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Assay Detail

CHEMBL1638849

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Functional
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 27 7.87 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18661 IMMEPIP 1 10.40
CHEMBL19010 IODOPROXYFAN 1 10.30
CHEMBL19439 IMETIT 1 9.90
CHEMBL82298 IMMETHRIDINE 1 9.80
CHEMBL268229 1 9.50
CHEMBL175782 METHIMEPIP 1 9.50
CHEMBL268490 1 9.40
CHEMBL1632409 CLOBENPROBIT 1 9.40
CHEMBL281576 1 9.30
CHEMBL90019 IMBUTAMINE 1 9.20
CHEMBL19173 PROXYFAN 1 8.50
CHEMBL417096 IMPENTAMINE 1 8.40
CHEMBL90 HISTAMINE 4.0 1 8.30
CHEMBL11919 1 8.00
CHEMBL91353 HOMOHISTAMINE 1 7.40
CHEMBL106612 IMIFURAMINE 1 7.40
CHEMBL106931 1 7.00
CHEMBL105803 1 7.00
CHEMBL320331 1 6.70
CHEMBL1196470 1 6.50
CHEMBL106913 1 6.10
CHEMBL321920 1 6.10
CHEMBL321860 1 5.50
CHEMBL106158 1 5.00
CHEMBL1632410 1 5.00
CHEMBL322256 1 5.00
CHEMBL106570 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18661 IMMEPIP EC50 = 0.03981 nM 10.40
CHEMBL19010 IODOPROXYFAN EC50 = 0.05012 nM 10.30
CHEMBL19439 IMETIT EC50 = 0.1259 nM 9.90
CHEMBL82298 IMMETHRIDINE EC50 = 0.1585 nM 9.80
CHEMBL268229 EC50 = 0.3162 nM 9.50
CHEMBL175782 METHIMEPIP EC50 = 0.3162 nM 9.50
CHEMBL268490 EC50 = 0.3981 nM 9.40
CHEMBL1632409 CLOBENPROBIT EC50 = 0.3981 nM 9.40
CHEMBL281576 EC50 = 0.5012 nM 9.30
CHEMBL90019 IMBUTAMINE EC50 = 0.631 nM 9.20
CHEMBL19173 PROXYFAN EC50 = 3.162 nM 8.50
CHEMBL417096 IMPENTAMINE EC50 = 3.981 nM 8.40
CHEMBL90 HISTAMINE EC50 = 5.012 nM 8.30
CHEMBL11919 EC50 = 10.0 nM 8.00
CHEMBL91353 HOMOHISTAMINE EC50 = 39.81 nM 7.40
CHEMBL106612 IMIFURAMINE EC50 = 39.81 nM 7.40
CHEMBL106931 EC50 = 100.0 nM 7.00
CHEMBL105803 EC50 = 100.0 nM 7.00
CHEMBL320331 EC50 = 199.53 nM 6.70
CHEMBL1196470 EC50 = 316.23 nM 6.50
CHEMBL106913 EC50 = 794.33 nM 6.10
CHEMBL321920 EC50 = 794.33 nM 6.10
CHEMBL321860 EC50 = 3162.28 nM 5.50
CHEMBL106158 EC50 = 10000.0 nM 5.00
CHEMBL1632410 EC50 = 10000.0 nM 5.00
CHEMBL322256 EC50 = 10000.0 nM 5.00
CHEMBL106570 EC50 > 100000.0 nM -