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Assay Detail

CHEMBL854221

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Binding
Inhibition of PTP1B
29
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Tyrosine-protein phosphatase non-receptor type 1 (CHEMBL335)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Monocyclic thiophenes as protein tyrosine phosphatase 1B inhibitors: capturing interactions with Asp48.
Wan ZK, Lee J, Xu W, Erbe DV, Joseph-McCarthy D, Follows BC, Zhang YL.
Bioorg Med Chem Lett (2006) 16 : 4941 -4945
PubMed 16806920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 5.94 6.85
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215335 1 6.85
CHEMBL383882 1 6.70
CHEMBL214912 1 6.60
CHEMBL214502 1 6.52
CHEMBL386616 1 6.44
CHEMBL214911 1 6.30
CHEMBL383967 1 6.24
CHEMBL212232 1 6.22
CHEMBL387242 1 6.21
CHEMBL214794 1 6.13
CHEMBL214378 1 6.09
CHEMBL385276 1 6.00
CHEMBL213662 1 6.00
CHEMBL438089 1 5.92
CHEMBL373883 1 5.85
CHEMBL212335 1 5.80
CHEMBL212285 1 5.60
CHEMBL385896 1 5.52
CHEMBL213758 1 5.50
CHEMBL215242 1 5.48
CHEMBL215656 1 5.40
CHEMBL215243 1 5.30
CHEMBL379196 1 5.05
CHEMBL373413 1 4.75
CHEMBL212605 1 -
CHEMBL445320 1 -
CHEMBL214736 1 -
CHEMBL212289 1 -
CHEMBL212296 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215335 Ki = 140.0 nM 6.85
CHEMBL383882 Ki = 200.0 nM 6.70
CHEMBL214912 Ki = 250.0 nM 6.60
CHEMBL214502 Ki = 300.0 nM 6.52
CHEMBL386616 Ki = 360.0 nM 6.44
CHEMBL214911 Ki = 500.0 nM 6.30
CHEMBL383967 Ki = 570.0 nM 6.24
CHEMBL212232 Ki = 600.0 nM 6.22
CHEMBL387242 Ki = 620.0 nM 6.21
CHEMBL214794 Ki = 740.0 nM 6.13
CHEMBL214378 Ki = 820.0 nM 6.09
CHEMBL385276 Ki = 1000.0 nM 6.00
CHEMBL213662 Ki = 1000.0 nM 6.00
CHEMBL438089 Ki = 1200.0 nM 5.92
CHEMBL373883 Ki = 1400.0 nM 5.85
CHEMBL212335 Ki = 1600.0 nM 5.80
CHEMBL212285 Ki = 2500.0 nM 5.60
CHEMBL385896 Ki = 3000.0 nM 5.52
CHEMBL213758 Ki = 3200.0 nM 5.50
CHEMBL215242 Ki = 3300.0 nM 5.48
CHEMBL215656 Ki = 4000.0 nM 5.40
CHEMBL215243 Ki = 5000.0 nM 5.30
CHEMBL379196 Ki = 9000.0 nM 5.05
CHEMBL373413 Ki = 18000.0 nM 4.75
CHEMBL212605 Ki > 1000000.0 nM -
CHEMBL445320 Ki > 1000000.0 nM -
CHEMBL214736 Activity - -
CHEMBL212289 Ki > 1000000.0 nM -
CHEMBL212296 Ki = 160000.0 nM -