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Assay Detail

CHEMBL4709934

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

Binding
Displacement of [3H]N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cells by microbeta scintillation analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Rational design of new multitarget histamine H receptor ligands as potential candidates for treatment of Alzheimer's disease.
Łażewska D,Bajda M,Kaleta M,Zaręba P,Doroz-Płonka A,Siwek A,Alachkar A,Mogilski S,Saad A,Kuder K,Olejarz-Maciej A,Godyń J,Stary D,Sudoł S,Więcek M,Latacz G,Walczak M,Handzlik J,Sadek B,Malawska B,Kieć-Kononowicz K
Eur J Med Chem (2020) 207 : 112743 -112743
PubMed 32882609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.68 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462605 PITOLISANT 4.0 1 7.52
CHEMBL4757387 1 7.25
CHEMBL4789324 1 7.07
CHEMBL4777210 1 7.01
CHEMBL4783624 1 7.00
CHEMBL4796334 1 7.00
CHEMBL4797681 1 6.96
CHEMBL4786252 1 6.85
CHEMBL4784081 1 6.83
CHEMBL4798732 1 6.82
CHEMBL4759463 1 6.81
CHEMBL4797355 1 6.77
CHEMBL4750579 1 6.76
CHEMBL4797867 1 6.69
CHEMBL4747044 1 6.62
CHEMBL4785098 1 6.55
CHEMBL4790939 1 6.36
CHEMBL4784025 1 6.35
CHEMBL4784501 1 6.33
CHEMBL4744451 1 6.30
CHEMBL4741039 1 6.28
CHEMBL4746282 1 6.22
CHEMBL4794003 1 5.97
CHEMBL4793206 1 5.96
CHEMBL887 RASAGILINE 4.0 1 -
CHEMBL396778 SAFINAMIDE 4.0 1 -
CHEMBL8706 CLORGILINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462605 PITOLISANT Ki = 30.0 nM 7.52
CHEMBL4757387 Ki = 56.0 nM 7.25
CHEMBL4789324 Ki = 86.0 nM 7.07
CHEMBL4777210 Ki = 97.0 nM 7.01
CHEMBL4783624 Ki = 100.0 nM 7.00
CHEMBL4796334 Ki = 100.0 nM 7.00
CHEMBL4797681 Ki = 110.0 nM 6.96
CHEMBL4786252 Ki = 140.0 nM 6.85
CHEMBL4784081 Ki = 148.0 nM 6.83
CHEMBL4798732 Ki = 150.0 nM 6.82
CHEMBL4759463 Ki = 156.0 nM 6.81
CHEMBL4797355 Ki = 170.0 nM 6.77
CHEMBL4750579 Ki = 172.0 nM 6.76
CHEMBL4797867 Ki = 203.0 nM 6.69
CHEMBL4747044 Ki = 238.0 nM 6.62
CHEMBL4785098 Ki = 282.0 nM 6.55
CHEMBL4790939 Ki = 436.0 nM 6.36
CHEMBL4784025 Ki = 448.0 nM 6.35
CHEMBL4784501 Ki = 465.0 nM 6.33
CHEMBL4744451 Ki = 496.0 nM 6.30
CHEMBL4741039 Ki = 520.0 nM 6.28
CHEMBL4746282 Ki = 602.0 nM 6.22
CHEMBL4794003 Ki = 1060.0 nM 5.97
CHEMBL4793206 Ki = 1105.0 nM 5.96
CHEMBL887 RASAGILINE Ki - -
CHEMBL396778 SAFINAMIDE Ki - -
CHEMBL8706 CLORGILINE Ki - -