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Assay Detail

CHEMBL694514

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

Functional
Antagonism of guinea pig ileum contraction at 100 nM mepyramine
8
Total Activities
5
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

Histaprodifens: synthesis, pharmacological in vitro evaluation, and molecular modeling of a new class of highly active and selective histamine H(1)-receptor agonists.
Elz S, Kramer K, Pertz HH, Detert H, ter Laak AM, Kühne R, Schunack W.
J Med Chem (2000) 43 : 1071 -1084
PubMed 10737740 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 8.93 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275035 2 9.13
CHEMBL275507 1 9.11
CHEMBL11553 2 9.11
CHEMBL274831 2 8.85
CHEMBL11515 1 8.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275035 Kd = 0.7413 nM 9.13
CHEMBL275507 Kd = 0.7762 nM 9.11
CHEMBL11553 Kd = 0.7762 nM 9.11
CHEMBL275035 Kd = 1.349 nM 8.87
CHEMBL11553 Kd = 1.38 nM 8.86
CHEMBL274831 Kd = 1.413 nM 8.85
CHEMBL11515 Kd = 1.549 nM 8.81
CHEMBL274831 Kd = 2.138 nM 8.67