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Assay Detail

CHEMBL1243677

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

Binding
Inhibition of SAP130 mediated cell growth in human WiDr cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Splicing factor 3B subunit 3 (CHEMBL1250378)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Splicing factor SF3b as a target of the antitumor natural product pladienolide.
Kotake Y, Sagane K, Owa T, Mimori-Kiyosue Y, Shimizu H, Uesugi M, Ishihama Y, Iwata M, Mizui Y.
Nat Chem Biol (2007) 3 : 570 -575
PubMed 17643112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.56 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1242745 PLADIENOLIDE B 1 9.00
CHEMBL1240972 1 8.49
CHEMBL1242564 PLA D 1 8.37
CHEMBL1242284 1 8.31
CHEMBL1242467 PLADIENOLIDE C 1 8.13
CHEMBL269732 TACROLIMUS ANHYDROUS 4.0 1 7.96
CHEMBL1242654 PLADIENOLIDE E 1 7.19
CHEMBL1242841 PLADIENOLIDE A 1 6.38
CHEMBL99 TRICHOSTATIN 1.0 1 6.24
CHEMBL1242374 PLADIENOLIDE F 1 5.54
CHEMBL374308 LACTACYSTIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1242745 PLADIENOLIDE B IC50 = 1.0 nM 9.00
CHEMBL1240972 IC50 = 3.2 nM 8.49
CHEMBL1242564 PLA D IC50 = 4.3 nM 8.37
CHEMBL1242284 IC50 = 4.9 nM 8.31
CHEMBL1242467 PLADIENOLIDE C IC50 = 7.4 nM 8.13
CHEMBL269732 TACROLIMUS ANHYDROUS IC50 = 10.9 nM 7.96
CHEMBL1242654 PLADIENOLIDE E IC50 = 65.2 nM 7.19
CHEMBL1242841 PLADIENOLIDE A IC50 = 418.1 nM 6.38
CHEMBL99 TRICHOSTATIN IC50 = 577.6 nM 6.24
CHEMBL1242374 PLADIENOLIDE F IC50 = 2894.2 nM 5.54
CHEMBL374308 LACTACYSTIN IC50 > 10000.0 nM -