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Assay Detail

CHEMBL670668

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

Binding
In vitro binding affinity at Dopamine receptor D2 in rat by displacing [3H]- spiperone from rat striatal membrane
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
de Paulis T, Kumar Y, Johansson L, Rämsby S, Florvall L, Hall H, Angeby-Möller K, Ogren SO.
J Med Chem (1985) 28 : 1263 -1269
PubMed 4040977 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.80 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267723 IOLOPRIDE 2.0 1 8.47
CHEMBL23403 1 8.33
CHEMBL22472 1 8.32
CHEMBL23437 1 8.20
CHEMBL54 HALOPERIDOL 4.0 1 7.92
CHEMBL283099 2 7.92
CHEMBL23228 1 7.72
CHEMBL268555 1 7.58
CHEMBL23845 1 7.41
CHEMBL23519 1 7.25
CHEMBL278767 1 7.19
CHEMBL431490 1 6.91
CHEMBL280953 1 6.82
CHEMBL26 SULPIRIDE 3.0 1 6.63
CHEMBL8945 1 6.50
CHEMBL276977 1 6.44
CHEMBL282925 1 6.04
CHEMBL278560 1 6.01
CHEMBL22242 REMOXIPRIDE 4.0 1 5.80
CHEMBL23464 1 5.55
CHEMBL279982 1 5.52
CHEMBL23932 1 5.50
CHEMBL282681 1 5.46
CHEMBL282463 1 4.89
CHEMBL282024 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267723 IOLOPRIDE IC50 = 3.4 nM 8.47
CHEMBL23403 IC50 = 4.7 nM 8.33
CHEMBL22472 IC50 = 4.8 nM 8.32
CHEMBL23437 IC50 = 6.3 nM 8.20
CHEMBL54 HALOPERIDOL IC50 = 12.0 nM 7.92
CHEMBL283099 IC50 = 12.0 nM 7.92
CHEMBL23228 IC50 = 19.0 nM 7.72
CHEMBL283099 IC50 = 21.0 nM 7.68
CHEMBL268555 IC50 = 26.0 nM 7.58
CHEMBL23845 IC50 = 39.0 nM 7.41
CHEMBL23519 IC50 = 56.0 nM 7.25
CHEMBL278767 IC50 = 64.0 nM 7.19
CHEMBL431490 IC50 = 123.0 nM 6.91
CHEMBL280953 IC50 = 150.0 nM 6.82
CHEMBL26 SULPIRIDE IC50 = 233.0 nM 6.63
CHEMBL8945 IC50 = 315.0 nM 6.50
CHEMBL276977 IC50 = 362.0 nM 6.44
CHEMBL282925 IC50 = 921.0 nM 6.04
CHEMBL278560 IC50 = 987.0 nM 6.01
CHEMBL22242 REMOXIPRIDE IC50 = 1570.0 nM 5.80
CHEMBL23464 IC50 = 2790.0 nM 5.55
CHEMBL279982 IC50 = 3020.0 nM 5.52
CHEMBL23932 IC50 = 3190.0 nM 5.50
CHEMBL282681 IC50 = 3500.0 nM 5.46
CHEMBL282463 IC50 = 13000.0 nM 4.89
CHEMBL282024 IC50 = 15300.0 nM 4.82