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Assay Detail

CHEMBL828842

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

Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.
Dyck B, Grigoriadis DE, Gross RS, Guo Z, Haddach M, Marinkovic D, McCarthy JR, Moorjani M, Regan CF, Saunders J, Schwaebe MK, Szabo T, Williams JP, Zhang X, Bozigian H, Chen TK.
J Med Chem (2005) 48 : 4100 -4110
PubMed 15943483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.61 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363414 1 8.54
CHEMBL296641 ANTALARMIN 1 8.51
CHEMBL195631 1 8.46
CHEMBL364016 1 8.38
CHEMBL195699 1 8.27
CHEMBL427168 1 8.22
CHEMBL195152 1 8.19
CHEMBL371407 1 8.14
CHEMBL309138 1 8.11
CHEMBL370501 1 7.89
CHEMBL194607 1 7.89
CHEMBL372009 1 7.80
CHEMBL191755 1 7.52
CHEMBL191903 1 7.40
CHEMBL371367 1 7.31
CHEMBL192288 1 7.26
CHEMBL192335 1 7.21
CHEMBL192082 1 6.92
CHEMBL434910 1 6.72
CHEMBL191780 1 5.72
CHEMBL191650 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363414 Ki = 2.9 nM 8.54
CHEMBL296641 ANTALARMIN Ki = 3.1 nM 8.51
CHEMBL195631 Ki = 3.5 nM 8.46
CHEMBL364016 Ki = 4.2 nM 8.38
CHEMBL195699 Ki = 5.4 nM 8.27
CHEMBL427168 Ki = 6.0 nM 8.22
CHEMBL195152 Ki = 6.5 nM 8.19
CHEMBL371407 Ki = 7.2 nM 8.14
CHEMBL309138 Ki = 7.8 nM 8.11
CHEMBL370501 Ki = 13.0 nM 7.89
CHEMBL194607 Ki = 13.0 nM 7.89
CHEMBL372009 Ki = 16.0 nM 7.80
CHEMBL191755 Ki = 30.0 nM 7.52
CHEMBL191903 Ki = 40.0 nM 7.40
CHEMBL371367 Ki = 49.0 nM 7.31
CHEMBL192288 Ki = 55.0 nM 7.26
CHEMBL192335 Ki = 62.0 nM 7.21
CHEMBL192082 Ki = 120.0 nM 6.92
CHEMBL434910 Ki = 190.0 nM 6.72
CHEMBL191780 Ki = 1900.0 nM 5.72
CHEMBL191650 Ki = 4100.0 nM 5.39