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Assay Detail

CHEMBL4131851

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

Binding
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of 2-imino and 2-hydrazono thiazolo[4,5-d]pyrimidines as corticotropin releasing factor (CRF) antagonists.
Teleb M, Kuppast B, Spyridaki K, Liapakis G, Fahmy H.
Eur J Med Chem (2017) 138 : 900 -908
PubMed 28750312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.73 7.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296641 ANTALARMIN 1 7.73
CHEMBL4160471 1 6.77
CHEMBL4161963 1 6.35
CHEMBL4170184 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296641 ANTALARMIN IC50 = 18.62 nM 7.73
CHEMBL4160471 IC50 = 169.82 nM 6.77
CHEMBL4161963 IC50 = 446.68 nM 6.35
CHEMBL4170184 IC50 = 891.25 nM 6.05