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Assay Detail

CHEMBL692983

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Binding
Inhibitory activity against human Histamine H1 receptor
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H1 receptor (CHEMBL231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists.
Govoni M, Bakker RA, van de Wetering I, Smit MJ, Menge WM, Timmerman H, Elz S, Schunack W, Leurs R.
J Med Chem (2003) 46 : 5812 -5824
PubMed 14667234 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.02 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511 PYRILAMINE 4.0 1 7.90
CHEMBL1241 TRIPELENNAMINE 4.0 1 7.40
CHEMBL90 HISTAMINE 4.0 1 6.80
CHEMBL158352 1 6.60
CHEMBL157217 1 6.40
CHEMBL157273 1 6.40
CHEMBL94249 1 6.30
CHEMBL152126 1 6.20
CHEMBL275507 1 6.10
CHEMBL24665 1 6.00
CHEMBL155188 1 6.00
CHEMBL152122 1 5.90
CHEMBL156071 1 5.90
CHEMBL32813 1 5.90
CHEMBL345185 1 5.70
CHEMBL287052 1 5.70
CHEMBL155314 1 5.70
CHEMBL359122 1 5.60
CHEMBL157842 1 5.60
CHEMBL90063 1 5.50
CHEMBL152221 1 5.40
CHEMBL154566 1 5.10
CHEMBL154068 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511 PYRILAMINE IC50 = 12.59 nM 7.90
CHEMBL1241 TRIPELENNAMINE IC50 = 39.81 nM 7.40
CHEMBL90 HISTAMINE IC50 = 158.49 nM 6.80
CHEMBL158352 IC50 = 251.19 nM 6.60
CHEMBL157217 IC50 = 398.11 nM 6.40
CHEMBL157273 IC50 = 398.11 nM 6.40
CHEMBL94249 IC50 = 501.19 nM 6.30
CHEMBL152126 IC50 = 630.96 nM 6.20
CHEMBL275507 IC50 = 794.33 nM 6.10
CHEMBL24665 IC50 = 1000.0 nM 6.00
CHEMBL155188 IC50 = 1000.0 nM 6.00
CHEMBL152122 IC50 = 1258.93 nM 5.90
CHEMBL156071 IC50 = 1258.93 nM 5.90
CHEMBL32813 IC50 = 1258.93 nM 5.90
CHEMBL345185 IC50 = 1995.26 nM 5.70
CHEMBL287052 IC50 = 1995.26 nM 5.70
CHEMBL155314 IC50 = 1995.26 nM 5.70
CHEMBL359122 IC50 = 2511.89 nM 5.60
CHEMBL157842 IC50 = 2511.89 nM 5.60
CHEMBL90063 IC50 = 3162.28 nM 5.50
CHEMBL152221 IC50 = 3981.07 nM 5.40
CHEMBL154566 IC50 = 7943.28 nM 5.10
CHEMBL154068 IC50 = 50118.72 nM 4.30