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Assay Detail

CHEMBL957333

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

Binding
Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in CHO cells
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.
Wijtmans M, Celanire S, Snip E, Gillard MR, Gelens E, Collart PP, Venhuis BJ, Christophe B, Hulscher S, van der Goot H, Lebon F, Timmerman H, Bakker RA, Lallemand BI, Leurs R, Talaga PE, de Esch IJ.
J Med Chem (2008) 51 : 2944 -2953
PubMed 18433114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.48 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14690 CLOBENPROPIT 1 9.47
CHEMBL18661 IMMEPIP 1 9.39
CHEMBL82298 IMMETHRIDINE 1 9.10
CHEMBL175782 METHIMEPIP 1 9.00
CHEMBL494982 1 8.90
CHEMBL449840 1 8.74
CHEMBL268229 1 8.70
CHEMBL451399 1 8.50
CHEMBL495376 1 8.40
CHEMBL278462 CIPRALISANT 2.0 1 8.40
CHEMBL493014 1 8.35
CHEMBL453433 1 7.60
CHEMBL489493 1 7.49
CHEMBL493012 1 7.48
CHEMBL493813 1 7.40
CHEMBL503542 1 7.39
CHEMBL447687 1 7.25
CHEMBL455266 1 7.05
CHEMBL503691 1 6.81
CHEMBL494421 1 6.79
CHEMBL506072 1 6.59
CHEMBL446011 1 6.38
CHEMBL493013 1 6.37
CHEMBL505616 1 6.27
CHEMBL495158 1 6.15
CHEMBL447902 1 6.09
CHEMBL500635 1 5.76
CHEMBL455475 1 5.60
CHEMBL498149 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14690 CLOBENPROPIT Ki = 0.3388 nM 9.47
CHEMBL18661 IMMEPIP Ki = 0.4074 nM 9.39
CHEMBL82298 IMMETHRIDINE Ki = 0.7943 nM 9.10
CHEMBL175782 METHIMEPIP Ki = 1.0 nM 9.00
CHEMBL494982 Ki = 1.259 nM 8.90
CHEMBL449840 Ki = 1.82 nM 8.74
CHEMBL268229 Ki = 1.995 nM 8.70
CHEMBL451399 Ki = 3.162 nM 8.50
CHEMBL495376 Ki = 3.981 nM 8.40
CHEMBL278462 CIPRALISANT Ki = 3.981 nM 8.40
CHEMBL493014 Ki = 4.467 nM 8.35
CHEMBL453433 Ki = 25.12 nM 7.60
CHEMBL489493 Ki = 32.36 nM 7.49
CHEMBL493012 Ki = 33.11 nM 7.48
CHEMBL493813 Ki = 39.81 nM 7.40
CHEMBL503542 Ki = 40.74 nM 7.39
CHEMBL447687 Ki = 56.23 nM 7.25
CHEMBL455266 Ki = 89.13 nM 7.05
CHEMBL503691 Ki = 154.88 nM 6.81
CHEMBL494421 Ki = 162.18 nM 6.79
CHEMBL506072 Ki = 257.04 nM 6.59
CHEMBL446011 Ki = 416.87 nM 6.38
CHEMBL493013 Ki = 426.58 nM 6.37
CHEMBL505616 Ki = 537.03 nM 6.27
CHEMBL495158 Ki = 707.95 nM 6.15
CHEMBL447902 Ki = 812.83 nM 6.09
CHEMBL500635 Ki = 1737.8 nM 5.76
CHEMBL455475 Ki = 2511.89 nM 5.60
CHEMBL498149 Ki = 2511.89 nM 5.60