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Assay Detail

CHEMBL930580

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Binding
Binding affinity at rat recombinant histamine H3 receptor in rat cortical membranes
ChEMBL ↗
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL4124) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Nersesian DL, Black LA, Miller TR, Vortherms TA, Esbenshade TA, Hancock AA, Cowart MD.
Bioorg Med Chem Lett (2008) 18 : 355 -359
PubMed 18077160 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 60 6.94 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429914 — — 1 8.41
CHEMBL269951 — — 1 8.23
CHEMBL441903 — — 1 8.15
CHEMBL271898 — — 1 7.92
CHEMBL257915 — — 1 7.52
CHEMBL270630 — — 1 7.46
CHEMBL403052 — — 1 7.43
CHEMBL271661 — — 1 7.40
CHEMBL402220 — — 1 7.39
CHEMBL402872 — — 1 7.37
CHEMBL402187 — — 1 7.21
CHEMBL404532 — — 1 7.20
CHEMBL272141 — — 1 7.14
CHEMBL255141 — — 1 7.09
CHEMBL402377 — — 1 7.05
CHEMBL404375 — — 1 6.96
CHEMBL402873 — — 1 6.85
CHEMBL408259 — — 1 6.82
CHEMBL406698 — — 1 6.80
CHEMBL271300 — — 1 6.80
CHEMBL439429 — — 1 6.80
CHEMBL272306 — — 1 6.77
CHEMBL271237 — — 1 6.68
CHEMBL408617 — — 1 6.66
CHEMBL271489 — — 1 6.64
CHEMBL272140 — — 1 6.64
CHEMBL404912 — — 1 6.62
CHEMBL257914 — — 1 6.62
CHEMBL404834 — — 1 6.62
CHEMBL257913 — — 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429914 — Ki = 3.9 nM 8.41
CHEMBL269951 — Ki = 5.9 nM 8.23
CHEMBL441903 — Ki = 7.1 nM 8.15
CHEMBL271898 — Ki = 12.0 nM 7.92
CHEMBL257915 — Ki = 30.0 nM 7.52
CHEMBL270630 — Ki = 35.0 nM 7.46
CHEMBL403052 — Ki = 37.0 nM 7.43
CHEMBL271661 — Ki = 40.0 nM 7.40
CHEMBL402220 — Ki = 41.0 nM 7.39
CHEMBL402872 — Ki = 43.0 nM 7.37
CHEMBL402187 — Ki = 62.0 nM 7.21
CHEMBL404532 — Ki = 63.0 nM 7.20
CHEMBL272141 — Ki = 72.0 nM 7.14
CHEMBL255141 — Ki = 81.0 nM 7.09
CHEMBL402377 — Ki = 89.0 nM 7.05
CHEMBL404375 — Ki = 110.0 nM 6.96
CHEMBL402873 — Ki = 140.0 nM 6.85
CHEMBL408259 — Ki = 150.0 nM 6.82
CHEMBL406698 — Ki = 160.0 nM 6.80
CHEMBL271300 — Ki = 160.0 nM 6.80
CHEMBL439429 — Ki = 160.0 nM 6.80
CHEMBL272306 — Ki = 170.0 nM 6.77
CHEMBL271237 — Ki = 210.0 nM 6.68
CHEMBL408617 — Ki = 220.0 nM 6.66
CHEMBL272140 — Ki = 230.0 nM 6.64
CHEMBL271489 — Ki = 230.0 nM 6.64
CHEMBL404912 — Ki = 240.0 nM 6.62
CHEMBL257914 — Ki = 240.0 nM 6.62
CHEMBL404834 — Ki = 240.0 nM 6.62
CHEMBL257913 — Ki = 260.0 nM 6.58
CHEMBL257235 — Ki = 260.0 nM 6.58
CHEMBL440996 — Ki = 280.0 nM 6.55
CHEMBL405070 — Ki = 320.0 nM 6.50
CHEMBL270595 — Ki = 320.0 nM 6.50
CHEMBL271722 — Ki = 320.0 nM 6.50
CHEMBL271226 — Ki = 320.0 nM 6.50
CHEMBL257911 — Ki = 330.0 nM 6.48
CHEMBL272988 — Ki = 340.0 nM 6.47
CHEMBL271492 — Ki = 340.0 nM 6.47
CHEMBL273002 — Ki = 340.0 nM 6.47
CHEMBL272307 — Ki = 370.0 nM 6.43
CHEMBL402415 — Ki = 440.0 nM 6.36
CHEMBL272951 — Ki > 320.0 nM -
CHEMBL272950 — Ki > 320.0 nM -
CHEMBL270807 — Ki > 320.0 nM -
CHEMBL405069 — Ki > 320.0 nM -
CHEMBL271504 — Ki > 320.0 nM -
CHEMBL429740 — Ki > 330.0 nM -
CHEMBL272131 — Ki > 320.0 nM -
CHEMBL404835 — Ki > 340.0 nM -