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Assay Detail

CHEMBL697540

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Binding
Binding affinity towards Histamine H3 receptor of rat cortical 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 H3 receptor (CHEMBL4124) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 7.86 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61120 — — 1 9.30
CHEMBL63125 — — 1 8.91
CHEMBL302196 — — 1 8.90
CHEMBL305144 — — 1 8.88
CHEMBL302829 — — 2 8.80
CHEMBL62421 — — 1 8.72
CHEMBL64406 — — 1 8.68
CHEMBL60401 — — 1 8.64
CHEMBL60837 — — 1 8.62
CHEMBL418666 — — 1 8.60
CHEMBL60143 — — 1 8.40
CHEMBL291821 — — 1 8.40
CHEMBL62596 — — 1 8.36
CHEMBL61792 — — 1 8.34
CHEMBL64059 — — 1 8.34
CHEMBL60435 — — 1 8.33
CHEMBL59733 — — 1 8.24
CHEMBL64608 — — 1 8.19
CHEMBL62660 — — 1 8.15
CHEMBL293033 — — 1 8.07
CHEMBL304888 — — 1 8.06
CHEMBL61288 — — 1 8.05
CHEMBL64321 — — 1 8.04
CHEMBL62808 — — 1 7.99
CHEMBL59931 — — 1 7.92
CHEMBL64896 — — 1 7.89
CHEMBL59870 — — 1 7.84
CHEMBL60598 — — 1 7.83
CHEMBL303369 — — 1 7.77
CHEMBL62804 — — 1 7.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61120 — Ki = 0.5012 nM 9.30
CHEMBL63125 — Ki = 1.23 nM 8.91
CHEMBL302196 — Ki = 1.259 nM 8.90
CHEMBL305144 — Ki = 1.318 nM 8.88
CHEMBL302829 — Ki = 1.585 nM 8.80
CHEMBL62421 — Ki = 1.905 nM 8.72
CHEMBL302829 — Ki = 1.95 nM 8.71
CHEMBL64406 — Ki = 2.089 nM 8.68
CHEMBL60401 — Ki = 2.291 nM 8.64
CHEMBL60837 — Ki = 2.399 nM 8.62
CHEMBL418666 — Ki = 2.512 nM 8.60
CHEMBL291821 — Ki = 3.981 nM 8.40
CHEMBL60143 — Ki = 3.981 nM 8.40
CHEMBL62596 — Ki = 4.365 nM 8.36
CHEMBL61792 — Ki = 4.571 nM 8.34
CHEMBL64059 — Ki = 4.571 nM 8.34
CHEMBL60435 — Ki = 4.677 nM 8.33
CHEMBL59733 — Ki = 5.754 nM 8.24
CHEMBL64608 — Ki = 6.457 nM 8.19
CHEMBL62660 — Ki = 7.079 nM 8.15
CHEMBL293033 — Ki = 8.511 nM 8.07
CHEMBL304888 — Ki = 8.71 nM 8.06
CHEMBL61288 — Ki = 8.913 nM 8.05
CHEMBL64321 — Ki = 9.12 nM 8.04
CHEMBL62808 — Ki = 10.23 nM 7.99
CHEMBL59931 — Ki = 12.02 nM 7.92
CHEMBL64896 — Ki = 12.88 nM 7.89
CHEMBL59870 — Ki = 14.45 nM 7.84
CHEMBL60598 — Ki = 14.79 nM 7.83
CHEMBL303369 — Ki = 16.98 nM 7.77
CHEMBL62804 — Ki = 20.42 nM 7.69
CHEMBL60559 — Ki = 22.91 nM 7.64
CHEMBL62903 — Ki = 23.44 nM 7.63
CHEMBL434785 — Ki = 26.3 nM 7.58
CHEMBL302468 — Ki = 27.54 nM 7.56
CHEMBL64124 — Ki = 28.84 nM 7.54
CHEMBL417215 — Ki = 29.51 nM 7.53
CHEMBL64461 — Ki = 30.2 nM 7.52
CHEMBL305371 — Ki = 30.2 nM 7.52
CHEMBL423666 — Ki = 42.66 nM 7.37
CHEMBL62050 — Ki = 43.65 nM 7.36
CHEMBL62716 — Ki = 52.48 nM 7.28
CHEMBL62266 — Ki = 53.7 nM 7.27
CHEMBL62741 — Ki = 61.66 nM 7.21
CHEMBL294087 — Ki = 75.86 nM 7.12
CHEMBL62592 — Ki = 79.43 nM 7.10
CHEMBL312958 — Ki = 97.72 nM 7.01
CHEMBL63112 — Ki = 112.2 nM 6.95
CHEMBL64120 — Ki = 120.23 nM 6.92
CHEMBL60189 — Ki = 131.83 nM 6.88