
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/s0960-894x(98)00406-5
5684 4072 None 43 Rat Functional pKd = 9.7 9.7 3 4
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/s0960-894x(98)00406-5
80 4072 None 43 Rat Functional pKd = 9.7 9.7 3 4
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/s0960-894x(98)00406-5
CHEMBL31354 4072 None 43 Rat Functional pKd = 9.7 9.7 3 4
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/s0960-894x(98)00406-5
9848499 207758 None 22 Rat Functional pKd = 9.5 9.5 - 0
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 2)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 2)
ChEMBL 491 6 0 7 2.9 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cc(Cl)cc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
CHEMBL79261 207758 None 22 Rat Functional pKd = 9.5 9.5 - 0
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 2)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 2)
ChEMBL 491 6 0 7 2.9 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cc(Cl)cc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
10344103 105677 None 0 Rat Functional pKd = 9.4 9.4 - 0
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 2)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 2)
ChEMBL 457 6 0 7 2.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
CHEMBL312339 105677 None 0 Rat Functional pKd = 9.4 9.4 - 0
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 2)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 2)
ChEMBL 457 6 0 7 2.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1016/s0960-894x(98)00406-5
10405775 104964 None 0 Rat Functional pKd = 7.8 7.8 - 1
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)
ChEMBL 352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL311275 104964 None 0 Rat Functional pKd = 7.8 7.8 - 1
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)
ChEMBL 352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1 10.1016/s0960-894x(98)00406-5
CHEMBL543139 104964 None 0 Rat Functional pKd = 7.8 7.8 - 1
Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes (experiment 1)
ChEMBL 352 6 0 4 3.6 c1ccc(CCCCN2CCN(c3cccc4c3OCCO4)CC2)cc1 10.1016/s0960-894x(98)00406-5
10020855 189379 None 0 Human Functional pKi = 10.6 10.6 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysisAgonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysis
ChEMBL 351 4 0 4 3.9 COc1cccc([C@H]2CC[C@H](N3CCN(c4ccccn4)CC3)CC2)c1 10.1016/j.bmc.2015.05.042
CHEMBL511857 189379 None 0 Human Functional pKi = 10.6 10.6 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysisAgonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysis
ChEMBL 351 4 0 4 3.9 COc1cccc([C@H]2CC[C@H](N3CCN(c4ccccn4)CC3)CC2)c1 10.1016/j.bmc.2015.05.042
9909089 187074 None 0 Human Functional pKi = 10.2 10.2 - 1
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL490417 187074 None 0 Human Functional pKi = 10.2 10.2 - 1
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
9909089 187074 None 0 Human Functional pKi = 10.2 10.2 - 1
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL490417 187074 None 0 Human Functional pKi = 10.2 10.2 - 1
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
46900606 16632 None 0 Human Functional pKi = 10.1 10.1 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C)nnn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241546 16632 None 0 Human Functional pKi = 10.1 10.1 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C)nnn4-5)CC3)cccc2n1 10.1021/jm100482n
46900459 16645 None 0 Human Functional pKi = 10.1 10.1 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnc(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241738 16645 None 0 Human Functional pKi = 10.1 10.1 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnc(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
9979309 193091 None 0 Human Functional pKi = 10.1 10.1 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL522257 193091 None 0 Human Functional pKi = 10.1 10.1 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
9979309 193091 None 0 Human Functional pKi = 10.1 10.1 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL522257 193091 None 0 Human Functional pKi = 10.1 10.1 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
18922713 98551 None 0 Rat Functional pKi = 10.1 10.1 - 1
Inhibition constant of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorInhibition constant of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 10.1021/jm000339w
CHEMBL276031 98551 None 0 Rat Functional pKi = 10.1 10.1 - 1
Inhibition constant of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptorInhibition constant of 50 uM forskolin-stimulated cAMP accumulation against 5-hydroxytryptamine 1A receptor
ChEMBL 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 10.1021/jm000339w
44592250 178958 None 0 Human Functional pKi = 10 10.0 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 442 5 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C4CC4)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469568 178958 None 0 Human Functional pKi = 10 10.0 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 442 5 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C4CC4)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
