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Assay Detail

CHEMBL699080

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

Functional
H1-antihistamine activity on guinea pig ileum
9
Total Activities
9
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

N-benzylpiperazino derivatives of 3-nitro-4-hydroxycoumarin with H1 antihistamine and mast cell stabilizing properties.
Buckle DR, Outred DJ, Smith H, Spicer BA.
J Med Chem (1984) 27 : 1452 -1457
PubMed 6208360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 7.62 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL534 KETOTIFEN 4.0 1 9.50
CHEMBL511 PYRILAMINE 4.0 1 9.10
CHEMBL35376 1 9.00
CHEMBL286017 1 8.40
CHEMBL32097 1 8.30
CHEMBL264756 1 7.90
CHEMBL286094 1 6.80
CHEMBL36517 1 5.60
CHEMBL32953 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL534 KETOTIFEN Kd = 0.3162 nM 9.50
CHEMBL511 PYRILAMINE Kd = 0.7943 nM 9.10
CHEMBL35376 Kd = 1.0 nM 9.00
CHEMBL286017 Kd = 3.981 nM 8.40
CHEMBL32097 Kd = 5.012 nM 8.30
CHEMBL264756 Kd = 12.59 nM 7.90
CHEMBL286094 Kd = 158.49 nM 6.80
CHEMBL36517 Kd = 2511.89 nM 5.60
CHEMBL32953 Kd = 100000.0 nM 4.00