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Assay Detail

CHEMBL4701477

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Binding
Binding affinity to at human H3 receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H receptor and cancer resistance proteins.
Szczepańska K,Kincses A,Vincze K,Szymańska E,Latacz G,Kuder KJ,Stark H,Spengler G,Handzlik J,Kieć-Kononowicz K
Bioorg Med Chem Lett (2020) 30 : 127522 -127522
PubMed 32871268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 5.88 7.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4547780 1 7.99
CHEMBL4581913 1 6.50
CHEMBL4170784 1 6.17
CHEMBL4166945 1 6.05
CHEMBL4473431 1 6.04
CHEMBL4467220 1 5.91
CHEMBL4445569 1 5.76
CHEMBL4162840 1 5.64
CHEMBL4519189 1 5.63
CHEMBL4163913 1 5.53
CHEMBL4170350 1 5.47
CHEMBL4453108 1 5.47
CHEMBL4452580 1 5.43
CHEMBL4166262 1 5.42
CHEMBL4159046 1 5.26
CHEMBL4171151 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4547780 Ki = 10.2 nM 7.99
CHEMBL4581913 Ki = 315.0 nM 6.50
CHEMBL4170784 Ki = 683.0 nM 6.17
CHEMBL4166945 Ki = 883.0 nM 6.05
CHEMBL4473431 Ki = 908.0 nM 6.04
CHEMBL4467220 Ki = 1230.0 nM 5.91
CHEMBL4445569 Ki = 1720.0 nM 5.76
CHEMBL4162840 Ki = 2264.0 nM 5.64
CHEMBL4519189 Ki = 2316.0 nM 5.63
CHEMBL4163913 Ki = 2957.0 nM 5.53
CHEMBL4170350 Ki = 3420.0 nM 5.47
CHEMBL4453108 Ki = 3390.0 nM 5.47
CHEMBL4452580 Ki = 3697.0 nM 5.43
CHEMBL4166262 Ki = 3827.0 nM 5.42
CHEMBL4159046 Ki = 5477.0 nM 5.26
CHEMBL4171151 Ki > 10000.0 nM -