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Assay Detail

CHEMBL693563

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Binding
Binding affinity for rat histamine H3 receptor on rat cortical cells
ChEMBL ↗
100
Total Activities
99
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 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.
Gfesser GA, Zhang H, Dinges J, Fox GB, Pan JB, Esbenshade TA, Yao BB, Witte D, Miller TR, Kang CH, Krueger KM, Bennani YL, Hancock AA, Faghih R.
Bioorg Med Chem Lett (2004) 14 : 673 -676
PubMed 14741266 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 100 8.46 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158714 — — 1 9.25
CHEMBL158761 — — 1 9.24
CHEMBL349692 — — 1 9.08
CHEMBL161202 — — 1 9.07
CHEMBL443817 — — 1 9.03
CHEMBL62803 — — 1 9.00
CHEMBL157585 — — 1 8.96
CHEMBL161743 — — 1 8.96
CHEMBL162595 — — 1 8.96
CHEMBL162129 — — 1 8.96
CHEMBL350385 — — 1 8.96
CHEMBL351192 — — 1 8.92
CHEMBL161138 — — 1 8.92
CHEMBL351101 — — 1 8.89
CHEMBL347909 — — 1 8.89
CHEMBL161479 — — 1 8.89
CHEMBL161785 — — 1 8.85
CHEMBL158802 — — 1 8.85
CHEMBL348328 — — 1 8.82
CHEMBL345860 — — 1 8.82
CHEMBL159078 — — 1 8.82
CHEMBL161056 — — 1 8.82
CHEMBL158765 — — 1 8.80
CHEMBL349879 — — 1 8.77
CHEMBL348279 — — 1 8.77
CHEMBL14720 — — 1 8.77
CHEMBL350741 — — 1 8.77
CHEMBL346710 — — 1 8.74
CHEMBL351918 — — 1 8.72
CHEMBL159085 — — 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158714 — Ki = 0.56 nM 9.25
CHEMBL158761 — Ki = 0.58 nM 9.24
CHEMBL349692 — Ki = 0.83 nM 9.08
CHEMBL161202 — Ki = 0.86 nM 9.07
CHEMBL443817 — Ki = 0.94 nM 9.03
CHEMBL62803 — Ki = 1.0 nM 9.00
CHEMBL157585 — Ki = 1.1 nM 8.96
CHEMBL162129 — Ki = 1.1 nM 8.96
CHEMBL161743 — Ki = 1.1 nM 8.96
CHEMBL350385 — Ki = 1.1 nM 8.96
CHEMBL162595 — Ki = 1.1 nM 8.96
CHEMBL161138 — Ki = 1.2 nM 8.92
CHEMBL351192 — Ki = 1.2 nM 8.92
CHEMBL351101 — Ki = 1.3 nM 8.89
CHEMBL347909 — Ki = 1.3 nM 8.89
CHEMBL161479 — Ki = 1.3 nM 8.89
CHEMBL158802 — Ki = 1.4 nM 8.85
CHEMBL161785 — Ki = 1.4 nM 8.85
CHEMBL345860 — Ki = 1.5 nM 8.82
CHEMBL348328 — Ki = 1.5 nM 8.82
CHEMBL161056 — Ki = 1.5 nM 8.82
CHEMBL159078 — Ki = 1.5 nM 8.82
CHEMBL158765 — Ki = 1.6 nM 8.80
CHEMBL348279 — Ki = 1.7 nM 8.77
CHEMBL14720 — Ki = 1.7 nM 8.77
CHEMBL349879 — Ki = 1.7 nM 8.77
CHEMBL350741 — Ki = 1.7 nM 8.77
CHEMBL346710 — Ki = 1.8 nM 8.74
CHEMBL351918 — Ki = 1.9 nM 8.72
CHEMBL159085 — Ki = 2.0 nM 8.70
CHEMBL347251 — Ki = 2.0 nM 8.70
CHEMBL158056 — Ki = 2.1 nM 8.68
CHEMBL161279 — Ki = 2.3 nM 8.64
CHEMBL161283 — Ki = 2.3 nM 8.64
CHEMBL161346 — Ki = 2.4 nM 8.62
CHEMBL160729 — Ki = 2.4 nM 8.62
CHEMBL158595 — Ki = 2.4 nM 8.62
CHEMBL162355 — Ki = 2.4 nM 8.62
CHEMBL352439 — Ki = 2.4 nM 8.62
CHEMBL350998 — Ki = 2.5 nM 8.60
CHEMBL349419 — Ki = 2.6 nM 8.59
CHEMBL161627 — Ki = 2.6 nM 8.59
CHEMBL157534 — Ki = 2.6 nM 8.59
CHEMBL345143 — Ki = 2.6 nM 8.59
CHEMBL161568 — Ki = 2.6 nM 8.59
CHEMBL346711 — Ki = 2.8 nM 8.55
CHEMBL161800 — Ki = 2.8 nM 8.55
CHEMBL350649 — Ki = 2.8 nM 8.55
CHEMBL158662 — Ki = 2.9 nM 8.54
CHEMBL161646 — Ki = 3.0 nM 8.52