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Assay Detail

CHEMBL3777826

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

Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in mouse CRF-R2 beta expressed in COS-M6 cells after 90 mins by gamma counting assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type COS-M6
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Corticotropin-releasing factor receptor 2 (CHEMBL2253)
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
Ki 7 9.29 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3774395 1 9.59
CHEMBL3774465 1 9.54
CHEMBL3774742 1 9.49
CHEMBL3775796 1 9.44
CHEMBL4299355 1 9.02
CHEMBL4299313 1 8.97
CHEMBL4299340 1 8.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3774395 Ki = 0.26 nM 9.59
CHEMBL3774465 Ki = 0.29 nM 9.54
CHEMBL3774742 Ki = 0.32 nM 9.49
CHEMBL3775796 Ki = 0.36 nM 9.44
CHEMBL4299355 Ki = 0.95 nM 9.02
CHEMBL4299313 Ki = 1.07 nM 8.97
CHEMBL4299340 Ki = 1.07 nM 8.97