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Assay Detail

CHEMBL697095

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

Binding
Affinity for displacement of [125I]iodoproxyfan from human histamine H3 receptors stably expressed in CHO cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.
Apelt J, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.
J Med Chem (2002) 45 : 1128 -1141
PubMed 11855993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 7.77 10.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14364 1 10.07
CHEMBL15153 1 10.04
CHEMBL15056 1 9.48
CHEMBL276938 1 9.28
CHEMBL14754 1 8.85
CHEMBL14484 1 8.82
CHEMBL277061 1 8.74
CHEMBL14595 1 8.44
CHEMBL14573 1 8.12
CHEMBL15289 1 8.11
CHEMBL15101 1 8.00
CHEMBL276305 1 7.92
CHEMBL15098 1 7.82
CHEMBL14665 1 7.75
CHEMBL14657 1 7.72
CHEMBL14816 1 7.58
CHEMBL14283 1 7.50
CHEMBL275617 1 7.47
CHEMBL14656 1 7.30
CHEMBL275874 1 7.16
CHEMBL14781 1 7.11
CHEMBL14849 1 7.09
CHEMBL14753 1 7.07
CHEMBL14524 1 7.05
CHEMBL277988 1 6.73
CHEMBL280011 1 6.72
CHEMBL14860 1 6.44
CHEMBL14498 1 6.42
CHEMBL14740 1 6.39
CHEMBL277113 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14364 Ki = 0.086 nM 10.07
CHEMBL15153 Ki = 0.091 nM 10.04
CHEMBL15056 Ki = 0.33 nM 9.48
CHEMBL276938 Ki = 0.53 nM 9.28
CHEMBL14754 Ki = 1.4 nM 8.85
CHEMBL14484 Ki = 1.5 nM 8.82
CHEMBL277061 Ki = 1.8 nM 8.74
CHEMBL14595 Ki = 3.6 nM 8.44
CHEMBL14573 Ki = 7.6 nM 8.12
CHEMBL15289 Ki = 7.8 nM 8.11
CHEMBL15101 Ki = 9.9 nM 8.00
CHEMBL276305 Ki = 12.0 nM 7.92
CHEMBL15098 Ki = 15.0 nM 7.82
CHEMBL14665 Ki = 18.0 nM 7.75
CHEMBL14657 Ki = 19.0 nM 7.72
CHEMBL14816 Ki = 26.0 nM 7.58
CHEMBL14283 Ki = 32.0 nM 7.50
CHEMBL275617 Ki = 34.0 nM 7.47
CHEMBL14656 Ki = 50.0 nM 7.30
CHEMBL275874 Ki = 70.0 nM 7.16
CHEMBL14781 Ki = 78.0 nM 7.11
CHEMBL14849 Ki = 82.0 nM 7.09
CHEMBL14753 Ki = 85.0 nM 7.07
CHEMBL14524 Ki = 90.0 nM 7.05
CHEMBL277988 Ki = 188.0 nM 6.73
CHEMBL280011 Ki = 191.0 nM 6.72
CHEMBL14860 Ki = 362.0 nM 6.44
CHEMBL14498 Ki = 378.0 nM 6.42
CHEMBL14740 Ki = 411.0 nM 6.39
CHEMBL277113 Ki = 1130.0 nM 5.95