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Assay Detail

CHEMBL2089751

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

Binding
Inhibition of human recombinant PTP1B using p-nitrophenyl phosphate as substrate assessed as p-nitrophenol release after 30 mins
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Rhododendric acid A, a new ursane-type PTP1B inhibitor from the endangered plant Rhododendron brachycarpum G. Don.
Choi YH, Zhou W, Oh J, Choe S, Kim DW, Lee SH, Na M.
Bioorg Med Chem Lett (2012) 22 : 6116 -6119
PubMed 22940448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.08 5.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169 URSOLIC ACID 2.0 1 5.51
CHEMBL426373 1 5.40
CHEMBL2086414 RHODODENDRIC ACID A 1 5.20
CHEMBL391533 COROSOLIC ACID 1 5.16
CHEMBL523622 1 5.13
CHEMBL2088611 1 4.76
CHEMBL2088612 ACTINIDIC ACID 1 4.75
CHEMBL1271052 ROTUNDIC ACID 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169 URSOLIC ACID IC50 = 3100.0 nM 5.51
CHEMBL426373 IC50 = 4000.0 nM 5.40
CHEMBL2086414 RHODODENDRIC ACID A IC50 = 6300.0 nM 5.20
CHEMBL391533 COROSOLIC ACID IC50 = 7000.0 nM 5.16
CHEMBL523622 IC50 = 7400.0 nM 5.13
CHEMBL2088611 IC50 = 17400.0 nM 4.76
CHEMBL2088612 ACTINIDIC ACID IC50 = 18000.0 nM 4.75
CHEMBL1271052 ROTUNDIC ACID IC50 = 20100.0 nM 4.70