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Assay Detail

CHEMBL1936043

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

Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Lead diversification. Application to existing drug molecules: mifepristone 1 and antalarmin 8.
Abid Masood M, Farrant E, Morao I, Bazin M, Perez M, Bunnage ME, Fancy SA, Peakman T.
Bioorg Med Chem Lett (2012) 22 : 723 -728
PubMed 22104142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.74 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1934749 1 8.22
CHEMBL1934751 1 7.96
CHEMBL296641 ANTALARMIN 1 7.50
CHEMBL1934750 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1934749 Ki = 6.0 nM 8.22
CHEMBL1934751 Ki = 11.0 nM 7.96
CHEMBL296641 ANTALARMIN Ki = 32.0 nM 7.50
CHEMBL1934750 Ki = 52.0 nM 7.28