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Assay Detail

CHEMBL664192

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

Binding
Binding affinity was determined against corticotropin releasing factor receptor 1
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Corticotropin-releasing factor receptor 1 (CHEMBL4649)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Corticotropin-releasing hormone receptor antagonists: framework design and synthesis guided by ligand conformational studies.
Hodge CN, Aldrich PE, Wasserman ZR, Fernandez CH, Nemeth GA, Arvanitis A, Cheeseman RS, Chorvat RJ, Ciganek E, Christos TE, Gilligan PJ, Krenitsky P, Scholfield E, Strucely P.
J Med Chem (1999) 42 : 819 -832
PubMed 10072680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.14 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL167241 1 9.00
CHEMBL46479 1 8.30
CHEMBL432496 1 7.66
CHEMBL46798 1 7.55
CHEMBL169838 1 7.54
CHEMBL353916 1 7.47
CHEMBL169359 1 7.44
CHEMBL166162 1 7.42
CHEMBL43216 1 7.37
CHEMBL167264 1 7.34
CHEMBL169784 1 7.33
CHEMBL355624 1 7.32
CHEMBL353774 1 7.17
CHEMBL355882 1 7.10
CHEMBL168568 1 7.02
CHEMBL166760 1 6.95
CHEMBL170487 1 6.65
CHEMBL168590 1 6.44
CHEMBL166946 1 6.35
CHEMBL166732 1 6.14
CHEMBL354092 1 5.89
CHEMBL415752 1 5.61
CHEMBL166945 1 -
CHEMBL169004 1 -
CHEMBL355136 1 -
CHEMBL355135 1 -
CHEMBL168591 1 -
CHEMBL165818 1 -
CHEMBL168784 1 -
CHEMBL355218 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL167241 Ki = 1.0 nM 9.00
CHEMBL46479 Ki = 5.0 nM 8.30
CHEMBL432496 Ki = 22.0 nM 7.66
CHEMBL46798 Ki = 28.0 nM 7.55
CHEMBL169838 Ki = 29.0 nM 7.54
CHEMBL353916 Ki = 34.0 nM 7.47
CHEMBL169359 Ki = 36.0 nM 7.44
CHEMBL166162 Ki = 38.0 nM 7.42
CHEMBL43216 Ki = 43.0 nM 7.37
CHEMBL167264 Ki = 46.0 nM 7.34
CHEMBL169784 Ki = 47.0 nM 7.33
CHEMBL355624 Ki = 48.0 nM 7.32
CHEMBL353774 Ki = 67.0 nM 7.17
CHEMBL355882 Ki = 79.0 nM 7.10
CHEMBL168568 Ki = 96.0 nM 7.02
CHEMBL166760 Ki = 112.0 nM 6.95
CHEMBL170487 Ki = 222.0 nM 6.65
CHEMBL168590 Ki = 363.0 nM 6.44
CHEMBL166946 Ki = 446.0 nM 6.35
CHEMBL166732 Ki = 722.0 nM 6.14
CHEMBL354092 Ki = 1277.0 nM 5.89
CHEMBL415752 Ki = 2462.0 nM 5.61
CHEMBL166945 Ki > 10000.0 nM -
CHEMBL169004 Ki > 100000.0 nM -
CHEMBL355136 Ki > 10000.0 nM -
CHEMBL355135 Ki > 10000.0 nM -
CHEMBL168591 Ki - -
CHEMBL165818 Ki > 10000.0 nM -
CHEMBL168784 Ki > 10000.0 nM -
CHEMBL355218 Ki > 10000.0 nM -
CHEMBL170055 Ki > 10000.0 nM -
CHEMBL169507 Ki > 100000.0 nM -
CHEMBL355289 Ki > 1000.0 nM -