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Assay Detail

CHEMBL695156

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Functional
Functional Histamine H1 receptor antagonistic activity in vitro assay on guinea pig ileum
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Histamine H1 receptor (CHEMBL3943)
Type SINGLE PROTEIN
Organism Cavia porcellus

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
Kd 16 4.89 5.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313803 1 5.60
CHEMBL89999 1 5.10
CHEMBL330688 1 5.10
CHEMBL91523 1 4.80
CHEMBL88746 1 4.70
CHEMBL88306 1 4.70
CHEMBL88362 1 4.20
CHEMBL328758 1 -
CHEMBL92541 1 -
CHEMBL90968 1 -
CHEMBL329116 1 -
CHEMBL91361 1 -
CHEMBL88958 1 -
CHEMBL88256 1 -
CHEMBL92168 1 -
CHEMBL88419 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313803 Kd = 2511.89 nM 5.60
CHEMBL89999 Kd = 7943.28 nM 5.10
CHEMBL330688 Kd = 7943.28 nM 5.10
CHEMBL91523 Kd = 15848.93 nM 4.80
CHEMBL88746 Kd = 19952.62 nM 4.70
CHEMBL88306 Kd = 19952.62 nM 4.70
CHEMBL88362 Kd = 63095.73 nM 4.20
CHEMBL328758 Kd > 100000.0 nM -
CHEMBL92541 Kd > 100000.0 nM -
CHEMBL90968 Kd > 31622.78 nM -
CHEMBL329116 Kd > 100000.0 nM -
CHEMBL91361 Kd > 316227.77 nM -
CHEMBL88958 Kd > 316227.77 nM -
CHEMBL88256 Kd > 100000.0 nM -
CHEMBL92168 Kd > 100000.0 nM -
CHEMBL88419 Kd = 251188.64 nM -