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Assay Detail

CHEMBL895213

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to 5HT1A receptor in rat cortex membrane
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cortex
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Ki 25 8.21 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231471 1 9.37
CHEMBL425833 1 9.16
CHEMBL396062 1 9.13
CHEMBL45305 BEFIRADOL 2.0 1 9.07
CHEMBL394530 1 8.92
CHEMBL56 8-OH-DPAT 1 8.85
CHEMBL394606 1 8.76
CHEMBL39 SEROTONIN 3.0 1 8.73
CHEMBL230963 1 8.65
CHEMBL394778 1 8.64
CHEMBL231273 1 8.47
CHEMBL230327 1 8.42
CHEMBL231373 1 8.32
CHEMBL230961 1 8.25
CHEMBL231372 1 8.19
CHEMBL230425 1 8.13
CHEMBL231068 FLIBANSERIN 4.0 1 7.93
CHEMBL231272 1 7.60
CHEMBL209821 NALUZOTAN 3.0 1 7.52
CHEMBL231271 1 7.25
CHEMBL230962 1 7.18
CHEMBL231069 1 7.02
CHEMBL231172 1 6.93
CHEMBL231170 1 6.66
CHEMBL231262 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231471 Ki = 0.4266 nM 9.37
CHEMBL425833 Ki = 0.6918 nM 9.16
CHEMBL396062 Ki = 0.7413 nM 9.13
CHEMBL45305 BEFIRADOL Ki = 0.8511 nM 9.07
CHEMBL394530 Ki = 1.202 nM 8.92
CHEMBL56 8-OH-DPAT Ki = 1.413 nM 8.85
CHEMBL394606 Ki = 1.738 nM 8.76
CHEMBL39 SEROTONIN Ki = 1.862 nM 8.73
CHEMBL230963 Ki = 2.239 nM 8.65
CHEMBL394778 Ki = 2.291 nM 8.64
CHEMBL231273 Ki = 3.388 nM 8.47
CHEMBL230327 Ki = 3.802 nM 8.42
CHEMBL231373 Ki = 4.786 nM 8.32
CHEMBL230961 Ki = 5.623 nM 8.25
CHEMBL231372 Ki = 6.457 nM 8.19
CHEMBL230425 Ki = 7.413 nM 8.13
CHEMBL231068 FLIBANSERIN Ki = 11.75 nM 7.93
CHEMBL231272 Ki = 25.12 nM 7.60
CHEMBL209821 NALUZOTAN Ki = 30.2 nM 7.52
CHEMBL231271 Ki = 56.23 nM 7.25
CHEMBL230962 Ki = 66.07 nM 7.18
CHEMBL231069 Ki = 95.5 nM 7.02
CHEMBL231172 Ki = 117.49 nM 6.93
CHEMBL231170 Ki = 218.78 nM 6.66
CHEMBL231262 Ki > 10000.0 nM -