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Assay Detail

CHEMBL4771176

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

ADMET
Displacement of [3H]-Raclopride from human D2 receptor (unknown origin) expressed in HEK293 cell membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
Nizi MG,Desantis J,Nakatani Y,Massari S,Mazzarella MA,Shetye G,Sabatini S,Barreca ML,Manfroni G,Felicetti T,Rushton-Green R,Hards K,Latacz G,Satała G,Bojarski AJ,Cecchetti V,Kolář MH,Handzlik J,Cook GM,Franzblau SG,Tabarrini O
Eur J Med Chem (2020) 201 : 112420 -112420
PubMed 32526553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.72 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479 THIORIDAZINE 4.0 1 8.10
CHEMBL4778666 1 6.43
CHEMBL4797066 1 6.19
CHEMBL4791959 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479 THIORIDAZINE Ki = 8.0 nM 8.10
CHEMBL4778666 Ki = 367.0 nM 6.43
CHEMBL4797066 Ki = 639.0 nM 6.19
CHEMBL4791959 Ki = 688.0 nM 6.16