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Assay Detail

CHEMBL3396059

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Functional
Antagonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin-stimulated cAMP-mediated reporter gene activity
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SK-N-MC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H4 receptor (CHEMBL3759)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diaminopyrimidines, diaminopyridines and diaminopyridazines as histamine H4 receptor modulators.
Savall BM, Meduna SP, Tays K, Cai H, Thurmond RL, McGovern P, Gaul M, Zhao BP, Edwards JP.
Bioorg Med Chem Lett (2015) 25 : 956 -959
PubMed 25595684 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 12 8.47 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3393547 1 10.10
CHEMBL3393526 1 9.20
CHEMBL3393532 1 9.00
CHEMBL3393535 1 9.00
CHEMBL3354816 1 8.50
CHEMBL3393548 1 8.10
CHEMBL3393557 1 8.10
CHEMBL3393553 1 8.00
CHEMBL3393556 1 8.00
CHEMBL3393550 1 7.80
CHEMBL3393533 1 7.40
CHEMBL3393534 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3393547 Kd = 0.07943 nM 10.10
CHEMBL3393526 Kd = 0.631 nM 9.20
CHEMBL3393532 Kd = 1.0 nM 9.00
CHEMBL3393535 Kd = 1.0 nM 9.00
CHEMBL3354816 Kd = 3.162 nM 8.50
CHEMBL3393548 Kd = 7.943 nM 8.10
CHEMBL3393557 Kd = 7.943 nM 8.10
CHEMBL3393553 Kd = 10.0 nM 8.00
CHEMBL3393556 Kd = 10.0 nM 8.00
CHEMBL3393550 Kd = 15.85 nM 7.80
CHEMBL3393533 Kd = 39.81 nM 7.40
CHEMBL3393534 Kd = 0.00631 nM -