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Assay Detail

CHEMBL3707672

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

Binding
Radioligand Binding Assay: Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Orexin receptor type 2 (CHEMBL1275216)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Pyridyl piperidine orexin receptor antagonists
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 8.82 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3655673 1 10.10
CHEMBL3235249 1 9.62
CHEMBL3655670 1 9.62
CHEMBL2107822 FILOREXANT 2.0 1 9.51
CHEMBL3655674 1 9.46
CHEMBL3655671 1 9.43
CHEMBL3655676 1 9.32
CHEMBL3655672 1 9.30
CHEMBL3655675 1 9.28
CHEMBL3655664 1 9.27
CHEMBL3655679 1 9.17
CHEMBL3655680 1 9.17
CHEMBL3655665 1 9.17
CHEMBL3655681 1 8.82
CHEMBL3655667 1 8.77
CHEMBL3655677 1 8.77
CHEMBL3655682 1 8.72
CHEMBL3655669 1 8.70
CHEMBL3655683 1 8.42
CHEMBL3655678 1 8.00
CHEMBL3655684 1 7.66
CHEMBL3655663 1 7.54
CHEMBL3655668 1 7.43
CHEMBL3655666 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3655673 Ki = 0.08 nM 10.10
CHEMBL3235249 Ki = 0.24 nM 9.62
CHEMBL3655670 Ki = 0.24 nM 9.62
CHEMBL2107822 FILOREXANT Ki = 0.31 nM 9.51
CHEMBL3655674 Ki = 0.35 nM 9.46
CHEMBL3655671 Ki = 0.37 nM 9.43
CHEMBL3655676 Ki = 0.48 nM 9.32
CHEMBL3655672 Ki = 0.5 nM 9.30
CHEMBL3655675 Ki = 0.53 nM 9.28
CHEMBL3655664 Ki = 0.54 nM 9.27
CHEMBL3655679 Ki = 0.67 nM 9.17
CHEMBL3655680 Ki = 0.68 nM 9.17
CHEMBL3655665 Ki = 0.67 nM 9.17
CHEMBL3655681 Ki = 1.5 nM 8.82
CHEMBL3655667 Ki = 1.7 nM 8.77
CHEMBL3655677 Ki = 1.7 nM 8.77
CHEMBL3655682 Ki = 1.9 nM 8.72
CHEMBL3655669 Ki = 2.0 nM 8.70
CHEMBL3655683 Ki = 3.8 nM 8.42
CHEMBL3655678 Ki = 10.0 nM 8.00
CHEMBL3655684 Ki = 22.0 nM 7.66
CHEMBL3655663 Ki = 29.0 nM 7.54
CHEMBL3655668 Ki = 37.0 nM 7.43
CHEMBL3655666 Ki = 410.0 nM 6.39