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Assay Detail

CHEMBL771315

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

Binding
Inhibitory effect against human protein-tyrosine phosphatase alpha (PTPalpha), using p-nitrophenyl phosphate substrate at pH 5.5.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Receptor-type tyrosine-protein phosphatase alpha (CHEMBL3918)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B.
Andersen HS, Olsen OH, Iversen LF, Sørensen AL, Mortensen SB, Christensen MS, Branner S, Hansen TK, Lau JF, Jeppesen L, Moran EJ, Su J, Bakir F, Judge L, Shahbaz M, Collins T, Vo T, Newman MJ, Ripka WC, Møller NP.
J Med Chem (2002) 45 : 4443 -4459
PubMed 12238924 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 4.08 4.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138025 1 4.28
CHEMBL343979 1 4.19
CHEMBL336908 1 4.05
CHEMBL138659 1 4.03
CHEMBL139423 1 4.00
CHEMBL336435 1 4.00
CHEMBL139923 1 4.00
CHEMBL138806 1 -
CHEMBL344585 1 -
CHEMBL342612 1 -
CHEMBL138406 1 -
CHEMBL342478 1 -
CHEMBL141481 1 -
CHEMBL341806 1 -
CHEMBL344412 1 -
CHEMBL139422 1 -
CHEMBL139491 1 -
CHEMBL139024 1 -
CHEMBL139489 1 -
CHEMBL138713 1 -
CHEMBL138575 1 -
CHEMBL336894 1 -
CHEMBL140929 1 -
CHEMBL138257 1 -
CHEMBL138151 1 -
CHEMBL138152 1 -
CHEMBL337132 1 -
CHEMBL139356 1 -
CHEMBL137867 1 -
CHEMBL343587 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138025 Ki = 52000.0 nM 4.28
CHEMBL343979 Ki = 65000.0 nM 4.19
CHEMBL336908 Ki = 89000.0 nM 4.05
CHEMBL138659 Ki = 93000.0 nM 4.03
CHEMBL139423 Ki = 100000.0 nM 4.00
CHEMBL336435 Ki = 100000.0 nM 4.00
CHEMBL139923 Ki = 100000.0 nM 4.00
CHEMBL342478 Ki = 180000.0 nM -
CHEMBL341558 Ki = 150000.0 nM -
CHEMBL141481 Ki = 700000.0 nM -
CHEMBL341806 Ki = 800000.0 nM -
CHEMBL344412 Ki = 280000.0 nM -
CHEMBL139422 Ki = 363000.0 nM -
CHEMBL139491 Ki = 1789000.0 nM -
CHEMBL139024 Ki = 530000.0 nM -
CHEMBL344585 Ki = 980000.0 nM -
CHEMBL423546 Ki = 210000.0 nM -
CHEMBL139590 Ki = 250000.0 nM -
CHEMBL337759 Ki = 210000.0 nM -
CHEMBL139050 Ki = 870000.0 nM -
CHEMBL336879 Ki = 2000000.0 nM -
CHEMBL337326 Ki = 2000000.0 nM -
CHEMBL138406 Ki = 1000000.0 nM -
CHEMBL342612 Ki = 1700000.0 nM -
CHEMBL138806 Ki = 170000.0 nM -
CHEMBL139489 Ki = 340000.0 nM -
CHEMBL138713 Ki = 2000000.0 nM -
CHEMBL138575 Ki = 200000.0 nM -
CHEMBL336894 Ki = 150000.0 nM -
CHEMBL140929 Ki = 2000000.0 nM -
CHEMBL138257 Ki = 200000.0 nM -
CHEMBL138151 Ki = 320000.0 nM -
CHEMBL138152 Ki = 290000.0 nM -
CHEMBL337132 Ki = 2000000.0 nM -
CHEMBL139356 Ki = 215000.0 nM -
CHEMBL137867 Ki = 250000.0 nM -
CHEMBL343587 Ki = 322000.0 nM -