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Assay Detail

CHEMBL1004666

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

Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
22
Total Activities
22
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

Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists.
Di Fabio R, St-Denis Y, Sabbatini FM, Andreotti D, Arban R, Bernasconi G, Braggio S, Blaney FE, Capelli AM, Castiglioni E, Di Modugno E, Donati D, Fazzolari E, Ratti E, Feriani A, Contini S, Gentile G, Ghirlanda D, Provera S, Marchioro C, Roberts KL, Mingardi A, Mattioli M, Nalin A, Pavone F, Spada S, Trist DG, Worby A.
J Med Chem (2008) 51 : 7370 -7379
PubMed 18989952 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.77 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL309138 1 7.55
CHEMBL458810 1 7.49
CHEMBL44698 1 7.40
CHEMBL456660 1 7.30
CHEMBL459173 1 7.25
CHEMBL514270 EMICERFONT 2.0 1 7.18
CHEMBL516170 1 7.17
CHEMBL456640 1 7.17
CHEMBL464185 1 7.05
CHEMBL515363 1 6.92
CHEMBL513937 1 6.92
CHEMBL458599 1 6.91
CHEMBL456448 1 6.84
CHEMBL464184 1 6.80
CHEMBL456449 1 6.51
CHEMBL457710 1 6.50
CHEMBL457742 1 6.44
CHEMBL458626 1 6.43
CHEMBL515532 1 6.10
CHEMBL457975 1 5.91
CHEMBL458600 1 5.71
CHEMBL515503 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL309138 IC50 = 28.18 nM 7.55
CHEMBL458810 IC50 = 32.36 nM 7.49
CHEMBL44698 IC50 = 39.81 nM 7.40
CHEMBL456660 IC50 = 50.12 nM 7.30
CHEMBL459173 IC50 = 56.23 nM 7.25
CHEMBL514270 EMICERFONT IC50 = 66.07 nM 7.18
CHEMBL516170 IC50 = 67.61 nM 7.17
CHEMBL456640 IC50 = 67.61 nM 7.17
CHEMBL464185 IC50 = 89.13 nM 7.05
CHEMBL515363 IC50 = 120.23 nM 6.92
CHEMBL513937 IC50 = 120.23 nM 6.92
CHEMBL458599 IC50 = 123.03 nM 6.91
CHEMBL456448 IC50 = 144.54 nM 6.84
CHEMBL464184 IC50 = 158.49 nM 6.80
CHEMBL456449 IC50 = 309.03 nM 6.51
CHEMBL457710 IC50 = 316.23 nM 6.50
CHEMBL457742 IC50 = 363.08 nM 6.44
CHEMBL458626 IC50 = 371.54 nM 6.43
CHEMBL515532 IC50 = 794.33 nM 6.10
CHEMBL457975 IC50 = 1230.27 nM 5.91
CHEMBL458600 IC50 = 1949.84 nM 5.71
CHEMBL515503 IC50 = 3235.94 nM 5.49