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Assay Detail

CHEMBL3777825

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

Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

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 10 9.13 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3775796 1 9.74
CHEMBL3774395 1 9.55
CHEMBL4299340 1 9.46
CHEMBL4299286 1 9.34
CHEMBL4299295 1 9.32
CHEMBL3775761 1 9.28
CHEMBL3775192 1 9.23
CHEMBL3774713 1 8.66
CHEMBL4299313 1 8.46
CHEMBL4299287 1 8.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3775796 Ki = 0.18 nM 9.74
CHEMBL3774395 Ki = 0.28 nM 9.55
CHEMBL4299340 Ki = 0.35 nM 9.46
CHEMBL4299286 Ki = 0.46 nM 9.34
CHEMBL4299295 Ki = 0.48 nM 9.32
CHEMBL3775761 Ki = 0.52 nM 9.28
CHEMBL3775192 Ki = 0.59 nM 9.23
CHEMBL3774713 Ki = 2.17 nM 8.66
CHEMBL4299313 Ki = 3.5 nM 8.46
CHEMBL4299287 Ki = 5.94 nM 8.23