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Assay Detail

CHEMBL985701

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Binding
Binding affinity to CRF1 receptor in human IMR32 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type IMR-32
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists.
Gilligan PJ, He L, Clarke T, Tivitmahaisoon P, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A, Krause C, McElroy J, Ward K, Shen H, Wong H, Grossman S, Nemeth G, Zaczek R, Arneric SP, Hartig P, Robertson DW, Trainor G.
J Med Chem (2009) 52 : 3073 -3083
PubMed 19361210 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.45 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484158 1 8.92
CHEMBL526149 1 8.70
CHEMBL506214 1 8.47
CHEMBL475306 1 8.33
CHEMBL483993 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484158 IC50 = 1.2 nM 8.92
CHEMBL526149 IC50 = 2.0 nM 8.70
CHEMBL506214 IC50 = 3.4 nM 8.47
CHEMBL475306 IC50 = 4.7 nM 8.33
CHEMBL483993 IC50 = 15.2 nM 7.82