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Assay Detail

CHEMBL889157

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Binding
Binding affinity to human histamine H3 receptor
16
Total Activities
15
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

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A new class of histamine H3 receptor antagonists derived from ligand based design.
Roche O, Rodríguez Sarmiento RM.
Bioorg Med Chem Lett (2007) 17 : 3670 -3675
PubMed 17498953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.59 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL425994 1 9.52
CHEMBL27979 A-349,821 1 9.31
CHEMBL129542 JNJ-5207852 2 9.24
CHEMBL351231 1 8.62
CHEMBL230939 1 8.62
CHEMBL230089 1 7.92
CHEMBL231042 1 7.75
CHEMBL396196 1 7.33
CHEMBL231145 1 7.06
CHEMBL231146 1 6.87
CHEMBL231144 1 6.82
CHEMBL397959 1 5.99
CHEMBL230087 1 5.96
CHEMBL396197 1 5.86
CHEMBL230088 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL425994 Ki = 0.3 nM 9.52
CHEMBL27979 A-349,821 Ki = 0.4898 nM 9.31
CHEMBL129542 JNJ-5207852 Ki = 0.5754 nM 9.24
CHEMBL129542 JNJ-5207852 Ki = 1.4 nM 8.85
CHEMBL351231 Ki = 2.4 nM 8.62
CHEMBL230939 Ki = 2.4 nM 8.62
CHEMBL230089 Ki = 12.0 nM 7.92
CHEMBL231042 Ki = 18.0 nM 7.75
CHEMBL396196 Ki = 47.0 nM 7.33
CHEMBL231145 Ki = 88.0 nM 7.06
CHEMBL231146 Ki = 135.0 nM 6.87
CHEMBL231144 Ki = 150.0 nM 6.82
CHEMBL397959 Ki = 1021.0 nM 5.99
CHEMBL230087 Ki = 1100.0 nM 5.96
CHEMBL396197 Ki = 1393.0 nM 5.86
CHEMBL230088 Ki = 1810.0 nM 5.74