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Assay Detail

CHEMBL2154958

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Binding
Binding affinity to human histamine H1 receptor
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Histamine H3 receptor as a drug discovery target.
Berlin M, Boyce CW, Ruiz Mde L.
J Med Chem (2011) 54 : 26 -53
PubMed 21062081 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.36 8.15
Kd 2 9.29 10.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL715 OLANZAPINE 4.0 1 10.06
CHEMBL42 CLOZAPINE 4.0 1 8.51
CHEMBL292195 1 8.15
CHEMBL2151156 1 7.90
CHEMBL1767164 GSK-1004723 2.0 1 7.80
CHEMBL2151155 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL715 OLANZAPINE Kd = 0.087 nM 10.06
CHEMBL42 CLOZAPINE Kd = 3.1 nM 8.51
CHEMBL292195 Ki = 7.0 nM 8.15
CHEMBL2151156 Ki = 12.59 nM 7.90
CHEMBL1767164 GSK-1004723 Ki = 15.85 nM 7.80
CHEMBL2151155 Ki = 2511.89 nM 5.60