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Assay Detail

CHEMBL4032441

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

Binding
Displacement of [125I]ABN from human dopamine D2 long receptor expressed in HEK293 cell membranes after 60 mins by scintillation counting method
16
Total Activities
16
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

Highly Selective Dopamine D3 Receptor Antagonists with Arylated Diazaspiro Alkane Cores.
Reilly SW, Griffin S, Taylor M, Sahlholm K, Weng CC, Xu K, Jacome DA, Luedtke RR, Mach RH.
J Med Chem (2017) 60 : 9905 -9910
PubMed 29125762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 5.27 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267930 SPIPERONE 2.0 1 10.22
CHEMBL4083252 1 6.58
CHEMBL4062553 1 5.21
CHEMBL4076516 1 5.20
CHEMBL4101993 1 5.12
CHEMBL4073927 1 5.01
CHEMBL4084262 1 4.96
CHEMBL4077251 1 4.67
CHEMBL4092015 1 4.53
CHEMBL4071189 1 4.42
CHEMBL4076086 1 4.24
CHEMBL4089290 1 4.22
CHEMBL4076527 1 4.08
CHEMBL4098399 1 -
CHEMBL4079642 1 -
CHEMBL4100699 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267930 SPIPERONE Ki = 0.06 nM 10.22
CHEMBL4083252 Ki = 260.0 nM 6.58
CHEMBL4062553 Ki = 6168.0 nM 5.21
CHEMBL4076516 Ki = 6370.0 nM 5.20
CHEMBL4101993 Ki = 7501.0 nM 5.12
CHEMBL4073927 Ki = 9792.0 nM 5.01
CHEMBL4084262 Ki = 10895.0 nM 4.96
CHEMBL4077251 Ki = 21216.0 nM 4.67
CHEMBL4092015 Ki = 29300.0 nM 4.53
CHEMBL4071189 Ki = 37579.0 nM 4.42
CHEMBL4076086 Ki = 57101.0 nM 4.24
CHEMBL4089290 Ki = 60152.0 nM 4.22
CHEMBL4076527 Ki = 83671.0 nM 4.08
CHEMBL4098399 Ki > 109574.0 nM -
CHEMBL4079642 Ki = 114945.0 nM -
CHEMBL4100699 Ki = 104847.0 nM -