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Assay Detail

CHEMBL693107

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 cloned human histamine H3 receptor expressed in C6 cells
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type C6
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

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 8.10 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL351231 1 9.35
CHEMBL159087 1 9.26
CHEMBL422893 1 9.15
CHEMBL161781 1 9.02
CHEMBL159519 1 8.92
CHEMBL345588 1 8.72
CHEMBL159617 1 8.66
CHEMBL160113 1 8.66
CHEMBL159565 1 8.64
CHEMBL162591 1 8.62
CHEMBL161130 1 8.52
CHEMBL346562 1 8.46
CHEMBL422360 1 8.41
CHEMBL439645 1 8.38
CHEMBL161796 1 8.29
CHEMBL159476 1 8.25
CHEMBL161534 1 8.24
CHEMBL350639 1 8.23
CHEMBL161101 1 8.23
CHEMBL2112921 1 8.21
CHEMBL350007 1 8.11
CHEMBL161825 1 8.06
CHEMBL161624 1 8.06
CHEMBL161133 1 8.00
CHEMBL159913 1 7.92
CHEMBL161142 1 7.92
CHEMBL158740 1 7.82
CHEMBL159648 1 7.80
CHEMBL159858 1 7.80
CHEMBL158164 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL351231 Ki = 0.45 nM 9.35
CHEMBL159087 Ki = 0.55 nM 9.26
CHEMBL422893 Ki = 0.7 nM 9.15
CHEMBL161781 Ki = 0.95 nM 9.02
CHEMBL159519 Ki = 1.2 nM 8.92
CHEMBL345588 Ki = 1.9 nM 8.72
CHEMBL159617 Ki = 2.2 nM 8.66
CHEMBL160113 Ki = 2.2 nM 8.66
CHEMBL159565 Ki = 2.3 nM 8.64
CHEMBL162591 Ki = 2.4 nM 8.62
CHEMBL161130 Ki = 3.0 nM 8.52
CHEMBL346562 Ki = 3.5 nM 8.46
CHEMBL422360 Ki = 3.9 nM 8.41
CHEMBL439645 Ki = 4.2 nM 8.38
CHEMBL161796 Ki = 5.1 nM 8.29
CHEMBL159476 Ki = 5.6 nM 8.25
CHEMBL161534 Ki = 5.8 nM 8.24
CHEMBL350639 Ki = 5.9 nM 8.23
CHEMBL161101 Ki = 5.9 nM 8.23
CHEMBL2112921 Ki = 6.2 nM 8.21
CHEMBL350007 Ki = 7.8 nM 8.11
CHEMBL161825 Ki = 8.8 nM 8.06
CHEMBL161624 Ki = 8.8 nM 8.06
CHEMBL161133 Ki = 10.0 nM 8.00
CHEMBL159913 Ki = 12.0 nM 7.92
CHEMBL161142 Ki = 12.0 nM 7.92
CHEMBL158740 Ki = 15.0 nM 7.82
CHEMBL159648 Ki = 16.0 nM 7.80
CHEMBL159858 Ki = 16.0 nM 7.80
CHEMBL158164 Ki = 17.0 nM 7.77
CHEMBL159282 Ki = 18.0 nM 7.75
CHEMBL159343 Ki = 36.0 nM 7.44
CHEMBL161198 Ki = 45.0 nM 7.35
CHEMBL159281 Ki = 49.0 nM 7.31
CHEMBL159463 Ki = 87.0 nM 7.06
CHEMBL436237 Ki = 150.0 nM 6.82
CHEMBL158774 Ki = 320.0 nM 6.50
CHEMBL162536 Ki = 600.0 nM 6.22