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Assay Detail

CHEMBL3755092

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

Binding
Binding affinity to recombinant human H3 receptor
8
Total Activities
8
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 H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.
Nirogi R, Shinde A, Tiriveedhi V, Kota L, Saraf SK, Badange RK, Mohammed AR, Subramanian R, Muddana N, Bhyrapuneni G, Abraham R.
Eur J Med Chem (2016) 108 : 655 -662
PubMed 26731168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.99 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3753475 1 10.52
CHEMBL3753901 1 10.00
CHEMBL3753093 1 9.05
CHEMBL3752655 1 9.00
CHEMBL3753703 1 8.92
CHEMBL2103862 BAVISANT 2.0 1 8.27
CHEMBL476323 MK-0249 2.0 1 8.17
CHEMBL3092650 GSK239512 2.0 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3753475 Ki = 0.03 nM 10.52
CHEMBL3753901 Ki = 0.1 nM 10.00
CHEMBL3753093 Ki = 0.9 nM 9.05
CHEMBL3752655 Ki = 1.0 nM 9.00
CHEMBL3753703 Ki = 1.2 nM 8.92
CHEMBL2103862 BAVISANT Ki = 5.4 nM 8.27
CHEMBL476323 MK-0249 Ki = 6.8 nM 8.17
CHEMBL3092650 GSK239512 Ki = 10.0 nM 8.00