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Assay Detail

CHEMBL840937

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Functional
Antagonistic activity against histamine H1 receptor
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Use of CoMFA in validating the conformation used in designing 4-(1H-benzimidazole-2-carbonyl)piperidines with H1/NK1 receptor antagonist activity
Vaz RJ, Maynard GD, Kudlacz EM, Bratton LD, Kane JM, Shatzer SA, Knippenberg RW
Bioorg Med Chem Lett (1997) 7 : 2825 -2830
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 8.21 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411691 1 8.35
CHEMBL273915 1 8.34
CHEMBL94788 1 8.30
CHEMBL430471 1 8.30
CHEMBL96441 1 8.24
CHEMBL328511 1 8.23
CHEMBL95029 1 8.22
CHEMBL318369 1 8.22
CHEMBL95243 1 8.22
CHEMBL327888 1 8.21
CHEMBL330499 1 8.20
CHEMBL94834 1 8.20
CHEMBL97240 1 8.20
CHEMBL95076 1 8.20
CHEMBL264007 1 8.20
CHEMBL330172 1 8.20
CHEMBL94480 1 8.20
CHEMBL93519 1 8.20
CHEMBL95125 1 8.20
CHEMBL322194 1 8.19
CHEMBL320003 1 8.19
CHEMBL93556 1 8.19
CHEMBL96141 1 8.19
CHEMBL96442 1 8.19
CHEMBL95127 1 8.19
CHEMBL98079 1 8.18
CHEMBL319535 1 8.18
CHEMBL94906 1 8.18
CHEMBL329055 1 8.18
CHEMBL94726 1 8.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411691 IC50 = 4.47 nM 8.35
CHEMBL273915 IC50 = 4.56 nM 8.34
CHEMBL94788 IC50 = 5.0 nM 8.30
CHEMBL430471 IC50 = 5.04 nM 8.30
CHEMBL96441 IC50 = 5.71 nM 8.24
CHEMBL328511 IC50 = 5.93 nM 8.23
CHEMBL95029 IC50 = 6.0 nM 8.22
CHEMBL318369 IC50 = 6.02 nM 8.22
CHEMBL95243 IC50 = 6.02 nM 8.22
CHEMBL327888 IC50 = 6.2 nM 8.21
CHEMBL93519 IC50 = 6.3 nM 8.20
CHEMBL94834 IC50 = 6.33 nM 8.20
CHEMBL97240 IC50 = 6.26 nM 8.20
CHEMBL95076 IC50 = 6.35 nM 8.20
CHEMBL330499 IC50 = 6.3 nM 8.20
CHEMBL264007 IC50 = 6.36 nM 8.20
CHEMBL330172 IC50 = 6.38 nM 8.20
CHEMBL94480 IC50 = 6.25 nM 8.20
CHEMBL95125 IC50 = 6.36 nM 8.20
CHEMBL322194 IC50 = 6.42 nM 8.19
CHEMBL95127 IC50 = 6.53 nM 8.19
CHEMBL96442 IC50 = 6.44 nM 8.19
CHEMBL96141 IC50 = 6.47 nM 8.19
CHEMBL93556 IC50 = 6.48 nM 8.19
CHEMBL320003 IC50 = 6.39 nM 8.19
CHEMBL98079 IC50 = 6.63 nM 8.18
CHEMBL319535 IC50 = 6.6 nM 8.18
CHEMBL94906 IC50 = 6.6 nM 8.18
CHEMBL329055 IC50 = 6.67 nM 8.18
CHEMBL94726 IC50 = 6.59 nM 8.18
CHEMBL327497 IC50 = 6.62 nM 8.18
CHEMBL330719 IC50 = 6.55 nM 8.18
CHEMBL320002 IC50 = 6.69 nM 8.18
CHEMBL97357 IC50 = 6.55 nM 8.18
CHEMBL330462 IC50 = 6.8 nM 8.17
CHEMBL96466 IC50 = 6.89 nM 8.16
CHEMBL95051 IC50 = 7.23 nM 8.14
CHEMBL98076 IC50 = 7.33 nM 8.13