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Assay Detail

CHEMBL692572

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Binding
Binding affinity for human recombinant 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 (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

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 8.22 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27979 A-349,821 1 9.31
CHEMBL24863 1 9.22
CHEMBL27501 1 9.16
CHEMBL283313 1 9.11
CHEMBL280590 1 9.11
CHEMBL25519 1 9.07
CHEMBL27933 1 9.01
CHEMBL26880 1 8.95
CHEMBL25342 1 8.68
CHEMBL279463 1 8.67
CHEMBL278462 CIPRALISANT 2.0 1 8.67
CHEMBL27697 1 8.62
CHEMBL2113223 1 8.54
CHEMBL27665 1 8.52
CHEMBL25685 1 8.46
CHEMBL27444 1 8.44
CHEMBL433031 1 8.43
CHEMBL2113224 1 8.41
CHEMBL436340 1 8.36
CHEMBL25205 1 8.33
CHEMBL281640 1 8.32
CHEMBL282903 1 8.29
CHEMBL2113222 1 8.26
CHEMBL24468 1 8.21
CHEMBL24198 1 8.21
CHEMBL27835 1 8.19
CHEMBL27339 1 8.19
CHEMBL24865 1 8.16
CHEMBL280895 1 8.16
CHEMBL27209 1 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27979 A-349,821 Ki = 0.4898 nM 9.31
CHEMBL24863 Ki = 0.6026 nM 9.22
CHEMBL27501 Ki = 0.6918 nM 9.16
CHEMBL283313 Ki = 0.7762 nM 9.11
CHEMBL280590 Ki = 0.7762 nM 9.11
CHEMBL25519 Ki = 0.8511 nM 9.07
CHEMBL27933 Ki = 0.9772 nM 9.01
CHEMBL26880 Ki = 1.122 nM 8.95
CHEMBL25342 Ki = 2.089 nM 8.68
CHEMBL279463 Ki = 2.138 nM 8.67
CHEMBL278462 CIPRALISANT Ki = 2.138 nM 8.67
CHEMBL27697 Ki = 2.399 nM 8.62
CHEMBL2113223 Ki = 2.884 nM 8.54
CHEMBL27665 Ki = 3.02 nM 8.52
CHEMBL25685 Ki = 3.467 nM 8.46
CHEMBL27444 Ki = 3.631 nM 8.44
CHEMBL433031 Ki = 3.715 nM 8.43
CHEMBL2113224 Ki = 3.89 nM 8.41
CHEMBL436340 Ki = 4.365 nM 8.36
CHEMBL25205 Ki = 4.677 nM 8.33
CHEMBL281640 Ki = 4.786 nM 8.32
CHEMBL282903 Ki = 5.129 nM 8.29
CHEMBL2113222 Ki = 5.495 nM 8.26
CHEMBL24198 Ki = 6.166 nM 8.21
CHEMBL24468 Ki = 6.166 nM 8.21
CHEMBL27835 Ki = 6.457 nM 8.19
CHEMBL27339 Ki = 6.457 nM 8.19
CHEMBL24865 Ki = 6.918 nM 8.16
CHEMBL280895 Ki = 6.918 nM 8.16
CHEMBL27209 Ki = 7.244 nM 8.14
CHEMBL25688 Ki = 7.244 nM 8.14
CHEMBL282685 Ki = 8.128 nM 8.09
CHEMBL282062 Ki = 8.128 nM 8.09
CHEMBL25501 Ki = 8.318 nM 8.08
CHEMBL24921 Ki = 9.772 nM 8.01
CHEMBL27115 Ki = 10.72 nM 7.97
CHEMBL282016 Ki = 11.22 nM 7.95
CHEMBL24352 Ki = 16.22 nM 7.79
CHEMBL24847 Ki = 18.2 nM 7.74
CHEMBL27545 Ki = 23.44 nM 7.63
CHEMBL28271 Ki = 24.55 nM 7.61
CHEMBL24126 Ki = 32.36 nM 7.49
CHEMBL25126 Ki = 37.15 nM 7.43
CHEMBL27343 Ki = 38.9 nM 7.41
CHEMBL281287 Ki = 40.74 nM 7.39
CHEMBL284320 Ki = 109.65 nM 6.96
CHEMBL283451 Ki = 181.97 nM 6.74
CHEMBL25290 Ki = 229.09 nM 6.64