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Assay Detail

CHEMBL895214

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Functional
Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity.
Maurel JL, Autin JM, Funes P, Newman-Tancredi A, Colpaert F, Vacher B.
J Med Chem (2007) 50 : 5024 -5033
PubMed 17803293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 6.70 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231471 1 8.00
CHEMBL45305 BEFIRADOL 2.0 1 7.63
CHEMBL56 8-OH-DPAT 1 7.49
CHEMBL396062 1 7.37
CHEMBL425833 1 7.16
CHEMBL394606 1 7.07
CHEMBL394778 1 7.05
CHEMBL209821 NALUZOTAN 3.0 1 7.03
CHEMBL231273 1 6.81
CHEMBL39 SEROTONIN 3.0 1 6.64
CHEMBL394530 1 6.64
CHEMBL230327 1 6.62
CHEMBL231373 1 6.51
CHEMBL230963 1 6.41
CHEMBL231372 1 6.35
CHEMBL231068 FLIBANSERIN 4.0 1 6.20
CHEMBL230425 1 5.69
CHEMBL231272 1 5.44
CHEMBL230961 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231471 EC50 = 10.0 nM 8.00
CHEMBL45305 BEFIRADOL EC50 = 23.44 nM 7.63
CHEMBL56 8-OH-DPAT EC50 = 32.36 nM 7.49
CHEMBL396062 EC50 = 42.66 nM 7.37
CHEMBL425833 EC50 = 69.18 nM 7.16
CHEMBL394606 EC50 = 85.11 nM 7.07
CHEMBL394778 EC50 = 89.13 nM 7.05
CHEMBL209821 NALUZOTAN EC50 = 93.33 nM 7.03
CHEMBL231273 EC50 = 154.88 nM 6.81
CHEMBL39 SEROTONIN EC50 = 229.09 nM 6.64
CHEMBL394530 EC50 = 229.09 nM 6.64
CHEMBL230327 EC50 = 239.88 nM 6.62
CHEMBL231373 EC50 = 309.03 nM 6.51
CHEMBL230963 EC50 = 389.05 nM 6.41
CHEMBL231372 EC50 = 446.68 nM 6.35
CHEMBL231068 FLIBANSERIN EC50 = 630.96 nM 6.20
CHEMBL230425 EC50 = 2041.74 nM 5.69
CHEMBL231272 EC50 = 3630.78 nM 5.44
CHEMBL230961 EC50 = 7943.28 nM 5.10