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Assay Detail

CHEMBL4481718

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Binding
Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Alkyl derivatives of 1,3,5-triazine as histamine H<sub>4</sub> receptor ligands.
Łażewska D, Mogilski S, Hagenow S, Kuder K, Głuch-Lutwin M, Siwek A, Więcek M, Kaleta M, Seibel U, Buschauer A, Filipek B, Stark H, Kieć-Kononowicz K.
Bioorg Med Chem (2019) 27 : 1254 -1262
PubMed 30792106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 6.39 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1305 ANTAZOLINE 4.0 1 7.14
CHEMBL129198 JNJ-7777120 1 6.11
CHEMBL4483783 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1305 ANTAZOLINE Kd = 72.44 nM 7.14
CHEMBL129198 JNJ-7777120 Kd = 776.25 nM 6.11
CHEMBL4483783 Kd = 1230.27 nM 5.91