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Assay Detail

CHEMBL3396058

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Functional
Agonist activity at human recombinant histamine H4 receptor expressed in SK-N-MC cells assessed as effect on forskolin-stimulated cAMP-mediated reporter gene activity
20
Total Activities
20
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
EC50 20 6.90 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3393542 1 8.40
CHEMBL3393539 1 7.82
CHEMBL3393546 1 7.70
CHEMBL3354815 1 7.60
CHEMBL3393529 1 7.32
CHEMBL3393543 1 7.12
CHEMBL3393538 1 7.08
CHEMBL3393544 1 7.07
CHEMBL3393541 1 7.04
CHEMBL3393536 1 6.95
CHEMBL3393556 1 6.00
CHEMBL3354816 1 5.50
CHEMBL3393550 1 5.50
CHEMBL3393547 1 5.50
CHEMBL3393535 1 -
CHEMBL3393534 1 -
CHEMBL3393548 1 -
CHEMBL3393533 1 -
CHEMBL3393532 1 -
CHEMBL3393557 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3393542 EC50 = 4.0 nM 8.40
CHEMBL3393539 EC50 = 15.0 nM 7.82
CHEMBL3393546 EC50 = 20.0 nM 7.70
CHEMBL3354815 EC50 = 25.0 nM 7.60
CHEMBL3393529 EC50 = 48.0 nM 7.32
CHEMBL3393543 EC50 = 75.0 nM 7.12
CHEMBL3393538 EC50 = 84.0 nM 7.08
CHEMBL3393544 EC50 = 86.0 nM 7.07
CHEMBL3393541 EC50 = 91.0 nM 7.04
CHEMBL3393536 EC50 = 112.0 nM 6.95
CHEMBL3393556 EC50 = 1000.0 nM 6.00
CHEMBL3354816 EC50 = 3162.0 nM 5.50
CHEMBL3393550 EC50 = 3160.0 nM 5.50
CHEMBL3393547 EC50 = 3162.0 nM 5.50
CHEMBL3393535 EC50 > 10000.0 nM -
CHEMBL3393534 EC50 > 10000.0 nM -
CHEMBL3393548 EC50 > 10000.0 nM -
CHEMBL3393533 EC50 > 10000.0 nM -
CHEMBL3393532 EC50 > 10000.0 nM -
CHEMBL3393557 EC50 > 10000.0 nM -