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Assay Detail

CHEMBL4711035

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

Binding
Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
22
Total Activities
22
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

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A dual-acting 5-HT receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties.
Canale V,Grychowska K,Kurczab R,Ryng M,Keeri AR,Satała G,Olejarz-Maciej A,Koczurkiewicz P,Drop M,Blicharz K,Piska K,Pękala E,Janiszewska P,Krawczyk M,Walczak M,Chaumont-Dubel S,Bojarski AJ,Marin P,Popik P,Zajdel P
Eur J Med Chem (2020) 208 : 112765 -112765
PubMed 32949963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.22 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370779 1 9.52
CHEMBL887 RASAGILINE 4.0 1 8.85
CHEMBL4784859 1 8.15
CHEMBL4741978 1 7.42
CHEMBL4742220 1 7.30
CHEMBL4780498 1 7.29
CHEMBL4761469 1 7.27
CHEMBL4754024 1 7.19
CHEMBL4757296 1 7.17
CHEMBL4780446 1 7.11
CHEMBL4793457 1 7.00
CHEMBL4794139 1 6.95
CHEMBL4780366 1 6.86
CHEMBL4778708 1 6.85
CHEMBL4792096 1 6.80
CHEMBL4777701 1 6.79
CHEMBL4786924 1 6.71
CHEMBL4754407 1 6.65
CHEMBL4796358 1 6.63
CHEMBL4745652 1 6.59
CHEMBL4750021 1 6.47
CHEMBL396778 SAFINAMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370779 Ki = 0.3 nM 9.52
CHEMBL887 RASAGILINE Ki = 1.4 nM 8.85
CHEMBL4784859 Ki = 7.0 nM 8.15
CHEMBL4741978 Ki = 38.0 nM 7.42
CHEMBL4742220 Ki = 50.0 nM 7.30
CHEMBL4780498 Ki = 51.0 nM 7.29
CHEMBL4761469 Ki = 54.0 nM 7.27
CHEMBL4754024 Ki = 65.0 nM 7.19
CHEMBL4757296 Ki = 68.0 nM 7.17
CHEMBL4780446 Ki = 77.0 nM 7.11
CHEMBL4793457 Ki = 100.0 nM 7.00
CHEMBL4794139 Ki = 113.0 nM 6.95
CHEMBL4780366 Ki = 137.0 nM 6.86
CHEMBL4778708 Ki = 140.0 nM 6.85
CHEMBL4792096 Ki = 158.0 nM 6.80
CHEMBL4777701 Ki = 162.0 nM 6.79
CHEMBL4786924 Ki = 195.0 nM 6.71
CHEMBL4754407 Ki = 223.0 nM 6.65
CHEMBL4796358 Ki = 232.0 nM 6.63
CHEMBL4745652 Ki = 259.0 nM 6.59
CHEMBL4750021 Ki = 340.0 nM 6.47
CHEMBL396778 SAFINAMIDE Ki - -