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Assay Detail

CHEMBL4819274

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

Binding
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cells incubated for 1 hr by microbeta counting method
21
Total Activities
21
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

Chlorine substituents and linker topology as factors of 5-HT<sub>6</sub>R activity for novel highly active 1,3,5-triazine derivatives with procognitive properties in vivo.
Sudoł S, Kucwaj-Brysz K, Kurczab R, Wilczyńska N, Jastrzębska-Więsek M, Satała G, Latacz G, Głuch-Lutwin M, Mordyl B, Żesławska E, Nitek W, Partyka A, Buzun K, Doroz-Płonka A, Wesołowska A, Bielawska A, Handzlik J.
Eur J Med Chem (2020) 203 : 112529 -112529
PubMed 32693296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.40 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4860275 1 8.22
CHEMBL4873623 1 8.22
CHEMBL715 OLANZAPINE 4.0 1 8.15
CHEMBL4876727 1 7.96
CHEMBL4858771 1 7.92
CHEMBL4846146 1 7.89
CHEMBL4855393 1 7.80
CHEMBL4864863 1 7.77
CHEMBL4847379 1 7.68
CHEMBL4869411 1 7.64
CHEMBL4447416 1 7.64
CHEMBL4864448 1 7.58
CHEMBL4860006 1 7.57
CHEMBL4849077 1 7.29
CHEMBL4873127 1 7.14
CHEMBL4857676 1 7.07
CHEMBL4861431 1 7.02
CHEMBL4860719 1 6.56
CHEMBL4849230 1 6.33
CHEMBL4867534 1 6.00
CHEMBL4868911 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4860275 Ki = 6.0 nM 8.22
CHEMBL4873623 Ki = 6.0 nM 8.22
CHEMBL715 OLANZAPINE Ki = 7.0 nM 8.15
CHEMBL4876727 Ki = 11.0 nM 7.96
CHEMBL4858771 Ki = 12.0 nM 7.92
CHEMBL4846146 Ki = 13.0 nM 7.89
CHEMBL4855393 Ki = 16.0 nM 7.80
CHEMBL4864863 Ki = 17.0 nM 7.77
CHEMBL4847379 Ki = 21.0 nM 7.68
CHEMBL4869411 Ki = 23.0 nM 7.64
CHEMBL4447416 Ki = 23.0 nM 7.64
CHEMBL4864448 Ki = 26.0 nM 7.58
CHEMBL4860006 Ki = 27.0 nM 7.57
CHEMBL4849077 Ki = 51.0 nM 7.29
CHEMBL4873127 Ki = 73.0 nM 7.14
CHEMBL4857676 Ki = 86.0 nM 7.07
CHEMBL4861431 Ki = 95.0 nM 7.02
CHEMBL4860719 Ki = 274.0 nM 6.56
CHEMBL4849230 Ki = 470.0 nM 6.33
CHEMBL4867534 Ki = 999.0 nM 6.00
CHEMBL4868911 Ki = 1061.0 nM 5.97