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Assay Detail

CHEMBL692987

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Binding
Binding affinity towards Histamine H1 receptor of human membranes.
ChEMBL ↗
54
Total Activities
53
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

Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.
Faghih R, Dwight W, Black L, Liu H, Gentles R, Phelan K, Esbenshade TA, Ireland L, Miller TR, Kang CH, Krueger KM, Fox GB, Hancock AA, Bennani YL.
Bioorg Med Chem Lett (2002) 12 : 2035 -2037
PubMed 12113836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 54 4.85 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64608 — — 1 5.82
CHEMBL61288 — — 1 5.76
CHEMBL63003 — — 1 5.70
CHEMBL302829 — — 2 5.68
CHEMBL62808 — — 1 5.64
CHEMBL60598 — — 1 5.48
CHEMBL64321 — — 1 5.48
CHEMBL63002 — — 1 5.36
CHEMBL302468 — — 1 5.34
CHEMBL59870 — — 1 5.33
CHEMBL418666 — — 1 5.33
CHEMBL60143 — — 1 5.26
CHEMBL63125 — — 1 5.17
CHEMBL64406 — — 1 5.09
CHEMBL63112 — — 1 5.09
CHEMBL417215 — — 1 5.03
CHEMBL62266 — — 1 5.03
CHEMBL60559 — — 1 5.01
CHEMBL291847 — — 1 5.01
CHEMBL305371 — — 1 5.01
CHEMBL62596 — — 1 5.00
CHEMBL64059 — — 1 5.00
CHEMBL64896 — — 1 5.00
CHEMBL59931 — — 1 4.99
CHEMBL434785 — — 1 4.97
CHEMBL60189 — — 1 4.92
CHEMBL305144 — — 1 4.90
CHEMBL62050 — — 1 4.87
CHEMBL303737 — — 1 4.84
CHEMBL62741 — — 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64608 — Ki = 1513.56 nM 5.82
CHEMBL61288 — Ki = 1737.8 nM 5.76
CHEMBL63003 — Ki = 1995.26 nM 5.70
CHEMBL302829 — Ki = 2089.3 nM 5.68
CHEMBL62808 — Ki = 2290.87 nM 5.64
CHEMBL60598 — Ki = 3311.31 nM 5.48
CHEMBL64321 — Ki = 3311.31 nM 5.48
CHEMBL63002 — Ki = 4365.16 nM 5.36
CHEMBL302468 — Ki = 4570.88 nM 5.34
CHEMBL59870 — Ki = 4677.35 nM 5.33
CHEMBL418666 — Ki = 4677.35 nM 5.33
CHEMBL60143 — Ki = 5495.41 nM 5.26
CHEMBL63125 — Ki = 6760.83 nM 5.17
CHEMBL63112 — Ki = 8128.31 nM 5.09
CHEMBL64406 — Ki = 8128.31 nM 5.09
CHEMBL417215 — Ki = 9332.54 nM 5.03
CHEMBL62266 — Ki = 9332.54 nM 5.03
CHEMBL305371 — Ki = 9772.37 nM 5.01
CHEMBL291847 — Ki = 9772.37 nM 5.01
CHEMBL60559 — Ki = 9772.37 nM 5.01
CHEMBL64059 — Ki = 10000.0 nM 5.00
CHEMBL64896 — Ki = 10000.0 nM 5.00
CHEMBL62596 — Ki = 10000.0 nM 5.00
CHEMBL59931 — Ki = 10232.93 nM 4.99
CHEMBL434785 — Ki = 10715.19 nM 4.97
CHEMBL60189 — Ki = 12022.64 nM 4.92
CHEMBL305144 — Ki = 12589.25 nM 4.90
CHEMBL62050 — Ki = 13489.63 nM 4.87
CHEMBL303737 — Ki = 14454.4 nM 4.84
CHEMBL62741 — Ki = 14454.4 nM 4.84
CHEMBL293033 — Ki = 16218.1 nM 4.79
CHEMBL303369 — Ki = 16595.87 nM 4.78
CHEMBL62903 — Ki = 16982.44 nM 4.77
CHEMBL60837 — Ki = 16982.44 nM 4.77
CHEMBL62592 — Ki = 19054.61 nM 4.72
CHEMBL312958 — Ki = 21379.62 nM 4.67
CHEMBL423666 — Ki = 21877.62 nM 4.66
CHEMBL62716 — Ki = 21877.62 nM 4.66
CHEMBL61120 — Ki = 28183.83 nM 4.55
CHEMBL294087 — Ki = 34673.69 nM 4.46
CHEMBL62421 — Ki = 35481.34 nM 4.45
CHEMBL64461 — Ki = 37153.52 nM 4.43
CHEMBL64124 — Ki = 45708.82 nM 4.34
CHEMBL304888 — Ki = 46773.51 nM 4.33
CHEMBL64120 — Ki = 46773.51 nM 4.33
CHEMBL291821 — Ki = 46773.51 nM 4.33
CHEMBL62660 — Ki = 46773.51 nM 4.33
CHEMBL62804 — Ki = 53703.18 nM 4.27
CHEMBL302196 — Ki = 69183.1 nM 4.16
CHEMBL302829 — Ki = 70794.58 nM 4.15