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Assay Detail

CHEMBL2089417

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Functional
Antagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulation
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type IMR-32
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor.
Takahashi Y, Hibi S, Hoshino Y, Kikuchi K, Shin K, Murata-Tai K, Fujisawa M, Ino M, Shibata H, Yonaga M.
J Med Chem (2012) 55 : 5255 -5269
PubMed 22587443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.02 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL309138 1 8.08
CHEMBL2087549 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL309138 Ki = 8.3 nM 8.08
CHEMBL2087549 Ki = 11.0 nM 7.96