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Assay Detail

CHEMBL949477

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 by SPA
44
Total Activities
44
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

Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: mapping of the receptor binding pocket by in silico docking studies.
Di Fabio R, Arban R, Bernasconi G, Braggio S, Blaney FE, Capelli AM, Castiglioni E, Donati D, Fazzolari E, Ratti E, Feriani A, Contini S, Gentile G, Ghirlanda D, Sabbatini FM, Andreotti D, Spada S, Marchioro C, Worby A, St-Denis Y.
J Med Chem (2008) 51 : 7273 -7286
PubMed 18975927 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 6.55 7.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL458968 1 7.56
CHEMBL516175 1 7.46
CHEMBL515843 1 7.40
CHEMBL44698 1 7.40
CHEMBL458825 1 7.27
CHEMBL462789 1 7.25
CHEMBL457714 1 7.23
CHEMBL504383 1 7.22
CHEMBL458824 1 7.06
CHEMBL459006 1 7.03
CHEMBL513967 1 7.00
CHEMBL514761 1 6.94
CHEMBL459007 1 6.90
CHEMBL458826 1 6.89
CHEMBL464390 1 6.84
CHEMBL462788 1 6.80
CHEMBL459174 1 6.79
CHEMBL465216 1 6.76
CHEMBL456651 1 6.67
CHEMBL457741 1 6.65
CHEMBL517910 1 6.64
CHEMBL514126 1 6.59
CHEMBL458101 1 6.59
CHEMBL459181 1 6.50
CHEMBL457740 1 6.44
CHEMBL458353 1 6.37
CHEMBL456241 1 6.07
CHEMBL458981 1 5.69
CHEMBL515070 1 5.63
CHEMBL514272 1 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL458968 IC50 = 27.54 nM 7.56
CHEMBL516175 IC50 = 34.67 nM 7.46
CHEMBL44698 IC50 = 39.81 nM 7.40
CHEMBL515843 IC50 = 39.81 nM 7.40
CHEMBL458825 IC50 = 53.7 nM 7.27
CHEMBL462789 IC50 = 56.23 nM 7.25
CHEMBL457714 IC50 = 58.88 nM 7.23
CHEMBL504383 IC50 = 60.26 nM 7.22
CHEMBL458824 IC50 = 87.1 nM 7.06
CHEMBL459006 IC50 = 93.33 nM 7.03
CHEMBL513967 IC50 = 100.0 nM 7.00
CHEMBL514761 IC50 = 114.82 nM 6.94
CHEMBL459007 IC50 = 125.89 nM 6.90
CHEMBL458826 IC50 = 128.82 nM 6.89
CHEMBL464390 IC50 = 144.54 nM 6.84
CHEMBL462788 IC50 = 158.49 nM 6.80
CHEMBL459174 IC50 = 162.18 nM 6.79
CHEMBL465216 IC50 = 173.78 nM 6.76
CHEMBL456651 IC50 = 213.8 nM 6.67
CHEMBL457741 IC50 = 223.87 nM 6.65
CHEMBL517910 IC50 = 229.09 nM 6.64
CHEMBL458101 IC50 = 257.04 nM 6.59
CHEMBL514126 IC50 = 257.04 nM 6.59
CHEMBL459181 IC50 = 316.23 nM 6.50
CHEMBL457740 IC50 = 363.08 nM 6.44
CHEMBL458353 IC50 = 426.58 nM 6.37
CHEMBL456241 IC50 = 851.14 nM 6.07
CHEMBL458981 IC50 = 2041.74 nM 5.69
CHEMBL515070 IC50 = 2344.23 nM 5.63
CHEMBL514272 IC50 = 2754.23 nM 5.56
CHEMBL458115 IC50 = 3467.37 nM 5.46
CHEMBL457708 IC50 = 3890.45 nM 5.41
CHEMBL458177 IC50 = 7413.1 nM 5.13
CHEMBL458780 IC50 = 8317.64 nM 5.08
CHEMBL458980 IC50 = 8709.64 nM 5.06
CHEMBL458169 IC50 > 10000.0 nM -
CHEMBL514717 IC50 > 10000.0 nM -
CHEMBL458598 IC50 > 10000.0 nM -
CHEMBL488592 IC50 > 10000.0 nM -
CHEMBL457707 IC50 > 10000.0 nM -
CHEMBL515055 IC50 > 10000.0 nM -
CHEMBL457522 IC50 > 10000.0 nM -
CHEMBL457503 IC50 > 10000.0 nM -
CHEMBL458839 IC50 > 10000.0 nM -