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Assay Detail

CHEMBL697326

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

Binding
Binding potency was determined by displacement of [3H]N-alpha-methyl histamine from histamine H3 receptor of rat cortical membranes
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.
Cowart M, Pratt JK, Stewart AO, Bennani YL, Esbenshade TA, Hancock AA.
Bioorg Med Chem Lett (2004) 14 : 689 -693
PubMed 14741270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 7.45 8.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL159087 1 8.79
CHEMBL422893 1 8.71
CHEMBL351231 1 8.49
CHEMBL159565 1 8.21
CHEMBL161781 1 8.19
CHEMBL159519 1 8.18
CHEMBL345588 1 8.16
CHEMBL159617 1 8.16
CHEMBL346562 1 8.00
CHEMBL161130 1 7.87
CHEMBL158740 1 7.79
CHEMBL161101 1 7.77
CHEMBL162591 1 7.67
CHEMBL160113 1 7.59
CHEMBL350639 1 7.59
CHEMBL422360 1 7.53
CHEMBL159858 1 7.48
CHEMBL2112921 1 7.46
CHEMBL161796 1 7.38
CHEMBL158164 1 7.37
CHEMBL350007 1 7.36
CHEMBL159476 1 7.35
CHEMBL161534 1 7.35
CHEMBL439645 1 7.33
CHEMBL161142 1 7.31
CHEMBL161133 1 7.30
CHEMBL161825 1 7.23
CHEMBL159648 1 7.20
CHEMBL159913 1 7.17
CHEMBL161624 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL159087 Ki = 1.622 nM 8.79
CHEMBL422893 Ki = 1.95 nM 8.71
CHEMBL351231 Ki = 3.236 nM 8.49
CHEMBL159565 Ki = 6.166 nM 8.21
CHEMBL161781 Ki = 6.457 nM 8.19
CHEMBL159519 Ki = 6.607 nM 8.18
CHEMBL345588 Ki = 6.918 nM 8.16
CHEMBL159617 Ki = 6.918 nM 8.16
CHEMBL346562 Ki = 10.0 nM 8.00
CHEMBL161130 Ki = 13.49 nM 7.87
CHEMBL158740 Ki = 16.22 nM 7.79
CHEMBL161101 Ki = 16.98 nM 7.77
CHEMBL162591 Ki = 21.38 nM 7.67
CHEMBL160113 Ki = 25.7 nM 7.59
CHEMBL350639 Ki = 25.7 nM 7.59
CHEMBL422360 Ki = 29.51 nM 7.53
CHEMBL159858 Ki = 33.11 nM 7.48
CHEMBL2112921 Ki = 34.67 nM 7.46
CHEMBL161796 Ki = 41.69 nM 7.38
CHEMBL158164 Ki = 42.66 nM 7.37
CHEMBL350007 Ki = 43.65 nM 7.36
CHEMBL159476 Ki = 44.67 nM 7.35
CHEMBL161534 Ki = 44.67 nM 7.35
CHEMBL439645 Ki = 46.77 nM 7.33
CHEMBL161142 Ki = 48.98 nM 7.31
CHEMBL161133 Ki = 50.12 nM 7.30
CHEMBL161825 Ki = 58.88 nM 7.23
CHEMBL159648 Ki = 63.1 nM 7.20
CHEMBL159913 Ki = 67.61 nM 7.17
CHEMBL161624 Ki = 95.5 nM 7.02
CHEMBL159343 Ki = 109.65 nM 6.96
CHEMBL159281 Ki = 138.04 nM 6.86
CHEMBL159463 Ki = 151.36 nM 6.82
CHEMBL161198 Ki = 162.18 nM 6.79
CHEMBL159282 Ki = 165.96 nM 6.78
CHEMBL436237 Ki = 257.04 nM 6.59
CHEMBL158774 Ki = 1621.81 nM 5.79
CHEMBL162536 Ki = 2187.76 nM 5.66