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Assay Detail

CHEMBL4819277

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

Binding
Displacement of [3H]-raclopride from human D2L receptor expressed in HEK293 cells measured after 1 hr by microbeta counting method
20
Total Activities
20
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

D(2) dopamine receptor (CHEMBL217)
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 20 6.49 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL715 OLANZAPINE 4.0 1 8.05
CHEMBL4864863 1 6.99
CHEMBL4860006 1 6.80
CHEMBL4860719 1 6.69
CHEMBL4858771 1 6.64
CHEMBL4849077 1 6.57
CHEMBL4860275 1 6.50
CHEMBL4868911 1 6.45
CHEMBL4876727 1 6.43
CHEMBL4846146 1 6.43
CHEMBL4864448 1 6.42
CHEMBL4873623 1 6.38
CHEMBL4849230 1 6.38
CHEMBL4855393 1 6.37
CHEMBL4873127 1 6.30
CHEMBL4869411 1 6.30
CHEMBL4857676 1 6.24
CHEMBL4861431 1 6.12
CHEMBL4447416 1 6.00
CHEMBL4847379 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL715 OLANZAPINE Ki = 9.0 nM 8.05
CHEMBL4864863 Ki = 103.0 nM 6.99
CHEMBL4860006 Ki = 157.0 nM 6.80
CHEMBL4860719 Ki = 206.0 nM 6.69
CHEMBL4858771 Ki = 229.0 nM 6.64
CHEMBL4849077 Ki = 270.0 nM 6.57
CHEMBL4860275 Ki = 320.0 nM 6.50
CHEMBL4868911 Ki = 356.0 nM 6.45
CHEMBL4876727 Ki = 368.0 nM 6.43
CHEMBL4846146 Ki = 375.0 nM 6.43
CHEMBL4864448 Ki = 377.0 nM 6.42
CHEMBL4873623 Ki = 421.0 nM 6.38
CHEMBL4849230 Ki = 413.0 nM 6.38
CHEMBL4855393 Ki = 432.0 nM 6.37
CHEMBL4873127 Ki = 506.0 nM 6.30
CHEMBL4869411 Ki = 495.0 nM 6.30
CHEMBL4857676 Ki = 580.0 nM 6.24
CHEMBL4861431 Ki = 754.0 nM 6.12
CHEMBL4447416 Ki = 1001.0 nM 6.00
CHEMBL4847379 Ki = 1506.0 nM 5.82