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Assay Detail

CHEMBL1787264

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Binding
Inhibition of TPA-induced degradation of Pdcd4 (amino acid 39-91) expressed in human HEK293 cells assessed as minimum compound concentration required for 50% recovery of Pdcd4-luciferase signal incubated for 8 hrs by luciferase reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Programmed cell death protein 4 (CHEMBL1781868)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cryptocaryols A-H, α-pyrone-containing 1,3-polyols from Cryptocarya sp. implicated in stabilizing the tumor suppressor Pdcd4.
Grkovic T, Blees JS, Colburn NH, Schmid T, Thomas CL, Henrich CJ, McMahon JB, Gustafson KR.
J Nat Prod (2011) 74 : 1015 -1020
PubMed 21539301 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 5.84 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413 SIROLIMUS 4.0 1 7.30
CHEMBL1784378 CRYPTOCARYOL G 1 5.89
CHEMBL1784375 CRYPTOCARYOL D 1 5.82
CHEMBL1784374 CRYPTOCARYOL C 1 5.80
CHEMBL1784376 CRYPTOCARYOL E 1 5.75
CHEMBL1784379 CRYPTOCARYOL H 1 5.75
CHEMBL1784373 CRYPTOCARYOL B 1 5.52
CHEMBL1784377 CRYPTOCARYOL F 1 5.46
CHEMBL1784372 CRYPTOCARYOL A 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413 SIROLIMUS EC50 = 50.0 nM 7.30
CHEMBL1784378 CRYPTOCARYOL G EC50 = 1300.0 nM 5.89
CHEMBL1784375 CRYPTOCARYOL D EC50 = 1500.0 nM 5.82
CHEMBL1784374 CRYPTOCARYOL C EC50 = 1600.0 nM 5.80
CHEMBL1784376 CRYPTOCARYOL E EC50 = 1800.0 nM 5.75
CHEMBL1784379 CRYPTOCARYOL H EC50 = 1800.0 nM 5.75
CHEMBL1784373 CRYPTOCARYOL B EC50 = 3000.0 nM 5.52
CHEMBL1784377 CRYPTOCARYOL F EC50 = 3500.0 nM 5.46
CHEMBL1784372 CRYPTOCARYOL A EC50 = 4900.0 nM 5.31