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Assay Detail

CHEMBL698414

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Binding
In vitro binding affinity against rat histamine H3 receptor
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H3 receptor (CHEMBL4124)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.
Meier G, Krause M, Hüls A, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.
J Med Chem (2004) 47 : 2678 -2687
PubMed 15115409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.32 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14638 CIPROXIFAN 1 9.31
CHEMBL260374 THIOPERAMIDE 1 8.40
CHEMBL88306 1 8.15
CHEMBL313803 1 7.96
CHEMBL93376 1 7.85
CHEMBL330688 1 7.85
CHEMBL329116 1 7.80
CHEMBL89999 1 7.70
CHEMBL89158 1 7.57
CHEMBL88746 1 7.48
CHEMBL88256 1 7.42
CHEMBL314526 1 7.25
CHEMBL92541 1 6.92
CHEMBL88711 1 6.84
CHEMBL91598 1 6.78
CHEMBL90821 1 6.74
CHEMBL88958 1 6.72
CHEMBL91361 1 6.70
CHEMBL90968 1 6.64
CHEMBL92168 1 6.54
CHEMBL328758 1 6.24
CHEMBL412673 1 6.17
CHEMBL91576 1 -
CHEMBL88419 1 -
CHEMBL328001 1 -
CHEMBL88362 1 -
CHEMBL315904 1 -
CHEMBL92329 1 -
CHEMBL91897 1 -
CHEMBL419133 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14638 CIPROXIFAN Ki = 0.49 nM 9.31
CHEMBL260374 THIOPERAMIDE Ki = 4.0 nM 8.40
CHEMBL88306 Ki = 7.0 nM 8.15
CHEMBL313803 Ki = 11.0 nM 7.96
CHEMBL93376 Ki = 14.0 nM 7.85
CHEMBL330688 Ki = 14.0 nM 7.85
CHEMBL329116 Ki = 16.0 nM 7.80
CHEMBL89999 Ki = 20.0 nM 7.70
CHEMBL89158 Ki = 27.0 nM 7.57
CHEMBL88746 Ki = 33.0 nM 7.48
CHEMBL88256 Ki = 38.0 nM 7.42
CHEMBL314526 Ki = 56.0 nM 7.25
CHEMBL92541 Ki = 120.0 nM 6.92
CHEMBL88711 Ki = 143.0 nM 6.84
CHEMBL91598 Ki = 167.0 nM 6.78
CHEMBL90821 Ki = 184.0 nM 6.74
CHEMBL88958 Ki = 190.0 nM 6.72
CHEMBL91361 Ki = 200.0 nM 6.70
CHEMBL90968 Ki = 230.0 nM 6.64
CHEMBL92168 Ki = 290.0 nM 6.54
CHEMBL328758 Ki = 580.0 nM 6.24
CHEMBL412673 Ki = 674.0 nM 6.17
CHEMBL91576 Ki > 500.0 nM -
CHEMBL88419 Ki > 500.0 nM -
CHEMBL328001 Ki ~ 400.0 nM -
CHEMBL88362 Ki >= 500.0 nM -
CHEMBL315904 Ki > 500.0 nM -
CHEMBL92329 Ki ~ 500.0 nM -
CHEMBL91897 Ki > 500.0 nM -
CHEMBL419133 Ki - nM -
CHEMBL91523 Ki - nM -
CHEMBL91427 Ki > 500.0 nM -
CHEMBL330063 Ki > 500.0 nM -