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Assay Detail

CHEMBL3388263

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

Binding
Displacement of [3H]histamine from human recombinant histamine H4 receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The effect of pK(a) on pyrimidine/pyridine-derived histamine H4 ligands.
Savall BM, Meduna SP, Venable J, Wei J, Smith RC, Hack MD, Thurmond RL, McGovern P, Edwards JP.
Bioorg Med Chem Lett (2014) 24 : 5489 -5492
PubMed 25455490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.55 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3236553 1 9.00
CHEMBL3354820 1 8.70
CHEMBL1770969 1 8.51
CHEMBL129198 JNJ-7777120 1 8.30
CHEMBL3354815 1 8.22
CHEMBL1770990 1 8.22
CHEMBL3354811 1 7.96
CHEMBL3354812 1 7.80
CHEMBL3354816 1 7.72
CHEMBL3236568 1 7.68
CHEMBL3354819 1 7.30
CHEMBL3354808 1 7.04
CHEMBL3354809 1 6.90
CHEMBL3354813 1 6.50
CHEMBL3354814 1 6.34
CHEMBL3354807 1 6.34
CHEMBL3354817 1 5.81
CHEMBL3354821 1 -
CHEMBL3236584 1 -
CHEMBL3354810 1 -
CHEMBL3354818 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3236553 Ki = 1.0 nM 9.00
CHEMBL3354820 Ki = 2.0 nM 8.70
CHEMBL1770969 Ki = 3.1 nM 8.51
CHEMBL129198 JNJ-7777120 Ki = 5.0 nM 8.30
CHEMBL3354815 Ki = 6.0 nM 8.22
CHEMBL1770990 Ki = 6.0 nM 8.22
CHEMBL3354811 Ki = 11.0 nM 7.96
CHEMBL3354812 Ki = 16.0 nM 7.80
CHEMBL3354816 Ki = 19.0 nM 7.72
CHEMBL3236568 Ki = 21.0 nM 7.68
CHEMBL3354819 Ki = 50.0 nM 7.30
CHEMBL3354808 Ki = 92.0 nM 7.04
CHEMBL3354809 Ki = 126.0 nM 6.90
CHEMBL3354813 Ki = 320.0 nM 6.50
CHEMBL3354814 Ki = 460.0 nM 6.34
CHEMBL3354807 Ki = 456.0 nM 6.34
CHEMBL3354817 Ki = 1547.0 nM 5.81
CHEMBL3354821 Ki > 10000.0 nM -
CHEMBL3236584 Ki > 10000.0 nM -
CHEMBL3354810 Ki > 10000.0 nM -
CHEMBL3354818 Ki > 1000.0 nM -