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Assay Detail

CHEMBL673000

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

Binding
Antidopamine activity in vitro by ability to displace [3H]spiperone from rat brain striatal preparations.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
de Paulis T, Kumar Y, Johansson L, Rämsby S, Hall H, Sällemark M, Angeby-Möller K, Ogren SO.
J Med Chem (1986) 29 : 61 -69
PubMed 3941414 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.45 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8946 ETICLOPRIDE 2.0 1 9.04
CHEMBL161122 1 8.82
CHEMBL62429 1 8.74
CHEMBL161668 1 8.64
CHEMBL161973 1 8.59
CHEMBL350287 1 8.52
CHEMBL23403 1 8.33
CHEMBL345223 1 8.30
CHEMBL161972 1 8.26
CHEMBL161417 1 8.18
CHEMBL159842 1 8.11
CHEMBL161177 1 8.10
CHEMBL161721 1 7.96
CHEMBL350997 1 7.96
CHEMBL293904 1 7.92
CHEMBL159292 1 7.77
CHEMBL161361 1 7.77
CHEMBL303334 1 7.58
CHEMBL8809 RACLOPRIDE 2.0 1 7.50
CHEMBL161418 1 7.24
CHEMBL350276 1 6.96
CHEMBL414454 1 6.82
CHEMBL450277 1 6.73
CHEMBL267044 LEVOSULPIRIDE 2.0 1 6.68
CHEMBL22242 REMOXIPRIDE 4.0 1 5.80
CHEMBL308129 1 5.54
CHEMBL159945 1 5.20
CHEMBL349416 1 4.89
CHEMBL25547 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8946 ETICLOPRIDE IC50 = 0.92 nM 9.04
CHEMBL161122 IC50 = 1.5 nM 8.82
CHEMBL62429 IC50 = 1.8 nM 8.74
CHEMBL161668 IC50 = 2.3 nM 8.64
CHEMBL161973 IC50 = 2.6 nM 8.59
CHEMBL350287 IC50 = 3.0 nM 8.52
CHEMBL23403 IC50 = 4.7 nM 8.33
CHEMBL345223 IC50 = 5.0 nM 8.30
CHEMBL161972 IC50 = 5.5 nM 8.26
CHEMBL161417 IC50 = 6.6 nM 8.18
CHEMBL159842 IC50 = 7.7 nM 8.11
CHEMBL161177 IC50 = 8.0 nM 8.10
CHEMBL161721 IC50 = 11.0 nM 7.96
CHEMBL350997 IC50 = 11.0 nM 7.96
CHEMBL293904 IC50 = 12.0 nM 7.92
CHEMBL159292 IC50 = 17.0 nM 7.77
CHEMBL161361 IC50 = 17.0 nM 7.77
CHEMBL303334 IC50 = 26.0 nM 7.58
CHEMBL8809 RACLOPRIDE IC50 = 32.0 nM 7.50
CHEMBL161418 IC50 = 58.0 nM 7.24
CHEMBL350276 IC50 = 110.0 nM 6.96
CHEMBL414454 IC50 = 150.0 nM 6.82
CHEMBL450277 IC50 = 185.0 nM 6.73
CHEMBL267044 LEVOSULPIRIDE IC50 = 210.0 nM 6.68
CHEMBL22242 REMOXIPRIDE IC50 = 1570.0 nM 5.80
CHEMBL308129 IC50 = 2920.0 nM 5.54
CHEMBL159945 IC50 = 6280.0 nM 5.20
CHEMBL349416 IC50 = 12900.0 nM 4.89
CHEMBL25547 IC50 = 59900.0 nM 4.22