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Assay Detail

CHEMBL671418

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

Binding
In vitro binding affinity at human cloned dopamine receptor D2 (long) stably 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(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition.
van Hes R, Smid P, Stroomer CN, Tipker K, Tulp MT, van der Heyden JA, McCreary AC, Hesselink MB, Kruse CG.
Bioorg Med Chem Lett (2003) 13 : 405 -408
PubMed 12565939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.63 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.52
CHEMBL133524 1 8.30
CHEMBL336771 1 8.00
CHEMBL335844 1 7.92
CHEMBL131495 1 7.80
CHEMBL340220 1 7.70
CHEMBL129979 1 7.70
CHEMBL334956 1 7.70
CHEMBL338270 1 7.60
CHEMBL339098 1 7.60
CHEMBL335259 1 7.60
CHEMBL414433 1 7.60
CHEMBL130261 1 7.40
CHEMBL421902 1 7.40
CHEMBL423706 1 7.40
CHEMBL422618 1 7.40
CHEMBL129852 1 7.00
CHEMBL27811 1 6.70
CHEMBL276520 INDALPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 3.0 nM 8.52
CHEMBL133524 Ki = 5.0 nM 8.30
CHEMBL336771 Ki = 10.0 nM 8.00
CHEMBL335844 Ki = 12.0 nM 7.92
CHEMBL131495 Ki = 16.0 nM 7.80
CHEMBL340220 Ki = 20.0 nM 7.70
CHEMBL129979 Ki = 20.0 nM 7.70
CHEMBL334956 Ki = 20.0 nM 7.70
CHEMBL338270 Ki = 25.0 nM 7.60
CHEMBL339098 Ki = 25.0 nM 7.60
CHEMBL335259 Ki = 25.0 nM 7.60
CHEMBL414433 Ki = 25.0 nM 7.60
CHEMBL130261 Ki = 40.0 nM 7.40
CHEMBL421902 Ki = 40.0 nM 7.40
CHEMBL423706 Ki = 40.0 nM 7.40
CHEMBL422618 Ki = 40.0 nM 7.40
CHEMBL129852 Ki = 100.0 nM 7.00
CHEMBL27811 Ki = 200.0 nM 6.70
CHEMBL276520 INDALPINE Ki > 1000.0 nM -