46900954 16659 None 0 Human Functional pKi = 9.9 9.9 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 6 1 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242081 16659 None 0 Human Functional pKi = 9.9 9.9 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 6 1 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46899637 16667 None 0 Human Functional pKi = 9.9 9.9 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 7 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NCC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242345 16667 None 0 Human Functional pKi = 9.9 9.9 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 7 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NCC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46899639 16676 None 0 Human Functional pKi = 9.9 9.9 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 5 0 7 4.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242533 16676 None 0 Human Functional pKi = 9.9 9.9 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 5 0 7 4.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46900150 16703 None 0 Human Functional pKi = 9.9 9.9 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nccn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242904 16703 None 0 Human Functional pKi = 9.9 9.9 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nccn4-5)CC3)cccc2n1 10.1021/jm100482n
44592209 179286 None 0 Human Functional pKi = 9.9 9.9 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 5 0 5 3.7 CCN1C(=O)COc2c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc21 10.1016/j.bmcl.2009.02.056
CHEMBL472290 179286 None 0 Human Functional pKi = 9.9 9.9 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 5 0 5 3.7 CCN1C(=O)COc2c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc21 10.1016/j.bmcl.2009.02.056
46900455 16640 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 493 4 0 6 5.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C(F)(F)F)cn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241641 16640 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 493 4 0 6 5.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C(F)(F)F)cn4-5)CC3)cccc2n1 10.1021/jm100482n
46900776 16646 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 496 5 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241824 16646 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 496 5 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
11712756 16650 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 482 5 1 7 3.3 CNC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241912 16650 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 482 5 1 7 3.3 CNC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
46900956 16661 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 6 1 7 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242167 16661 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 6 1 7 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46899638 16671 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 5 0 7 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242436 16671 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 5 0 7 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
44138104 178938 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1021/jm100482n
CHEMBL469345 178938 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1021/jm100482n
44138104 178938 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL469345 178938 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44138104 178938 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469345 178938 None 0 Human Functional pKi = 9.8 9.8 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
10948133 165374 None 0 Human Functional pKi = 9.8 9.8 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysisAgonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysis
ChEMBL 351 5 0 4 3.4 COc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)CC2 10.1016/j.bmc.2015.05.042
CHEMBL423181 165374 None 0 Human Functional pKi = 9.8 9.8 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysisAgonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysis
ChEMBL 351 5 0 4 3.4 COc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)CC2 10.1016/j.bmc.2015.05.042
46900451 16633 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 439 4 0 6 4.3 Cc1cn2c(n1)COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241547 16633 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 439 4 0 6 4.3 Cc1cn2c(n1)COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
46900453 16634 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 453 4 0 6 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C)c(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241548 16634 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 453 4 0 6 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C)c(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
46900457 16641 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4cncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241642 16641 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4cncn4-5)CC3)cccc2n1 10.1021/jm100482n
46900782 16655 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 510 6 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241998 16655 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 510 6 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
44592296 178941 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 434 4 0 5 3.4 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469374 178941 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 434 4 0 5 3.4 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
44592297 189599 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 448 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL513875 189599 None 0 Human Functional pKi = 9.7 9.7 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 448 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
9868889 72654 None 0 Human Functional pKi = 9.7 9.7 - 0
Displacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptorDisplacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cccnc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL199443 72654 None 0 Human Functional pKi = 9.7 9.7 - 0
Displacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptorDisplacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cccnc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
10787793 13400 None 0 Rat Functional pKi = 9.7 9.7 - 0
Antagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptorAntagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptor
ChEMBL 411 6 1 4 3.5 COc1ccccc1N1CCN(C[C@@H](C)NC(=O)C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)CC1 10.1021/jm9806704
CHEMBL1192653 13400 None 0 Rat Functional pKi = 9.7 9.7 - 0
Antagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptorAntagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptor
ChEMBL 411 6 1 4 3.5 COc1ccccc1N1CCN(C[C@@H](C)NC(=O)C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)CC1 10.1021/jm9806704
CHEMBL543932 13400 None 0 Rat Functional pKi = 9.7 9.7 - 0
Antagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptorAntagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptor
ChEMBL 411 6 1 4 3.5 COc1ccccc1N1CCN(C[C@@H](C)NC(=O)C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)CC1 10.1021/jm9806704
44364825 13837 None 0 Rat Functional pKi = 9.6 9.6 - 0
Antagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptorAntagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptor
ChEMBL 383 6 1 4 2.8 COc1ccccc1N1CCN(CCNC(=O)C23CC4C[C@@H](C[C@H]2C4)C3)CC1 10.1021/jm9806704
CHEMBL1195804 13837 None 0 Rat Functional pKi = 9.6 9.6 - 0
Antagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptorAntagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptor
ChEMBL 383 6 1 4 2.8 COc1ccccc1N1CCN(CCNC(=O)C23CC4C[C@@H](C[C@H]2C4)C3)CC1 10.1021/jm9806704
CHEMBL555379 13837 None 0 Rat Functional pKi = 9.6 9.6 - 0
Antagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptorAntagonist activity against rat hippocampal tissue 5-hydroxytryptamine 1A receptor
ChEMBL 383 6 1 4 2.8 COc1ccccc1N1CCN(CCNC(=O)C23CC4C[C@@H](C[C@H]2C4)C3)CC1 10.1021/jm9806704
46900958 16666 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 6 1 7 4.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242257 16666 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 6 1 7 4.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
44138098 189581 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL513715 189581 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1021/jm100482n
44138098 189581 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL513715 189581 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1A receptor expressed in HEK293 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44592207 189472 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL512724 189472 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
44138098 189581 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL513715 189581 None 0 Human Functional pKi = 9.6 9.6 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
44405730 169022 None 0 Human Functional pKi = 9.5 9.5 - 0
Displacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptorDisplacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccncc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL438619 169022 None 0 Human Functional pKi = 9.5 9.5 - 0
Displacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptorDisplacement of [35S]GTP-gamma-S from human recombinant 5HT1A receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccncc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
10248163 31571 None 0 Human Functional pKi = 9.5 9.5 -288 3
Agonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysisAgonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysis
ChEMBL 363 5 0 4 4.0 COc1cccc2c1CCC/C2=C\CCN1CCN(c2ccccn2)CC1 10.1016/j.bmc.2015.05.042
CHEMBL140406 31571 None 0 Human Functional pKi = 9.5 9.5 -288 3
Agonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysisAgonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysis
ChEMBL 363 5 0 4 4.0 COc1cccc2c1CCC/C2=C\CCN1CCN(c2ccccn2)CC1 10.1016/j.bmc.2015.05.042
46900612 16643 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 467 5 0 7 4.2 CC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241736 16643 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 467 5 0 7 4.2 CC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
11655728 16651 None 7 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241913 16651 None 7 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
44592294 189372 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 4 0 5 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL511815 189372 None 0 Human Functional pKi = 9.5 9.5 - 0
Antagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1A assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 4 0 5 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
11046644 30712 None 0 Human Functional pKi = 9.4 9.4 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysisAgonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysis
ChEMBL 361 6 0 4 4.0 COc1cccc2c(CCCN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2015.05.042
CHEMBL139505 30712 None 0 Human Functional pKi = 9.4 9.4 - 1
Agonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysisAgonist activity at human 5-HT1A receptor expressed in human HeLa cell membranes assessed as stimulation of [35S]GTPgammaS binding after 20 mins by liquid scintillation counting analysis
ChEMBL 361 6 0 4 4.0 COc1cccc2c(CCCN3CCN(c4ccccn4)CC3)cccc12 10.1016/j.bmc.2015.05.042
46899640 16683 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 5 0 7 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242623 16683 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillati