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Assay Detail

CHEMBL1837869

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Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of potent, metabolically stable purine CRF-1 antagonists with differentiated binding kinetic profiles.
Miller DC, Klute W, Brown AD.
Bioorg Med Chem Lett (2011) 21 : 6108 -6111
PubMed 21889333 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 8.90 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45187 1 9.55
CHEMBL1836947 1 9.54
CHEMBL309138 1 9.52
CHEMBL1836945 1 9.43
CHEMBL1836944 1 8.52
CHEMBL1836932 1 7.92
CHEMBL568606 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45187 Kd = 0.279 nM 9.55
CHEMBL1836947 Kd = 0.291 nM 9.54
CHEMBL309138 Kd = 0.303 nM 9.52
CHEMBL1836945 Kd = 0.373 nM 9.43
CHEMBL1836944 Kd = 3.0 nM 8.52
CHEMBL1836932 Kd = 12.0 nM 7.92
CHEMBL568606 Kd = 14.0 nM 7.85