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Assay Detail

CHEMBL692842

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Functional
Histamine H2-receptor activity on isolated spontaneously beating guinea pig atrium
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H2 receptor (CHEMBL2882)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.
Sasse A, Sadek B, Ligneau X, Elz S, Pertz HH, Luger P, Ganellin CR, Arrang JM, Schwartz JC, Schunack W, Stark H.
J Med Chem (2000) 43 : 3335 -3343
PubMed 10966752 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 4.63 4.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112753 1 4.80
CHEMBL326624 1 4.70
CHEMBL115091 1 4.40
CHEMBL112099 1 -
CHEMBL113404 1 -
CHEMBL113403 1 -
CHEMBL322481 1 -
CHEMBL112681 1 -
CHEMBL115169 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112753 Kd = 15848.93 nM 4.80
CHEMBL326624 Kd = 19952.62 nM 4.70
CHEMBL115091 Kd = 39810.72 nM 4.40
CHEMBL112099 Kd > 50118.72 nM -
CHEMBL113404 Kd > 50118.72 nM -
CHEMBL113403 Kd > 50118.72 nM -
CHEMBL322481 Kd = 125892.54 nM -
CHEMBL112681 Kd = 158489.32 nM -
CHEMBL115169 Kd > 50118.72 nM -