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Assay Detail

CHEMBL1109765

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

Binding
Binding affinity to OX1 receptor by radioligand displacement assay
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Orexin/Hypocretin receptor type 1 (CHEMBL5113)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.
Coleman PJ, Schreier JD, McGaughey GB, Bogusky MJ, Cox CD, Hartman GD, Ball RG, Harrell CM, Reiss DR, Prueksaritanont T, Winrow CJ, Renger JJ.
Bioorg Med Chem Lett (2010) 20 : 2311 -2315
PubMed 20207138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.98 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093725 1 9.40
CHEMBL1091110 3 9.15
CHEMBL1089406 1 9.00
CHEMBL469146 1 8.92
CHEMBL1091111 1 7.92
CHEMBL1091112 1 6.06
CHEMBL1093724 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093725 Ki = 0.4 nM 9.40
CHEMBL1091110 Ki = 0.7 nM 9.15
CHEMBL1089406 Ki = 1.0 nM 9.00
CHEMBL469146 Ki = 1.2 nM 8.92
CHEMBL1091110 Ki = 2.3 nM 8.64
CHEMBL1091111 Ki = 12.0 nM 7.92
CHEMBL1091110 Ki = 110.0 nM 6.96
CHEMBL1091112 Ki = 870.0 nM 6.06
CHEMBL1093724 Ki = 1700.0 nM 5.77