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Assay Detail

CHEMBL3241202

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

Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
9
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
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 substituted pyrimidines as corticotropin releasing factor (CRF) receptor ligands.
Kuppast B, Spyridaki K, Liapakis G, Fahmy H.
Eur J Med Chem (2014) 78 : 1 -9
PubMed 24675175 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.68 7.73
Inhibition 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296641 ANTALARMIN 1 7.73
CHEMBL3235706 2 6.61
CHEMBL3235700 2 6.56
CHEMBL3235703 2 6.27
CHEMBL3235705 2 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296641 ANTALARMIN IC50 = 18.62 nM 7.73
CHEMBL3235706 IC50 = 245.47 nM 6.61
CHEMBL3235700 IC50 = 275.42 nM 6.56
CHEMBL3235703 IC50 = 537.03 nM 6.27
CHEMBL3235705 IC50 = 588.84 nM 6.23
CHEMBL3235700 Inhibition - % -
CHEMBL3235703 Inhibition - % -
CHEMBL3235705 Inhibition - % -
CHEMBL3235706 Inhibition - % -