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Assay Detail

CHEMBL674990

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Binding
Binding affinity at Dopamine receptor D3 in CHO cells by radioligand displacement.
17
Total Activities
17
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

A series of 6- and 7-piperazinyl- and -piperidinylmethylbenzoxazinones with dopamine D4 antagonist activity: discovery of a potential atypical antipsychotic agent.
Belliotti TR, Wustrow DJ, Brink WA, Zoski KT, Shih YH, Whetzel SZ, Georgic LM, Corbin AE, Akunne HC, Heffner TG, Pugsley TA, Wise LD.
J Med Chem (1999) 42 : 5181 -5187
PubMed 10602703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.41 7.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL149233 1 7.98
CHEMBL151533 1 7.11
CHEMBL150173 1 6.68
CHEMBL151286 1 6.63
CHEMBL149497 1 6.37
CHEMBL346389 1 6.17
CHEMBL147130 1 6.08
CHEMBL147059 1 6.07
CHEMBL150181 1 6.06
CHEMBL150129 1 5.75
CHEMBL345552 1 5.60
CHEMBL346398 1 -
CHEMBL348435 1 -
CHEMBL147011 1 -
CHEMBL146757 1 -
CHEMBL267014 L-745870 1 -
CHEMBL149596 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL149233 Ki = 10.4 nM 7.98
CHEMBL151533 Ki = 78.5 nM 7.11
CHEMBL150173 Ki = 208.0 nM 6.68
CHEMBL151286 Ki = 232.0 nM 6.63
CHEMBL149497 Ki = 428.0 nM 6.37
CHEMBL346389 Ki = 679.0 nM 6.17
CHEMBL147130 Ki = 839.0 nM 6.08
CHEMBL147059 Ki = 859.0 nM 6.07
CHEMBL150181 Ki = 864.0 nM 6.06
CHEMBL150129 Ki = 1790.0 nM 5.75
CHEMBL345552 Ki = 2490.0 nM 5.60
CHEMBL346398 Ki > 3030.0 nM -
CHEMBL348435 Ki > 3030.0 nM -
CHEMBL147011 Ki > 3030.0 nM -
CHEMBL146757 Ki > 3030.0 nM -
CHEMBL267014 L-745870 Ki > 3030.0 nM -
CHEMBL149596 Ki > 3030.0 nM -