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Assay Detail

CHEMBL664960

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Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL ↗
113
Total Activities
110
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type 293-EBNA
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis, corticotropin-releasing factor receptor binding affinity, and pharmacokinetic properties of triazolo-, imidazo-, and pyrrolopyrimidines and -pyridines.
Chorvat RJ, Bakthavatchalam R, Beck JP, Gilligan PJ, Wilde RG, Cocuzza AJ, Hobbs FW, Cheeseman RS, Curry M, Rescinito JP, Krenitsky P, Chidester D, Yarem JA, Klaczkiewicz JD, Hodge CN, Aldrich PE, Wasserman ZR, Fernandez CH, Zaczek R, Fitzgerald LW, Huang SM, Shen HL, Wong YN, Chien BM, Arvanitis A.
J Med Chem (1999) 42 : 833 -848
PubMed 10072681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 113 7.73 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL354886 — — 1 9.10
CHEMBL296641 ANTALARMIN — 1 9.08
CHEMBL168554 — — 1 9.05
CHEMBL354982 — — 1 8.85
CHEMBL355214 — — 1 8.82
CHEMBL9946 CP-154526 — 1 8.79
CHEMBL168936 — — 1 8.72
CHEMBL169248 — — 1 8.72
CHEMBL169010 — — 1 8.66
CHEMBL166669 — — 1 8.55
CHEMBL167017 — — 1 8.54
CHEMBL9633 — — 1 8.52
CHEMBL169952 — — 1 8.51
CHEMBL171202 — — 2 8.49
CHEMBL423444 — — 1 8.46
CHEMBL354940 — — 1 8.46
CHEMBL435468 — — 1 8.46
CHEMBL169430 — — 1 8.44
CHEMBL10504 — — 1 8.43
CHEMBL355049 — — 1 8.41
CHEMBL355689 — — 1 8.40
CHEMBL352340 — — 1 8.37
CHEMBL353732 — — 1 8.37
CHEMBL367110 — — 1 8.36
CHEMBL168676 — — 1 8.36
CHEMBL169781 — — 1 8.35
CHEMBL355329 — — 1 8.34
CHEMBL169561 — — 1 8.33
CHEMBL352353 — — 1 8.33
CHEMBL168449 — — 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL354886 — Ki = 0.8 nM 9.10
CHEMBL296641 ANTALARMIN Ki = 0.84 nM 9.08
CHEMBL168554 — Ki = 0.9 nM 9.05
CHEMBL354982 — Ki = 1.4 nM 8.85
CHEMBL355214 — Ki = 1.5 nM 8.82
CHEMBL9946 CP-154526 Ki = 1.61 nM 8.79
CHEMBL168936 — Ki = 1.9 nM 8.72
CHEMBL169248 — Ki = 1.9 nM 8.72
CHEMBL169010 — Ki = 2.2 nM 8.66
CHEMBL166669 — Ki = 2.8 nM 8.55
CHEMBL167017 — Ki = 2.9 nM 8.54
CHEMBL9633 — Ki = 3.0 nM 8.52
CHEMBL169952 — Ki = 3.1 nM 8.51
CHEMBL171202 — Ki = 3.2 nM 8.49
CHEMBL435468 — Ki = 3.5 nM 8.46
CHEMBL423444 — Ki = 3.5 nM 8.46
CHEMBL354940 — Ki = 3.5 nM 8.46
CHEMBL169430 — Ki = 3.6 nM 8.44
CHEMBL10504 — Ki = 3.7 nM 8.43
CHEMBL355049 — Ki = 3.9 nM 8.41
CHEMBL355689 — Ki = 4.0 nM 8.40
CHEMBL353732 — Ki = 4.3 nM 8.37
CHEMBL352340 — Ki = 4.3 nM 8.37
CHEMBL168676 — Ki = 4.4 nM 8.36
CHEMBL367110 — Ki = 4.4 nM 8.36
CHEMBL169781 — Ki = 4.5 nM 8.35
CHEMBL355329 — Ki = 4.6 nM 8.34
CHEMBL352353 — Ki = 4.7 nM 8.33
CHEMBL169561 — Ki = 4.7 nM 8.33
CHEMBL168449 — Ki = 5.0 nM 8.30
CHEMBL172684 — Ki = 5.1 nM 8.29
CHEMBL355721 — Ki = 5.2 nM 8.28
CHEMBL169577 — Ki = 5.2 nM 8.28
CHEMBL168664 — Ki = 5.7 nM 8.24
CHEMBL167777 — Ki = 5.9 nM 8.23
CHEMBL169416 — Ki = 6.1 nM 8.21
CHEMBL168823 — Ki = 6.1 nM 8.21
CHEMBL168476 — Ki = 6.7 nM 8.17
CHEMBL169280 — Ki = 7.1 nM 8.15
CHEMBL165478 — Ki = 7.1 nM 8.15
CHEMBL169083 — Ki = 7.1 nM 8.15
CHEMBL169955 — Ki = 7.4 nM 8.13
CHEMBL169416 — Ki = 7.5 nM 8.12
CHEMBL169979 — Ki = 7.6 nM 8.12
CHEMBL424539 — Ki = 7.5 nM 8.12
CHEMBL353891 — Ki = 8.0 nM 8.10
CHEMBL352438 — Ki = 9.2 nM 8.04
CHEMBL169416 — Ki = 9.4 nM 8.03
CHEMBL170788 — Ki = 9.7 nM 8.01
CHEMBL169641 — Ki = 9.8 nM 8.01