Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL663520

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

Functional
Antagonistic activity for Corticotropin releasing factor receptor 1
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Corticotropin-releasing factor receptor 1 (CHEMBL1800)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Use of the Suzuki reaction for the synthesis of aryl-substituted heterocycles as corticotropin-releasing hormone (CRH) antagonists.
Cocuzza AJ, Chidester DR, Culp S, Fitzgerald L, Gilligan P.
Bioorg Med Chem Lett (1999) 9 : 1063 -1066
PubMed 10230641 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.75 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10154 1 8.70
CHEMBL9946 CP-154526 1 8.57
CHEMBL9633 1 8.46
CHEMBL10504 1 8.43
CHEMBL10082 1 8.26
CHEMBL273839 1 8.01
CHEMBL276263 1 7.67
CHEMBL10080 1 7.64
CHEMBL10142 1 7.49
CHEMBL10174 1 7.48
CHEMBL10091 1 7.22
CHEMBL10090 1 7.02
CHEMBL10315 1 6.78
CHEMBL10279 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10154 Ki = 2.0 nM 8.70
CHEMBL9946 CP-154526 Ki = 2.7 nM 8.57
CHEMBL9633 Ki = 3.5 nM 8.46
CHEMBL10504 Ki = 3.7 nM 8.43
CHEMBL10082 Ki = 5.5 nM 8.26
CHEMBL273839 Ki = 9.7 nM 8.01
CHEMBL276263 Ki = 21.4 nM 7.67
CHEMBL10080 Ki = 23.1 nM 7.64
CHEMBL10142 Ki = 32.3 nM 7.49
CHEMBL10174 Ki = 33.4 nM 7.48
CHEMBL10091 Ki = 60.3 nM 7.22
CHEMBL10090 Ki = 95.5 nM 7.02
CHEMBL10315 Ki = 168.0 nM 6.78
CHEMBL10279 Ki = 202.0 nM 6.70