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Assay Detail

CHEMBL2076244

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

Functional
TP_TRANSPORTER: inhibition of TEA uptake in Xenopus laevis oocytes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Xenopus laevis
Cell Type Oocyte
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Solute carrier family 22 member 1 (CHEMBL2073670)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Drug excretion mediated by a new prototype of polyspecific transporter.
Gründemann D, Gorboulev V, Gambaryan S, Veyhl M, Koepsell H.
Nature (1994) 372 : 549 -552
PubMed 7990927 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.63 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2074851 Cyanine-863 1 6.89
CHEMBL1197556 1 6.44
CHEMBL2074704 TETRAPENTYLAMMONIUM 1 6.37
CHEMBL170 QUININE 4.0 1 6.03
CHEMBL72 DESIPRAMINE 4.0 1 5.55
CHEMBL2074659 MEPIPERPHENIDOL BROMIDE -1.0 1 5.28
CHEMBL640 PROCAINAMIDE 4.0 1 4.89
CHEMBL311617 1 4.89
CHEMBL2074647 METIPRENALINE 2.0 1 4.37
CHEMBL110739 CORTICOSTERONE 3.0 1 -
CHEMBL772 RESERPINE 4.0 1 -
CHEMBL1209651 TETRAMETHYLAMMONIUM 1 -
CHEMBL11978 NICOTINYL METHYLAMIDE -1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2074851 Cyanine-863 Ki = 130.0 nM 6.89
CHEMBL1197556 Ki = 360.0 nM 6.44
CHEMBL2074704 TETRAPENTYLAMMONIUM Ki = 430.0 nM 6.37
CHEMBL170 QUININE Ki = 930.0 nM 6.03
CHEMBL72 DESIPRAMINE Ki = 2800.0 nM 5.55
CHEMBL2074659 MEPIPERPHENIDOL BROMIDE Ki = 5200.0 nM 5.28
CHEMBL640 PROCAINAMIDE Ki = 13000.0 nM 4.89
CHEMBL311617 Ki = 13000.0 nM 4.89
CHEMBL2074647 METIPRENALINE Ki = 43000.0 nM 4.37
CHEMBL110739 CORTICOSTERONE Ki > 10000.0 nM -
CHEMBL772 RESERPINE Ki > 20000.0 nM -
CHEMBL1209651 TETRAMETHYLAMMONIUM Ki = 1000000.0 nM -
CHEMBL11978 NICOTINYL METHYLAMIDE Ki = 1000000.0 nM -