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Assay Detail

CHEMBL697960

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Functional
Functional Histamine H3 receptor antagonistic activity in vitro assay on synaptosomes of rat cerebral cortex
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Brain
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 15 7.24 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88306 1 8.20
CHEMBL313803 1 8.00
CHEMBL330688 1 7.90
CHEMBL329116 1 7.80
CHEMBL89999 1 7.70
CHEMBL88746 1 7.50
CHEMBL88256 1 7.40
CHEMBL92541 1 6.90
CHEMBL91361 1 6.70
CHEMBL88958 1 6.70
CHEMBL90968 1 6.60
CHEMBL92168 1 6.50
CHEMBL328758 1 6.20
CHEMBL88362 1 -
CHEMBL88419 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88306 Ki = 6.31 nM 8.20
CHEMBL313803 Ki = 10.0 nM 8.00
CHEMBL330688 Ki = 12.59 nM 7.90
CHEMBL329116 Ki = 15.85 nM 7.80
CHEMBL89999 Ki = 19.95 nM 7.70
CHEMBL88746 Ki = 31.62 nM 7.50
CHEMBL88256 Ki = 39.81 nM 7.40
CHEMBL92541 Ki = 125.89 nM 6.90
CHEMBL91361 Ki = 199.53 nM 6.70
CHEMBL88958 Ki = 199.53 nM 6.70
CHEMBL90968 Ki = 251.19 nM 6.60
CHEMBL92168 Ki = 316.23 nM 6.50
CHEMBL328758 Ki = 630.96 nM 6.20
CHEMBL88362 Ki ~ 1995262314968882.8 nM -
CHEMBL88419 Ki < 1000.0 nM -