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Assay Detail

CHEMBL2077061

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Functional
TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM) in OCT3-expressing HRPE cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HRPE
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Solute carrier family 22 member 3 (CHEMBL1770033)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain.
Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V.
J Biol Chem (1998) 273 : 32776 -32786
PubMed 9830022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.33 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 5.96
CHEMBL110739 CORTICOSTERONE 3.0 1 5.31
CHEMBL1498 DESOXYCORTICOSTERONE 1 5.08
CHEMBL103 PROGESTERONE 4.0 1 4.98
CHEMBL59 DOPAMINE 4.0 1 -
CHEMBL1437 NOREPINEPHRINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 1100.0 nM 5.96
CHEMBL110739 CORTICOSTERONE IC50 = 4900.0 nM 5.31
CHEMBL1498 DESOXYCORTICOSTERONE IC50 = 8400.0 nM 5.08
CHEMBL103 PROGESTERONE IC50 = 10500.0 nM 4.98
CHEMBL59 DOPAMINE IC50 = 384000.0 nM -
CHEMBL1437 NOREPINEPHRINE IC50 = 434000.0 nM -