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Assay Detail

CHEMBL3591126

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

Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
33
Total Activities
33
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(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Using click chemistry toward novel 1,2,3-triazole-linked dopamine D3 receptor ligands.
Keck TM, Banala AK, Slack RD, Burzynski C, Bonifazi A, Okunola-Bakare OM, Moore M, Deschamps JR, Rais R, Slusher BS, Newman AH.
Bioorg Med Chem (2015) 23 : 4000 -4012
PubMed 25650314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 6.23 6.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3588981 1 6.65
CHEMBL3588920 1 6.63
CHEMBL3588982 1 6.57
CHEMBL3588913 1 6.52
CHEMBL3588914 1 6.48
CHEMBL3588915 1 6.45
CHEMBL3588983 1 6.37
CHEMBL2430443 1 6.32
CHEMBL3353895 1 6.31
CHEMBL3588919 1 6.29
CHEMBL3588921 1 6.23
CHEMBL1627305 1 5.58
CHEMBL3589652 1 5.43
CHEMBL3588918 1 5.35
CHEMBL3588987 1 -
CHEMBL3588988 1 -
CHEMBL3588989 1 -
CHEMBL3588990 1 -
CHEMBL3588991 1 -
CHEMBL3588992 1 -
CHEMBL3588994 1 -
CHEMBL3588995 1 -
CHEMBL3588996 1 -
CHEMBL3588997 1 -
CHEMBL3588998 1 -
CHEMBL3589650 1 -
CHEMBL3588917 1 -
CHEMBL3589651 1 -
CHEMBL3588916 1 -
CHEMBL3588993 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3588981 Ki = 222.0 nM 6.65
CHEMBL3588920 Ki = 232.0 nM 6.63
CHEMBL3588982 Ki = 269.0 nM 6.57
CHEMBL3588913 Ki = 299.0 nM 6.52
CHEMBL3588914 Ki = 329.0 nM 6.48
CHEMBL3588915 Ki = 353.0 nM 6.45
CHEMBL3588983 Ki = 425.0 nM 6.37
CHEMBL2430443 Ki = 480.0 nM 6.32
CHEMBL3353895 Ki = 486.0 nM 6.31
CHEMBL3588919 Ki = 510.0 nM 6.29
CHEMBL3588921 Ki = 588.0 nM 6.23
CHEMBL1627305 Ki = 2600.0 nM 5.58
CHEMBL3589652 Ki = 3670.0 nM 5.43
CHEMBL3588918 Ki = 4450.0 nM 5.35
CHEMBL3588984 Ki > 1000.0 nM -
CHEMBL3588985 Ki > 20000.0 nM -
CHEMBL3588986 Ki > 2000.0 nM -
CHEMBL3588987 Ki > 1000.0 nM -
CHEMBL3588988 Ki > 10000.0 nM -
CHEMBL3588989 Ki > 2000.0 nM -
CHEMBL3588990 Ki > 2000.0 nM -
CHEMBL3588991 Ki > 3000.0 nM -
CHEMBL3588992 Ki > 3000.0 nM -
CHEMBL3588994 Ki > 3000.0 nM -
CHEMBL3588995 Ki > 20000.0 nM -
CHEMBL3588996 Ki > 7000.0 nM -
CHEMBL3588997 Ki - -
CHEMBL3588998 Ki - -
CHEMBL3589650 Ki - -
CHEMBL3588917 Ki > 2000.0 nM -
CHEMBL3589651 Ki - -
CHEMBL3588916 Ki > 1000.0 nM -
CHEMBL3588993 Ki > 1000.0 nM -