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Assay Detail

CHEMBL870503

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Binding
Inhibition of PTP1B by pNPP assay
ChEMBL ↗
57
Total Activities
57
Compounds Tested
1
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

Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.
Combs AP, Zhu W, Crawley ML, Glass B, Polam P, Sparks RB, Modi D, Takvorian A, McLaughlin E, Yue EW, Wasserman Z, Bower M, Wei M, Rupar M, Ala PJ, Reid BM, Ellis D, Gonneville L, Emm T, Taylor N, Yeleswaram S, Li Y, Wynn R, Burn TC, Hollis G, Liu PC, Metcalf B.
J Med Chem (2006) 49 : 3774 -3789
PubMed 16789735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 7.01 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377141 — — 1 8.00
CHEMBL381584 — — 1 7.82
CHEMBL378614 — — 1 7.80
CHEMBL211352 — — 1 7.75
CHEMBL208114 — — 1 7.75
CHEMBL210836 — — 1 7.50
CHEMBL377989 — — 1 7.46
CHEMBL211655 — — 1 7.46
CHEMBL424880 — — 1 7.37
CHEMBL212260 — — 1 7.35
CHEMBL377735 — — 1 7.32
CHEMBL208604 — — 1 7.30
CHEMBL207489 — — 1 7.29
CHEMBL206950 — — 1 7.29
CHEMBL264833 — — 1 7.28
CHEMBL212147 — — 1 7.22
CHEMBL383437 — — 1 7.20
CHEMBL436933 — — 1 7.17
CHEMBL210324 — — 1 7.14
CHEMBL377441 — — 1 7.12
CHEMBL209107 — — 1 7.11
CHEMBL208985 — — 1 7.10
CHEMBL380164 — — 1 7.10
CHEMBL211033 — — 1 7.10
CHEMBL210965 — — 1 7.10
CHEMBL211076 — — 1 7.07
CHEMBL211171 — — 1 7.03
CHEMBL377774 — — 1 6.96
CHEMBL210159 — — 1 6.96
CHEMBL437119 — — 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377141 — IC50 = 10.0 nM 8.00
CHEMBL381584 — IC50 = 15.0 nM 7.82
CHEMBL378614 — IC50 = 16.0 nM 7.80
CHEMBL211352 — IC50 = 18.0 nM 7.75
CHEMBL208114 — IC50 = 18.0 nM 7.75
CHEMBL210836 — IC50 = 32.0 nM 7.50
CHEMBL377989 — IC50 = 35.0 nM 7.46
CHEMBL211655 — IC50 = 35.0 nM 7.46
CHEMBL424880 — IC50 = 43.0 nM 7.37
CHEMBL212260 — IC50 = 45.0 nM 7.35
CHEMBL377735 — IC50 = 48.0 nM 7.32
CHEMBL208604 — IC50 = 50.0 nM 7.30
CHEMBL207489 — IC50 = 51.0 nM 7.29
CHEMBL206950 — IC50 = 51.0 nM 7.29
CHEMBL264833 — IC50 = 53.0 nM 7.28
CHEMBL212147 — IC50 = 60.0 nM 7.22
CHEMBL383437 — IC50 = 63.0 nM 7.20
CHEMBL436933 — IC50 = 67.0 nM 7.17
CHEMBL210324 — IC50 = 72.0 nM 7.14
CHEMBL377441 — IC50 = 76.0 nM 7.12
CHEMBL209107 — IC50 = 77.0 nM 7.11
CHEMBL208985 — IC50 = 80.0 nM 7.10
CHEMBL380164 — IC50 = 80.0 nM 7.10
CHEMBL211033 — IC50 = 80.0 nM 7.10
CHEMBL210965 — IC50 = 79.0 nM 7.10
CHEMBL211076 — IC50 = 85.0 nM 7.07
CHEMBL211171 — IC50 = 94.0 nM 7.03
CHEMBL377774 — IC50 = 110.0 nM 6.96
CHEMBL210159 — IC50 = 110.0 nM 6.96
CHEMBL437119 — IC50 = 110.0 nM 6.96
CHEMBL207492 — IC50 = 110.0 nM 6.96
CHEMBL378746 — IC50 = 120.0 nM 6.92
CHEMBL210837 — IC50 = 120.0 nM 6.92
CHEMBL376950 — IC50 = 130.0 nM 6.89
CHEMBL209304 — IC50 = 130.0 nM 6.89
CHEMBL264347 — IC50 = 140.0 nM 6.85
CHEMBL378747 — IC50 = 140.0 nM 6.85
CHEMBL377978 — IC50 = 140.0 nM 6.85
CHEMBL438957 — IC50 = 150.0 nM 6.82
CHEMBL211990 — IC50 = 160.0 nM 6.80
CHEMBL207645 — IC50 = 160.0 nM 6.80
CHEMBL209197 — IC50 = 160.0 nM 6.80
CHEMBL377816 — IC50 = 160.0 nM 6.80
CHEMBL209180 — IC50 = 170.0 nM 6.77
CHEMBL208982 — IC50 = 190.0 nM 6.72
CHEMBL208984 — IC50 = 240.0 nM 6.62
CHEMBL377138 — IC50 = 240.0 nM 6.62
CHEMBL382311 — IC50 = 240.0 nM 6.62
CHEMBL378992 — IC50 = 280.0 nM 6.55
CHEMBL377476 — IC50 = 300.0 nM 6.52