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Assay Detail

CHEMBL670108

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

Binding
Inhibition of 3[H] WIN-35 428 binding to Dopamine transporter (DAT)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Expansion of structure-activity studies of piperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935) compounds by altering substitutions in the N-benzyl moiety and behavioral pharmacology of selected molecules.
Dutta AK, Davis MC, Fei XS, Beardsley PM, Cook CD, Reith ME.
J Med Chem (2002) 45 : 654 -662
PubMed 11806716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.80 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36074 1 9.02
CHEMBL158427 1 8.53
CHEMBL348100 1 8.39
CHEMBL159128 1 8.35
CHEMBL423061 1 8.09
CHEMBL157757 1 7.94
CHEMBL160812 1 7.84
CHEMBL440191 1 7.71
CHEMBL159184 1 7.57
CHEMBL158832 1 7.20
CHEMBL160897 1 7.19
CHEMBL160559 1 6.95
CHEMBL160488 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36074 IC50 = 0.96 nM 9.02
CHEMBL158427 IC50 = 2.96 nM 8.53
CHEMBL348100 IC50 = 4.1 nM 8.39
CHEMBL159128 IC50 = 4.5 nM 8.35
CHEMBL423061 IC50 = 8.23 nM 8.09
CHEMBL157757 IC50 = 11.6 nM 7.94
CHEMBL160812 IC50 = 14.3 nM 7.84
CHEMBL440191 IC50 = 19.6 nM 7.71
CHEMBL159184 IC50 = 26.9 nM 7.57
CHEMBL158832 IC50 = 63.1 nM 7.20
CHEMBL160897 IC50 = 65.1 nM 7.19
CHEMBL160559 IC50 = 113.0 nM 6.95
CHEMBL160488 IC50 = 240.0 nM 6.62