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Assay Detail

CHEMBL1100658

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

Binding
Displacement of [3H]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
Łazewska D, Wiecek M, Ligneau X, Kottke T, Weizel L, Seifert R, Schunack W, Stark H, Kieć-Kononowicz K.
Bioorg Med Chem Lett (2009) 19 : 6682 -6685
PubMed 19846299 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.60 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14690 CLOBENPROPIT 1 8.62
CHEMBL1076267 1 8.33
CHEMBL1081541 1 8.08
CHEMBL1080089 1 7.92
CHEMBL1081719 1 7.89
CHEMBL1081718 1 7.89
CHEMBL1080263 1 7.82
CHEMBL1079553 1 7.72
CHEMBL1080262 1 7.68
CHEMBL1079552 1 7.54
CHEMBL1081720 1 7.52
CHEMBL1080090 1 7.51
CHEMBL1079747 1 7.43
CHEMBL1079918 1 7.39
CHEMBL1079554 1 7.38
CHEMBL14638 CIPROXIFAN 1 7.34
CHEMBL1076266 1 7.31
CHEMBL1076275 1 7.28
CHEMBL260374 THIOPERAMIDE 1 7.22
CHEMBL1076300 1 7.13
CHEMBL1079746 1 7.12
CHEMBL1079748 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14690 CLOBENPROPIT Ki = 2.4 nM 8.62
CHEMBL1076267 Ki = 4.7 nM 8.33
CHEMBL1081541 Ki = 8.3 nM 8.08
CHEMBL1080089 Ki = 12.0 nM 7.92
CHEMBL1081719 Ki = 13.0 nM 7.89
CHEMBL1081718 Ki = 13.0 nM 7.89
CHEMBL1080263 Ki = 15.0 nM 7.82
CHEMBL1079553 Ki = 19.0 nM 7.72
CHEMBL1080262 Ki = 21.0 nM 7.68
CHEMBL1079552 Ki = 29.0 nM 7.54
CHEMBL1081720 Ki = 30.0 nM 7.52
CHEMBL1080090 Ki = 31.0 nM 7.51
CHEMBL1079747 Ki = 37.0 nM 7.43
CHEMBL1079918 Ki = 41.0 nM 7.39
CHEMBL1079554 Ki = 42.0 nM 7.38
CHEMBL14638 CIPROXIFAN Ki = 46.0 nM 7.34
CHEMBL1076266 Ki = 49.0 nM 7.31
CHEMBL1076275 Ki = 52.0 nM 7.28
CHEMBL260374 THIOPERAMIDE Ki = 60.0 nM 7.22
CHEMBL1076300 Ki = 74.0 nM 7.13
CHEMBL1079746 Ki = 75.0 nM 7.12
CHEMBL1079748 Ki = 91.0 nM 7.04