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Assay Detail

CHEMBL697541

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Binding
Binding affinity towards rat cortical H3 receptor
48
Total Activities
48
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

Synthesis and SAR of aminoalkoxy-biaryl-4-carboxamides: novel and selective histamine H3 receptor antagonists.
Faghih R, Dwight W, Pan JB, Fox GB, Krueger KM, Esbenshade TA, McVey JM, Marsh K, Bennani YL, Hancock AA.
Bioorg Med Chem Lett (2003) 13 : 1325 -1328
PubMed 12657274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 7.73 9.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278462 CIPRALISANT 2.0 1 9.71
CHEMBL280590 1 8.99
CHEMBL27979 A-349,821 1 8.78
CHEMBL283313 1 8.69
CHEMBL433031 1 8.55
CHEMBL25519 1 8.55
CHEMBL24863 1 8.53
CHEMBL25205 1 8.44
CHEMBL25342 1 8.42
CHEMBL27933 1 8.38
CHEMBL27501 1 8.29
CHEMBL26880 1 8.18
CHEMBL279463 1 8.14
CHEMBL25685 1 8.08
CHEMBL27209 1 8.06
CHEMBL27697 1 8.05
CHEMBL281640 1 8.04
CHEMBL27444 1 7.99
CHEMBL27665 1 7.89
CHEMBL282903 1 7.86
CHEMBL24468 1 7.79
CHEMBL436340 1 7.76
CHEMBL2113223 1 7.73
CHEMBL27115 1 7.68
CHEMBL27835 1 7.67
CHEMBL25501 1 7.59
CHEMBL2113222 1 7.56
CHEMBL280895 1 7.55
CHEMBL282685 1 7.54
CHEMBL2113224 1 7.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278462 CIPRALISANT Ki = 0.195 nM 9.71
CHEMBL280590 Ki = 1.023 nM 8.99
CHEMBL27979 A-349,821 Ki = 1.66 nM 8.78
CHEMBL283313 Ki = 2.042 nM 8.69
CHEMBL433031 Ki = 2.818 nM 8.55
CHEMBL25519 Ki = 2.818 nM 8.55
CHEMBL24863 Ki = 2.951 nM 8.53
CHEMBL25205 Ki = 3.631 nM 8.44
CHEMBL25342 Ki = 3.802 nM 8.42
CHEMBL27933 Ki = 4.169 nM 8.38
CHEMBL27501 Ki = 5.129 nM 8.29
CHEMBL26880 Ki = 6.607 nM 8.18
CHEMBL279463 Ki = 7.244 nM 8.14
CHEMBL25685 Ki = 8.318 nM 8.08
CHEMBL27209 Ki = 8.71 nM 8.06
CHEMBL27697 Ki = 8.913 nM 8.05
CHEMBL281640 Ki = 9.12 nM 8.04
CHEMBL27444 Ki = 10.23 nM 7.99
CHEMBL27665 Ki = 12.88 nM 7.89
CHEMBL282903 Ki = 13.8 nM 7.86
CHEMBL24468 Ki = 16.22 nM 7.79
CHEMBL436340 Ki = 17.38 nM 7.76
CHEMBL2113223 Ki = 18.62 nM 7.73
CHEMBL27115 Ki = 20.89 nM 7.68
CHEMBL27835 Ki = 21.38 nM 7.67
CHEMBL25501 Ki = 25.7 nM 7.59
CHEMBL2113222 Ki = 27.54 nM 7.56
CHEMBL280895 Ki = 28.18 nM 7.55
CHEMBL282685 Ki = 28.84 nM 7.54
CHEMBL2113224 Ki = 29.51 nM 7.53
CHEMBL24865 Ki = 30.9 nM 7.51
CHEMBL24198 Ki = 32.36 nM 7.49
CHEMBL27339 Ki = 33.11 nM 7.48
CHEMBL25688 Ki = 41.69 nM 7.38
CHEMBL282062 Ki = 42.66 nM 7.37
CHEMBL24921 Ki = 42.66 nM 7.37
CHEMBL24847 Ki = 52.48 nM 7.28
CHEMBL282016 Ki = 57.54 nM 7.24
CHEMBL27545 Ki = 70.79 nM 7.15
CHEMBL24352 Ki = 97.72 nM 7.01
CHEMBL28271 Ki = 112.2 nM 6.95
CHEMBL25126 Ki = 114.82 nM 6.94
CHEMBL24126 Ki = 128.82 nM 6.89
CHEMBL27343 Ki = 134.9 nM 6.87
CHEMBL281287 Ki = 177.83 nM 6.75
CHEMBL25290 Ki = 218.78 nM 6.66
CHEMBL284320 Ki = 407.38 nM 6.39
CHEMBL283451 Ki = 478.63 nM 6.32