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Assay Detail

CHEMBL973670

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Binding
Displacement of [3H]NAMH from human full length histamine H3 receptor expressed in rat C6 cells
ChEMBL ↗
44
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL264) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
Zhao C, Sun M, Bennani YL, Gopalakrishnan SM, Witte DG, Miller TR, Krueger KM, Browman KE, Thiffault C, Wetter J, Marsh KC, Hancock AA, Esbenshade TA, Cowart MD.
J Med Chem (2008) 51 : 5423 -5430
PubMed 18683917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 8.02 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL451821 — — 2 9.68
CHEMBL454109 — — 2 9.66
CHEMBL510387 — — 2 9.43
CHEMBL502704 — — 2 8.94
CHEMBL510825 — — 2 8.79
CHEMBL454664 — — 2 8.78
CHEMBL507565 — — 2 8.48
CHEMBL191703 CONESSINE 2.0 2 8.27
CHEMBL453878 — — 2 8.11
CHEMBL455645 — — 2 7.91
CHEMBL454425 — — 2 7.79
CHEMBL454108 — — 2 7.72
CHEMBL488891 — — 1 7.71
CHEMBL508478 — — 2 7.63
CHEMBL455401 — — 2 7.51
CHEMBL488209 — — 2 7.42
CHEMBL510426 — — 2 7.40
CHEMBL455400 — — 2 7.30
CHEMBL509205 — — 2 7.22
CHEMBL455644 — — 2 7.22
CHEMBL14638 CIPROXIFAN — 1 7.20
CHEMBL260374 THIOPERAMIDE — 1 7.14
CHEMBL488210 — — 2 6.96
CHEMBL519889 — — 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL451821 — Ki = 0.2089 nM 9.68
CHEMBL451821 — Ki = 0.21 nM 9.68
CHEMBL454109 — Ki = 0.22 nM 9.66
CHEMBL454109 — Ki = 0.2239 nM 9.65
CHEMBL510387 — Ki = 0.37 nM 9.43
CHEMBL510387 — Ki = 0.3715 nM 9.43
CHEMBL502704 — Ki = 1.148 nM 8.94
CHEMBL502704 — Ki = 1.15 nM 8.94
CHEMBL510825 — Ki = 1.622 nM 8.79
CHEMBL510825 — Ki = 1.62 nM 8.79
CHEMBL454664 — Ki = 1.66 nM 8.78
CHEMBL454664 — Ki = 1.66 nM 8.78
CHEMBL507565 — Ki = 3.31 nM 8.48
CHEMBL507565 — Ki = 3.311 nM 8.48
CHEMBL191703 CONESSINE Ki = 5.37 nM 8.27
CHEMBL191703 CONESSINE Ki = 5.37 nM 8.27
CHEMBL453878 — Ki = 7.762 nM 8.11
CHEMBL453878 — Ki = 7.76 nM 8.11
CHEMBL455645 — Ki = 12.3 nM 7.91
CHEMBL455645 — Ki = 12.3 nM 7.91
CHEMBL454425 — Ki = 16.22 nM 7.79
CHEMBL454425 — Ki = 16.2 nM 7.79
CHEMBL454108 — Ki = 19.05 nM 7.72
CHEMBL454108 — Ki = 19.0 nM 7.72
CHEMBL488891 — Ki = 19.7 nM 7.71
CHEMBL508478 — Ki = 23.44 nM 7.63
CHEMBL508478 — Ki = 23.4 nM 7.63
CHEMBL455401 — Ki = 30.9 nM 7.51
CHEMBL455401 — Ki = 30.9 nM 7.51
CHEMBL488209 — Ki = 38.0 nM 7.42
CHEMBL488209 — Ki = 38.02 nM 7.42
CHEMBL510426 — Ki = 39.81 nM 7.40
CHEMBL510426 — Ki = 39.8 nM 7.40
CHEMBL455400 — Ki = 50.1 nM 7.30
CHEMBL455400 — Ki = 50.12 nM 7.30
CHEMBL509205 — Ki = 60.26 nM 7.22
CHEMBL509205 — Ki = 60.3 nM 7.22
CHEMBL455644 — Ki = 60.26 nM 7.22
CHEMBL455644 — Ki = 60.3 nM 7.22
CHEMBL14638 CIPROXIFAN Ki = 63.1 nM 7.20
CHEMBL260374 THIOPERAMIDE Ki = 72.44 nM 7.14
CHEMBL488210 — Ki = 110.0 nM 6.96
CHEMBL488210 — Ki = 109.65 nM 6.96
CHEMBL519889 — Ki = 543.0 nM 6.26