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Assay Detail

CHEMBL671406

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

Binding
In vitro ability to inhibit the binding of [3H]spiperone to dopamine receptor D2 in rat striatal membranes.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Potential antipsychotic agents 5. Synthesis and antidopaminergic properties of substituted 5,6-dimethoxysalicylamides and related compounds.
Högberg T, Bengtsson S, de Paulis T, Johansson L, Ström P, Hall H, Ogren SO.
J Med Chem (1990) 33 : 1155 -1163
PubMed 1969484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.48 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1907702 1 9.11
CHEMBL8946 ETICLOPRIDE 2.0 1 9.04
CHEMBL76402 1 8.85
CHEMBL1907692 1 8.77
CHEMBL3085403 1 8.72
CHEMBL1907700 1 8.64
CHEMBL1907695 1 8.62
CHEMBL305916 1 8.06
CHEMBL54 HALOPERIDOL 4.0 1 7.92
CHEMBL283099 1 7.92
CHEMBL1907697 1 7.72
CHEMBL1907693 1 7.68
CHEMBL8809 RACLOPRIDE 2.0 1 7.50
CHEMBL3085402 1 7.48
CHEMBL1907694 1 7.36
CHEMBL1907691 1 7.25
CHEMBL1907690 1 7.17
CHEMBL1907698 1 7.15
CHEMBL1907915 1 7.10
CHEMBL1907696 1 6.69
CHEMBL267044 LEVOSULPIRIDE 2.0 1 6.68
CHEMBL1907701 1 6.38
CHEMBL16252 1 6.09
CHEMBL1907699 1 5.76
CHEMBL1907703 1 5.53
CHEMBL1907914 1 5.21
CHEMBL416352 1 -
CHEMBL1907913 1 -
CHEMBL16135 1 -
CHEMBL1202419 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1907702 IC50 = 0.77 nM 9.11
CHEMBL8946 ETICLOPRIDE IC50 = 0.92 nM 9.04
CHEMBL76402 IC50 = 1.4 nM 8.85
CHEMBL1907692 IC50 = 1.7 nM 8.77
CHEMBL3085403 IC50 = 1.9 nM 8.72
CHEMBL1907700 IC50 = 2.3 nM 8.64
CHEMBL1907695 IC50 = 2.4 nM 8.62
CHEMBL305916 IC50 = 8.8 nM 8.06
CHEMBL54 HALOPERIDOL IC50 = 12.0 nM 7.92
CHEMBL283099 IC50 = 12.0 nM 7.92
CHEMBL1907697 IC50 = 19.0 nM 7.72
CHEMBL1907693 IC50 = 21.0 nM 7.68
CHEMBL8809 RACLOPRIDE IC50 = 32.0 nM 7.50
CHEMBL3085402 IC50 = 33.0 nM 7.48
CHEMBL1907694 IC50 = 44.0 nM 7.36
CHEMBL1907691 IC50 = 56.0 nM 7.25
CHEMBL1907690 IC50 = 67.0 nM 7.17
CHEMBL1907698 IC50 = 71.0 nM 7.15
CHEMBL1907915 IC50 = 79.0 nM 7.10
CHEMBL1907696 IC50 = 205.0 nM 6.69
CHEMBL267044 LEVOSULPIRIDE IC50 = 210.0 nM 6.68
CHEMBL1907701 IC50 = 420.0 nM 6.38
CHEMBL16252 IC50 = 820.0 nM 6.09
CHEMBL1907699 IC50 = 1750.0 nM 5.76
CHEMBL1907703 IC50 = 2960.0 nM 5.53
CHEMBL1907914 IC50 = 6170.0 nM 5.21
CHEMBL416352 IC50 - nM -
CHEMBL1907913 IC50 - nM -
CHEMBL16135 IC50 - nM -
CHEMBL1202419 IC50 - nM -
CHEMBL16160 IC50 - nM -
CHEMBL416355 IC50 - nM -