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Assay Detail

CHEMBL3762401

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

Binding
Displacement of [3H]-spiperone from human dopamine D2S receptor expressed in HEK293 cell membranes
23
Total Activities
23
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

Improving selectivity of dopamine D3 receptor ligands.
Capet M, Calmels T, Levoin N, Danvy D, Berrebi-Bertrand I, Stark H, Schwartz JC, Lecomte JM.
Bioorg Med Chem Lett (2016) 26 : 885 -888
PubMed 26723530 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.45 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3758991 1 7.89
CHEMBL3758368 1 7.47
CHEMBL3759441 1 7.28
CHEMBL3758610 1 7.26
CHEMBL3759865 1 7.02
CHEMBL3760110 1 6.88
CHEMBL26962 1 6.78
CHEMBL25236 BP-897 1 6.73
CHEMBL218203 1 6.62
CHEMBL3758741 1 6.52
CHEMBL3759607 1 6.51
CHEMBL3758913 1 6.49
CHEMBL3759491 1 6.43
CHEMBL3758881 1 6.39
CHEMBL3760063 1 6.32
CHEMBL3758665 1 6.04
CHEMBL154508 1 5.94
CHEMBL3759312 1 5.81
CHEMBL3758711 1 5.81
CHEMBL3759513 1 5.48
CHEMBL3758330 1 5.30
CHEMBL3758920 1 4.92
CHEMBL3758403 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3758991 Ki = 13.0 nM 7.89
CHEMBL3758368 Ki = 34.0 nM 7.47
CHEMBL3759441 Ki = 52.0 nM 7.28
CHEMBL3758610 Ki = 55.0 nM 7.26
CHEMBL3759865 Ki = 95.0 nM 7.02
CHEMBL3760110 Ki = 131.0 nM 6.88
CHEMBL26962 Ki = 168.0 nM 6.78
CHEMBL25236 BP-897 Ki = 186.0 nM 6.73
CHEMBL218203 Ki = 238.0 nM 6.62
CHEMBL3758741 Ki = 302.0 nM 6.52
CHEMBL3759607 Ki = 310.0 nM 6.51
CHEMBL3758913 Ki = 322.0 nM 6.49
CHEMBL3759491 Ki = 373.0 nM 6.43
CHEMBL3758881 Ki = 404.0 nM 6.39
CHEMBL3760063 Ki = 482.0 nM 6.32
CHEMBL3758665 Ki = 911.0 nM 6.04
CHEMBL154508 Ki = 1149.0 nM 5.94
CHEMBL3759312 Ki = 1549.0 nM 5.81
CHEMBL3758711 Ki = 1553.0 nM 5.81
CHEMBL3759513 Ki = 3323.0 nM 5.48
CHEMBL3758330 Ki = 5031.0 nM 5.30
CHEMBL3758920 Ki = 12143.0 nM 4.92
CHEMBL3758403 Ki - -