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Assay Detail

CHEMBL3778915

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

Functional
Antagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type AtT20
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Corticotropin-releasing factor receptor 1 (CHEMBL2446)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Characterization of Multisubstituted Corticotropin Releasing Factor (CRF) Peptide Antagonists (Astressins).
Erchegyi J, Wang L, Gulyas J, Samant M, Perrin MH, Lewis K, Miller C, Vaughan J, Donaldson C, Fischer W, Low W, Yakabi S, Karasawa H, Taché Y, Rivier C, Rivier J.
J Med Chem (2016) 59 : 854 -866
PubMed 26789203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 9.27 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3775924 1 9.38
CHEMBL3774395 1 9.36
CHEMBL4299295 1 9.35
CHEMBL3774939 1 9.15
CHEMBL3775796 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3775924 EC50 = 0.42 nM 9.38
CHEMBL3774395 EC50 = 0.44 nM 9.36
CHEMBL4299295 EC50 = 0.45 nM 9.35
CHEMBL3774939 EC50 = 0.7 nM 9.15
CHEMBL3775796 EC50 = 0.8 nM 9.10