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Assay Detail

CHEMBL998751

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

Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
29
Total Activities
29
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

2-Arylpyrimidines: novel CRF-1 receptor antagonists.
Yoon T, De Lombaert S, Brodbeck R, Gulianello M, Krause JE, Hutchison A, Horvath RF, Ge P, Kehne J, Hoffman D, Chandrasekhar J, Doller D, Hodgetts KJ.
Bioorg Med Chem Lett (2008) 18 : 4486 -4490
PubMed 18672365 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.57 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL498311 1 9.70
CHEMBL1628268 1 8.70
CHEMBL524616 1 8.70
CHEMBL525716 1 8.70
CHEMBL9946 CP-154526 1 8.52
CHEMBL309138 1 8.52
CHEMBL497651 1 8.22
CHEMBL438888 1 8.22
CHEMBL497652 1 8.10
CHEMBL498667 1 8.05
CHEMBL497653 1 8.05
CHEMBL497301 1 7.82
CHEMBL498318 1 7.80
CHEMBL524617 1 7.66
CHEMBL498319 1 7.48
CHEMBL527030 1 7.28
CHEMBL497287 1 7.12
CHEMBL451660 1 7.03
CHEMBL510224 1 6.56
CHEMBL526829 1 6.45
CHEMBL526828 1 6.29
CHEMBL498480 1 6.25
CHEMBL523074 1 6.22
CHEMBL496269 1 5.94
CHEMBL497286 1 5.79
CHEMBL497283 1 -
CHEMBL496270 1 -
CHEMBL497465 1 -
CHEMBL497466 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL498311 Ki = 0.2 nM 9.70
CHEMBL1628268 Ki = 2.0 nM 8.70
CHEMBL524616 Ki = 2.0 nM 8.70
CHEMBL525716 Ki = 2.0 nM 8.70
CHEMBL9946 CP-154526 Ki = 3.0 nM 8.52
CHEMBL309138 Ki = 3.0 nM 8.52
CHEMBL497651 Ki = 6.0 nM 8.22
CHEMBL438888 Ki = 6.0 nM 8.22
CHEMBL497652 Ki = 8.0 nM 8.10
CHEMBL498667 Ki = 9.0 nM 8.05
CHEMBL497653 Ki = 9.0 nM 8.05
CHEMBL497301 Ki = 15.0 nM 7.82
CHEMBL498318 Ki = 16.0 nM 7.80
CHEMBL524617 Ki = 22.0 nM 7.66
CHEMBL498319 Ki = 33.0 nM 7.48
CHEMBL527030 Ki = 53.0 nM 7.28
CHEMBL497287 Ki = 76.0 nM 7.12
CHEMBL451660 Ki = 94.0 nM 7.03
CHEMBL510224 Ki = 277.0 nM 6.56
CHEMBL526829 Ki = 354.0 nM 6.45
CHEMBL526828 Ki = 507.0 nM 6.29
CHEMBL498480 Ki = 561.0 nM 6.25
CHEMBL523074 Ki = 604.0 nM 6.22
CHEMBL496269 Ki = 1150.0 nM 5.94
CHEMBL497286 Ki = 1610.0 nM 5.79
CHEMBL497283 Ki > 5000.0 nM -
CHEMBL496270 Ki > 10000.0 nM -
CHEMBL497465 Ki > 10000.0 nM -
CHEMBL497466 Ki > 10000.0 nM -