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Assay Detail

CHEMBL3778916

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

Functional
Antagonist activity at CRF-R2 beta in rat A7r5 cells assessed as inhibition of rat Ucn1 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 Rattus norvegicus
Cell Type A7R5
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Corticotropin-releasing factor receptor 2 (CHEMBL3581)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 9.07 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4299295 1 9.20
CHEMBL3774395 1 9.11
CHEMBL3774939 1 9.04
CHEMBL3775796 1 9.00
CHEMBL3775217 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4299295 EC50 = 0.63 nM 9.20
CHEMBL3774395 EC50 = 0.77 nM 9.11
CHEMBL3774939 EC50 = 0.91 nM 9.04
CHEMBL3775796 EC50 = 1.0 nM 9.00
CHEMBL3775217 EC50 = 1.0 nM 9.00