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Assay Detail

CHEMBL827940

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

Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists.
Huang CQ, Wilcoxen KM, Grigoriadis DE, McCarthy JR, Chen C.
Bioorg Med Chem Lett (2004) 14 : 3943 -3947
PubMed 15225703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.17 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333713 1 7.80
CHEMBL184930 1 7.31
CHEMBL184850 1 6.82
CHEMBL183148 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333713 IC50 = 16.0 nM 7.80
CHEMBL184930 IC50 = 49.0 nM 7.31
CHEMBL184850 IC50 = 150.0 nM 6.82
CHEMBL183148 IC50 = 180.0 nM 6.75