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Assay Detail

CHEMBL4154392

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]Nalpha-methylhistamine from recombinant human H3 receptor expressed in HEK293 cells after 90 mins by liquid scintillation counting method
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands.
Szczepańska K, Karcz T, Mogilski S, Siwek A, Kuder KJ, Latacz G, Kubacka M, Hagenow S, Lubelska A, Olejarz A, Kotańska M, Sadek B, Stark H, Kieć-Kononowicz K.
Eur J Med Chem (2018) 152 : 223 -234
PubMed 29723785 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.13 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4173079 1 8.08
CHEMBL4173854 1 7.80
CHEMBL4159018 1 7.66
CHEMBL4165880 1 7.51
CHEMBL4162433 1 7.42
CHEMBL4160557 1 6.92
CHEMBL4163949 1 6.32
CHEMBL4170784 1 6.17
CHEMBL4166945 1 6.05
CHEMBL4162840 1 5.64
CHEMBL4163913 1 5.53
CHEMBL4170350 1 5.47
CHEMBL4173801 1 5.44
CHEMBL4166262 1 5.42
CHEMBL4165061 1 5.28
CHEMBL4175250 1 5.27
CHEMBL4159046 1 5.26
CHEMBL4167380 1 5.21
CHEMBL4163474 1 5.09
CHEMBL4174172 1 5.06
CHEMBL4159479 1 -
CHEMBL4171151 1 -
CHEMBL4174596 1 -
CHEMBL4175362 1 -
CHEMBL4174564 1 -
CHEMBL4161040 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4173079 Ki = 8.4 nM 8.08
CHEMBL4173854 Ki = 16.0 nM 7.80
CHEMBL4159018 Ki = 22.0 nM 7.66
CHEMBL4165880 Ki = 30.6 nM 7.51
CHEMBL4162433 Ki = 37.8 nM 7.42
CHEMBL4160557 Ki = 120.0 nM 6.92
CHEMBL4163949 Ki = 482.0 nM 6.32
CHEMBL4170784 Ki = 683.0 nM 6.17
CHEMBL4166945 Ki = 883.0 nM 6.05
CHEMBL4162840 Ki = 2264.0 nM 5.64
CHEMBL4163913 Ki = 2957.0 nM 5.53
CHEMBL4170350 Ki = 3420.0 nM 5.47
CHEMBL4173801 Ki = 3654.0 nM 5.44
CHEMBL4166262 Ki = 3827.0 nM 5.42
CHEMBL4165061 Ki = 5196.0 nM 5.28
CHEMBL4175250 Ki = 5405.0 nM 5.27
CHEMBL4159046 Ki = 5477.0 nM 5.26
CHEMBL4167380 Ki = 6212.0 nM 5.21
CHEMBL4163474 Ki = 8156.0 nM 5.09
CHEMBL4174172 Ki = 8740.0 nM 5.06
CHEMBL4159479 Ki > 10000.0 nM -
CHEMBL4171151 Ki > 10000.0 nM -
CHEMBL4174596 Ki > 10000.0 nM -
CHEMBL4175362 Ki > 10000.0 nM -
CHEMBL4174564 Ki > 10000.0 nM -
CHEMBL4161040 Ki > 10000.0 nM -