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Assay Detail

CHEMBL973673

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

Binding
Displacement of [3H]NAMH from histamine H3 receptor in rat cortex
ChEMBL ↗
41
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL4124) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 41 7.49 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL454109 — — 2 9.31
CHEMBL14638 CIPROXIFAN — 1 9.20
CHEMBL502704 — — 2 8.64
CHEMBL451821 — — 2 8.59
CHEMBL510387 — — 2 8.54
CHEMBL510825 — — 2 8.17
CHEMBL260374 THIOPERAMIDE — 1 8.15
CHEMBL507565 — — 2 7.95
CHEMBL454664 — — 2 7.62
CHEMBL488209 — — 2 7.61
CHEMBL191703 CONESSINE 2.0 1 7.61
CHEMBL455645 — — 2 7.42
CHEMBL453878 — — 2 7.21
CHEMBL454108 — — 2 6.86
CHEMBL508478 — — 2 6.85
CHEMBL454425 — — 2 6.81
CHEMBL510426 — — 2 6.71
CHEMBL455401 — — 2 6.62
CHEMBL509205 — — 2 6.59
CHEMBL488210 — — 2 6.59
CHEMBL455400 — — 2 6.53
CHEMBL455644 — — 2 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL454109 — Ki = 0.4898 nM 9.31
CHEMBL454109 — Ki = 0.49 nM 9.31
CHEMBL14638 CIPROXIFAN Ki = 0.631 nM 9.20
CHEMBL502704 — Ki = 2.291 nM 8.64
CHEMBL502704 — Ki = 2.29 nM 8.64
CHEMBL451821 — Ki = 2.57 nM 8.59
CHEMBL451821 — Ki = 2.57 nM 8.59
CHEMBL510387 — Ki = 2.884 nM 8.54
CHEMBL510387 — Ki = 2.88 nM 8.54
CHEMBL510825 — Ki = 6.761 nM 8.17
CHEMBL510825 — Ki = 6.76 nM 8.17
CHEMBL260374 THIOPERAMIDE Ki = 7.079 nM 8.15
CHEMBL507565 — Ki = 11.22 nM 7.95
CHEMBL507565 — Ki = 11.2 nM 7.95
CHEMBL454664 — Ki = 23.99 nM 7.62
CHEMBL454664 — Ki = 24.0 nM 7.62
CHEMBL488209 — Ki = 24.5 nM 7.61
CHEMBL191703 CONESSINE Ki = 24.55 nM 7.61
CHEMBL488209 — Ki = 24.55 nM 7.61
CHEMBL455645 — Ki = 38.02 nM 7.42
CHEMBL455645 — Ki = 38.0 nM 7.42
CHEMBL453878 — Ki = 61.7 nM 7.21
CHEMBL453878 — Ki = 61.66 nM 7.21
CHEMBL454108 — Ki = 138.0 nM 6.86
CHEMBL454108 — Ki = 138.04 nM 6.86
CHEMBL508478 — Ki = 141.0 nM 6.85
CHEMBL508478 — Ki = 141.25 nM 6.85
CHEMBL454425 — Ki = 154.88 nM 6.81
CHEMBL454425 — Ki = 155.0 nM 6.81
CHEMBL510426 — Ki = 195.0 nM 6.71
CHEMBL510426 — Ki = 194.98 nM 6.71
CHEMBL455401 — Ki = 240.0 nM 6.62
CHEMBL455401 — Ki = 239.88 nM 6.62
CHEMBL509205 — Ki = 257.0 nM 6.59
CHEMBL509205 — Ki = 257.04 nM 6.59
CHEMBL488210 — Ki = 257.04 nM 6.59
CHEMBL488210 — Ki = 257.0 nM 6.59
CHEMBL455400 — Ki = 295.0 nM 6.53
CHEMBL455400 — Ki = 295.12 nM 6.53
CHEMBL455644 — Ki = 380.19 nM 6.42
CHEMBL455644 — Ki = 380.0 nM 6.42