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Assay Detail

CHEMBL998752

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

Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type AtT20
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

2-Arylpyrimidines: novel CRF-1 receptor antagonists.
Yoon T, De Lombaert S, Brodbeck R, Gulianello M, Krause JE, Hutchison A, Horvath RF, Ge P, Kehne J, Hoffman D, Chandrasekhar J, Doller D, Hodgetts KJ.
Bioorg Med Chem Lett (2008) 18 : 4486 -4490
PubMed 18672365 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.20 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL525716 1 9.00
CHEMBL497653 1 8.15
CHEMBL438888 1 7.92
CHEMBL497652 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL525716 IC50 = 1.0 nM 9.00
CHEMBL497653 IC50 = 7.0 nM 8.15
CHEMBL438888 IC50 = 12.0 nM 7.92
CHEMBL497652 IC50 = 19.0 nM 7.72