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Assay Detail

CHEMBL674413

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

Binding
In vitro displacement of [3H]spiperone from the cloned human dopamine receptor D3 stably expressed in CHO cells
28
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.
Einsiedel J, Thomas C, Hübner H, Gmeiner P.
Bioorg Med Chem Lett (2000) 10 : 2041 -2044
PubMed 10987445 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 6.09 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62602 1 7.19
CHEMBL2111527 1 7.12
CHEMBL2111525 1 7.08
CHEMBL267044 LEVOSULPIRIDE 2.0 1 7.06
CHEMBL64139 1 6.94
CHEMBL65641 1 6.92
CHEMBL62624 1 6.69
CHEMBL2111528 1 6.66
CHEMBL293225 1 6.24
CHEMBL293645 1 6.19
CHEMBL59749 2 6.18
CHEMBL64288 1 6.18
CHEMBL42 CLOZAPINE 4.0 1 6.02
CHEMBL64696 1 5.98
CHEMBL64668 1 5.92
CHEMBL64325 1 5.92
CHEMBL64566 1 5.89
CHEMBL64752 1 5.77
CHEMBL2111526 1 5.73
CHEMBL64376 1 5.69
CHEMBL302186 1 5.64
CHEMBL294780 1 5.40
CHEMBL64043 1 5.28
CHEMBL62601 1 5.23
CHEMBL59702 1 5.21
CHEMBL62996 1 5.12
CHEMBL62703 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62602 Ki = 65.0 nM 7.19
CHEMBL2111527 Ki = 75.0 nM 7.12
CHEMBL2111525 Ki = 83.0 nM 7.08
CHEMBL267044 LEVOSULPIRIDE Ki = 88.0 nM 7.06
CHEMBL64139 Ki = 115.0 nM 6.94
CHEMBL65641 Ki = 120.0 nM 6.92
CHEMBL62624 Ki = 205.0 nM 6.69
CHEMBL2111528 Ki = 220.0 nM 6.66
CHEMBL293225 Ki = 580.0 nM 6.24
CHEMBL293645 Ki = 640.0 nM 6.19
CHEMBL64288 Ki = 660.0 nM 6.18
CHEMBL59749 Ki = 660.0 nM 6.18
CHEMBL59749 Ki = 880.0 nM 6.06
CHEMBL42 CLOZAPINE Ki = 960.0 nM 6.02
CHEMBL64696 Ki = 1050.0 nM 5.98
CHEMBL64668 Ki = 1200.0 nM 5.92
CHEMBL64325 Ki = 1190.0 nM 5.92
CHEMBL64566 Ki = 1300.0 nM 5.89
CHEMBL64752 Ki = 1700.0 nM 5.77
CHEMBL2111526 Ki = 1850.0 nM 5.73
CHEMBL64376 Ki = 2050.0 nM 5.69
CHEMBL302186 Ki = 2300.0 nM 5.64
CHEMBL294780 Ki = 3950.0 nM 5.40
CHEMBL64043 Ki = 5250.0 nM 5.28
CHEMBL62601 Ki = 5850.0 nM 5.23
CHEMBL59702 Ki = 6100.0 nM 5.21
CHEMBL62996 Ki = 7600.0 nM 5.12
CHEMBL62703 Ki = 8400.0 nM 5.08