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Assay Detail

CHEMBL693111

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

Binding
Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressing CHO cells
42
Total Activities
42
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

Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.
Mikó T, Ligneau X, Pertz HH, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.
J Med Chem (2003) 46 : 1523 -1530
PubMed 12672253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 6.96 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14690 CLOBENPROPIT 1 8.62
CHEMBL416053 1 8.55
CHEMBL290613 1 7.58
CHEMBL38123 1 7.57
CHEMBL544243 1 7.43
CHEMBL36630 1 7.38
CHEMBL14638 CIPROXIFAN 1 7.34
CHEMBL39716 1 7.26
CHEMBL260374 THIOPERAMIDE 1 7.22
CHEMBL284528 1 7.18
CHEMBL39603 1 7.08
CHEMBL39705 ACETOPROXIFAN 1 7.06
CHEMBL37709 1 7.06
CHEMBL36549 1 7.06
CHEMBL288431 1 7.05
CHEMBL417888 1 7.04
CHEMBL544242 1 7.04
CHEMBL39956 1 7.02
CHEMBL289641 1 6.97
CHEMBL285060 1 6.94
CHEMBL288125 1 6.92
CHEMBL290712 1 6.91
CHEMBL39791 1 6.91
CHEMBL441780 1 6.90
CHEMBL38207 1 6.90
CHEMBL35869 1 6.89
CHEMBL36590 1 6.83
CHEMBL39951 1 6.80
CHEMBL39644 1 6.79
CHEMBL417156 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14690 CLOBENPROPIT Ki = 2.4 nM 8.62
CHEMBL416053 Ki = 2.8 nM 8.55
CHEMBL290613 Ki = 26.0 nM 7.58
CHEMBL38123 Ki = 27.0 nM 7.57
CHEMBL544243 Ki = 37.0 nM 7.43
CHEMBL36630 Ki = 42.0 nM 7.38
CHEMBL14638 CIPROXIFAN Ki = 46.0 nM 7.34
CHEMBL39716 Ki = 55.0 nM 7.26
CHEMBL260374 THIOPERAMIDE Ki = 60.0 nM 7.22
CHEMBL284528 Ki = 66.0 nM 7.18
CHEMBL39603 Ki = 84.0 nM 7.08
CHEMBL37709 Ki = 87.0 nM 7.06
CHEMBL36549 Ki = 88.0 nM 7.06
CHEMBL39705 ACETOPROXIFAN Ki = 87.0 nM 7.06
CHEMBL288431 Ki = 90.0 nM 7.05
CHEMBL417888 Ki = 92.0 nM 7.04
CHEMBL544242 Ki = 91.0 nM 7.04
CHEMBL39956 Ki = 95.0 nM 7.02
CHEMBL289641 Ki = 107.0 nM 6.97
CHEMBL285060 Ki = 114.0 nM 6.94
CHEMBL288125 Ki = 119.0 nM 6.92
CHEMBL290712 Ki = 124.0 nM 6.91
CHEMBL39791 Ki = 123.0 nM 6.91
CHEMBL441780 Ki = 126.0 nM 6.90
CHEMBL38207 Ki = 125.0 nM 6.90
CHEMBL35869 Ki = 129.0 nM 6.89
CHEMBL36590 Ki = 149.0 nM 6.83
CHEMBL39951 Ki = 157.0 nM 6.80
CHEMBL39644 Ki = 163.0 nM 6.79
CHEMBL417156 Ki = 167.0 nM 6.78
CHEMBL39369 Ki = 169.0 nM 6.77
CHEMBL37737 Ki = 201.0 nM 6.70
CHEMBL40005 Ki = 227.0 nM 6.64
CHEMBL39980 Ki = 238.0 nM 6.62
CHEMBL39846 Ki = 253.0 nM 6.60
CHEMBL38378 Ki = 257.0 nM 6.59
CHEMBL34844 Ki = 334.0 nM 6.48
CHEMBL36548 Ki = 530.0 nM 6.28
CHEMBL37997 Ki = 550.0 nM 6.26
CHEMBL289935 Ki = 761.0 nM 6.12
CHEMBL415878 Ki = 890.0 nM 6.05
CHEMBL38149 Ki = 1130.0 nM 5.95