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Assay Detail

CHEMBL1638845

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

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

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-N-MC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Histamine H4 receptor agonists.
Igel P, Dove S, Buschauer A.
Bioorg Med Chem Lett (2010) 20 : 7191 -7199
PubMed 21044842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.11 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18661 IMMEPIP 1 9.30
CHEMBL19010 IODOPROXYFAN 1 9.20
CHEMBL82298 IMMETHRIDINE 1 9.10
CHEMBL175782 METHIMEPIP 1 9.00
CHEMBL19439 IMETIT 1 8.80
CHEMBL1632409 CLOBENPROBIT 1 8.60
CHEMBL281576 1 8.50
CHEMBL268490 1 8.40
CHEMBL90019 IMBUTAMINE 1 8.40
CHEMBL417096 IMPENTAMINE 1 8.30
CHEMBL268229 1 8.20
CHEMBL90 HISTAMINE 4.0 1 8.00
CHEMBL19173 PROXYFAN 1 7.90
CHEMBL91353 HOMOHISTAMINE 1 7.30
CHEMBL11919 1 7.20
CHEMBL106931 1 6.70
CHEMBL106612 IMIFURAMINE 1 6.60
CHEMBL105803 1 6.60
CHEMBL320331 1 6.50
CHEMBL1196470 1 6.00
CHEMBL106913 1 5.80
CHEMBL321920 1 5.70
CHEMBL321860 1 5.70
CHEMBL106158 1 5.20
CHEMBL1632410 1 5.20
CHEMBL275443 4-METHYLHISTAMINE 1 5.20
CHEMBL108649 1 5.10
CHEMBL322256 1 5.00
CHEMBL106570 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18661 IMMEPIP Ki = 0.5012 nM 9.30
CHEMBL19010 IODOPROXYFAN Ki = 0.631 nM 9.20
CHEMBL82298 IMMETHRIDINE Ki = 0.7943 nM 9.10
CHEMBL175782 METHIMEPIP Ki = 1.0 nM 9.00
CHEMBL19439 IMETIT Ki = 1.585 nM 8.80
CHEMBL1632409 CLOBENPROBIT Ki = 2.512 nM 8.60
CHEMBL281576 Ki = 3.162 nM 8.50
CHEMBL268490 Ki = 3.981 nM 8.40
CHEMBL90019 IMBUTAMINE Ki = 3.981 nM 8.40
CHEMBL417096 IMPENTAMINE Ki = 5.012 nM 8.30
CHEMBL268229 Ki = 6.31 nM 8.20
CHEMBL90 HISTAMINE Ki = 10.0 nM 8.00
CHEMBL19173 PROXYFAN Ki = 12.59 nM 7.90
CHEMBL91353 HOMOHISTAMINE Ki = 50.12 nM 7.30
CHEMBL11919 Ki = 63.1 nM 7.20
CHEMBL106931 Ki = 199.53 nM 6.70
CHEMBL106612 IMIFURAMINE Ki = 251.19 nM 6.60
CHEMBL105803 Ki = 251.19 nM 6.60
CHEMBL320331 Ki = 316.23 nM 6.50
CHEMBL1196470 Ki = 1000.0 nM 6.00
CHEMBL106913 Ki = 1584.89 nM 5.80
CHEMBL321920 Ki = 1995.26 nM 5.70
CHEMBL321860 Ki = 1995.26 nM 5.70
CHEMBL106158 Ki = 6309.57 nM 5.20
CHEMBL1632410 Ki = 6309.57 nM 5.20
CHEMBL275443 4-METHYLHISTAMINE Ki = 6309.57 nM 5.20
CHEMBL108649 Ki = 7943.28 nM 5.10
CHEMBL322256 Ki = 10000.0 nM 5.00
CHEMBL106570 Ki = 19952.62 nM 4.70