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Assay Detail

CHEMBL2076808

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
11
Total Activities
11
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 2 (CHEMBL1743122)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cloning and characterization of two human polyspecific organic cation transporters.
Gorboulev V, Ulzheimer JC, Akhoundova A, Ulzheimer-Teuber I, Karbach U, Quester S, Baumann C, Lang F, Busch AE, Koepsell H.
DNA Cell Biol (1997) 16 : 871 -881
PubMed 9260930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.63 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1197556 1 7.00
CHEMBL2074851 Cyanine-863 1 6.68
CHEMBL2074704 TETRAPENTYLAMMONIUM 1 5.82
CHEMBL311617 1 5.62
CHEMBL170 QUININE 4.0 1 5.47
CHEMBL2074659 MEPIPERPHENIDOL BROMIDE -1.0 1 5.32
CHEMBL72 DESIPRAMINE 4.0 1 4.80
CHEMBL640 PROCAINAMIDE 4.0 1 4.30
CHEMBL1209651 TETRAMETHYLAMMONIUM 1 -
CHEMBL11978 NICOTINYL METHYLAMIDE -1.0 1 -
CHEMBL2074647 METIPRENALINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1197556 Ki = 100.0 nM 7.00
CHEMBL2074851 Cyanine-863 Ki = 210.0 nM 6.68
CHEMBL2074704 TETRAPENTYLAMMONIUM Ki = 1500.0 nM 5.82
CHEMBL311617 Ki = 2400.0 nM 5.62
CHEMBL170 QUININE Ki = 3400.0 nM 5.47
CHEMBL2074659 MEPIPERPHENIDOL BROMIDE Ki = 4800.0 nM 5.32
CHEMBL72 DESIPRAMINE Ki = 16000.0 nM 4.80
CHEMBL640 PROCAINAMIDE Ki = 50000.0 nM 4.30
CHEMBL1209651 TETRAMETHYLAMMONIUM Ki = 180000.0 nM -
CHEMBL11978 NICOTINYL METHYLAMIDE Ki = 266000.0 nM -
CHEMBL2074647 METIPRENALINE Ki = 570000.0 nM -