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Assay Detail

CHEMBL663519

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

Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
19
Total Activities
18
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 (CHEMBL1800)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacophore development for corticotropin-releasing hormone: new insights into inhibitor activity.
Keller PA, Bowman M, Dang KH, Garner J, Leach SP, Smith R, McCluskey A.
J Med Chem (1999) 42 : 2351 -2357
PubMed 10395475 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.80 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45281 1 8.77
CHEMBL306482 1 8.64
CHEMBL75859 1 8.60
CHEMBL77716 1 8.42
CHEMBL77006 2 7.52
CHEMBL306618 1 7.24
CHEMBL77391 1 6.94
CHEMBL308544 1 6.89
CHEMBL307419 1 6.31
CHEMBL419636 1 6.31
CHEMBL78035 1 5.98
CHEMBL305671 1 5.98
CHEMBL80806 1 5.86
CHEMBL307871 1 5.83
CHEMBL78271 1 5.77
CHEMBL77527 1 5.68
CHEMBL309789 1 5.10
CHEMBL78203 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45281 Ki = 1.7 nM 8.77
CHEMBL306482 Ki = 2.3 nM 8.64
CHEMBL75859 Ki = 2.5 nM 8.60
CHEMBL77716 Ki = 3.8 nM 8.42
CHEMBL77006 Ki = 30.0 nM 7.52
CHEMBL306618 Ki = 57.0 nM 7.24
CHEMBL77391 Ki = 115.0 nM 6.94
CHEMBL308544 Ki = 130.0 nM 6.89
CHEMBL77006 Ki = 253.0 nM 6.60
CHEMBL419636 Ki = 490.0 nM 6.31
CHEMBL307419 Ki = 490.0 nM 6.31
CHEMBL78035 Ki = 1050.0 nM 5.98
CHEMBL305671 Ki = 1050.0 nM 5.98
CHEMBL80806 Ki = 1390.0 nM 5.86
CHEMBL307871 Ki = 1470.0 nM 5.83
CHEMBL78271 Ki = 1690.0 nM 5.77
CHEMBL77527 Ki = 2100.0 nM 5.68
CHEMBL309789 Ki = 8000.0 nM 5.10
CHEMBL78203 Ki > 10000.0 nM -