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Assay Detail

CHEMBL994498

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

Functional
Antagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH production
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Pituitary gland cell
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Corticotropin-releasing factor receptor 1 (CHEMBL4649)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
Gilligan PJ, Clarke T, He L, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A, Krause C, McElroy JF, Ward K, Zeller K, Wong H, Bai S, Saye J, Grossman S, Zaczek R, Arneric SP, Hartig P, Robertson D, Trainor G.
J Med Chem (2009) 52 : 3084 -3092
PubMed 19361209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.89 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL482950 PEXACERFONT 3.0 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL482950 PEXACERFONT IC50 = 129.0 nM 6.89