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Assay Detail

CHEMBL675944

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Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
19
Total Activities
19
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(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Isoindolinone enantiomers having affinity for the dopamine D4 receptor.
Belliotti TR, Brink WA, Kesten SR, Rubin JR, Wustrow DJ, Zoski KT, Whetzel SZ, Corbin AE, Pugsley TA, Heffner TG, Wise LD.
Bioorg Med Chem Lett (1998) 8 : 1499 -1502
PubMed 9873377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.68 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267014 L-745870 1 9.04
CHEMBL37170 1 8.11
CHEMBL37885 1 8.07
CHEMBL38262 1 8.06
CHEMBL37604 1 8.03
CHEMBL37169 1 8.00
CHEMBL36313 1 7.96
CHEMBL287078 1 7.91
CHEMBL38349 1 7.68
CHEMBL37638 1 7.65
CHEMBL34239 1 7.61
CHEMBL290351 1 7.56
CHEMBL35182 1 7.46
CHEMBL37706 1 7.43
CHEMBL35093 1 7.38
CHEMBL285543 1 7.22
CHEMBL36337 1 7.11
CHEMBL38046 1 7.09
CHEMBL35114 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267014 L-745870 Ki = 0.91 nM 9.04
CHEMBL37170 Ki = 7.8 nM 8.11
CHEMBL37885 Ki = 8.6 nM 8.07
CHEMBL38262 Ki = 8.8 nM 8.06
CHEMBL37604 Ki = 9.3 nM 8.03
CHEMBL37169 Ki = 10.0 nM 8.00
CHEMBL36313 Ki = 11.0 nM 7.96
CHEMBL287078 Ki = 12.4 nM 7.91
CHEMBL38349 Ki = 20.8 nM 7.68
CHEMBL37638 Ki = 22.6 nM 7.65
CHEMBL34239 Ki = 24.5 nM 7.61
CHEMBL290351 Ki = 27.8 nM 7.56
CHEMBL35182 Ki = 35.1 nM 7.46
CHEMBL37706 Ki = 37.3 nM 7.43
CHEMBL35093 Ki = 42.0 nM 7.38
CHEMBL285543 Ki = 60.0 nM 7.22
CHEMBL36337 Ki = 78.6 nM 7.11
CHEMBL38046 Ki = 81.4 nM 7.09
CHEMBL35114 Ki = 333.0 nM 6.48