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Assay Detail

CHEMBL1638839

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Binding
Displacement of [3H]-histamine from human histamine H4 receptor expressed in Sf9 cells coexpressing RGS19, Galphai2, Gbeta1gamma2
ChEMBL ↗
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H4 receptor (CHEMBL3759) ↗
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 44 6.66 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19439 IMETIT — 1 8.20
CHEMBL1632409 CLOBENPROBIT — 1 8.10
CHEMBL90 HISTAMINE 4.0 1 8.10
CHEMBL306077 — — 1 8.10
CHEMBL281576 — — 1 8.00
CHEMBL72769 — — 1 8.00
CHEMBL90019 IMBUTAMINE — 1 8.00
CHEMBL19010 IODOPROXYFAN — 1 7.90
CHEMBL18661 IMMEPIP — 1 7.70
CHEMBL72424 — — 1 7.60
CHEMBL309819 — — 1 7.60
CHEMBL12608 IMPROMIDINE 2.0 1 7.60
CHEMBL91353 HOMOHISTAMINE — 1 7.50
CHEMBL1196470 — — 1 7.50
CHEMBL12160 BURIMAMIDE — 1 7.40
CHEMBL275443 4-METHYLHISTAMINE — 1 7.30
CHEMBL19173 PROXYFAN — 1 7.30
CHEMBL72431 — — 1 7.30
CHEMBL308913 — — 1 7.20
CHEMBL72372 — — 1 6.90
CHEMBL321860 — — 1 6.90
CHEMBL106158 — — 1 6.70
CHEMBL82298 IMMETHRIDINE — 1 6.60
CHEMBL417096 IMPENTAMINE — 1 6.60
CHEMBL268229 — — 1 6.60
CHEMBL12344 DIMAPRIT — 1 6.50
CHEMBL268490 — — 1 6.50
CHEMBL320331 — — 1 6.40
CHEMBL12620 2-METHYLHISTAMINE — 1 6.10
CHEMBL106612 IMIFURAMINE — 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19439 IMETIT Ki = 6.31 nM 8.20
CHEMBL1632409 CLOBENPROBIT Ki = 7.943 nM 8.10
CHEMBL90 HISTAMINE Ki = 7.943 nM 8.10
CHEMBL306077 — Ki = 7.943 nM 8.10
CHEMBL281576 — Ki = 10.0 nM 8.00
CHEMBL72769 — Ki = 10.0 nM 8.00
CHEMBL90019 IMBUTAMINE Ki = 10.0 nM 8.00
CHEMBL19010 IODOPROXYFAN Ki = 12.59 nM 7.90
CHEMBL18661 IMMEPIP Ki = 19.95 nM 7.70
CHEMBL72424 — Ki = 25.12 nM 7.60
CHEMBL309819 — Ki = 25.12 nM 7.60
CHEMBL12608 IMPROMIDINE Ki = 25.12 nM 7.60
CHEMBL91353 HOMOHISTAMINE Ki = 31.62 nM 7.50
CHEMBL1196470 — Ki = 31.62 nM 7.50
CHEMBL12160 BURIMAMIDE Ki = 39.81 nM 7.40
CHEMBL275443 4-METHYLHISTAMINE Ki = 50.12 nM 7.30
CHEMBL72431 — Ki = 50.12 nM 7.30
CHEMBL19173 PROXYFAN Ki = 50.12 nM 7.30
CHEMBL308913 — Ki = 63.1 nM 7.20
CHEMBL72372 — Ki = 125.89 nM 6.90
CHEMBL321860 — Ki = 125.89 nM 6.90
CHEMBL106158 — Ki = 199.53 nM 6.70
CHEMBL82298 IMMETHRIDINE Ki = 251.19 nM 6.60
CHEMBL268229 — Ki = 251.19 nM 6.60
CHEMBL417096 IMPENTAMINE Ki = 251.19 nM 6.60
CHEMBL12344 DIMAPRIT Ki = 316.23 nM 6.50
CHEMBL268490 — Ki = 316.23 nM 6.50
CHEMBL320331 — Ki = 398.11 nM 6.40
CHEMBL12620 2-METHYLHISTAMINE Ki = 794.33 nM 6.10
CHEMBL106612 IMIFURAMINE Ki = 794.33 nM 6.10
CHEMBL105803 — Ki = 1000.0 nM 6.00
CHEMBL24665 — Ki = 1258.93 nM 5.90
CHEMBL26116 — Ki = 1584.89 nM 5.80
CHEMBL175782 METHIMEPIP Ki = 1995.26 nM 5.70
CHEMBL321920 — Ki = 2511.89 nM 5.60
CHEMBL1632408 AMSELAMINE Ki = 2511.89 nM 5.60
CHEMBL11919 — Ki = 3981.07 nM 5.40
CHEMBL293762 AMTHAMINE Ki = 5011.87 nM 5.30
CHEMBL106913 — Ki = 6309.57 nM 5.20
CHEMBL108649 — Ki = 7943.28 nM 5.10
CHEMBL106931 — Ki = 12589.25 nM 4.90
CHEMBL1632410 — Ki = 12589.25 nM 4.90
CHEMBL106570 — Ki = 19952.62 nM 4.70
CHEMBL322256 — Ki = 19952.62 nM 4.70