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Assay Detail

CHEMBL5587075

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

Binding
Inhibition of His-tagged PP5 (169 to 499 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells using pNPP as substrate incubated for 30 mins
26
Total Activities
26
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

Tissue factor pathway inhibitor 2 (CHEMBL6066240)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Synthesis of 7-Oxabicyclo[2.2.1]heptane-2,3-dicarboxylic Acid Derivatives as PP5 Inhibitors To Reverse Temozolomide Resistance in Glioblastoma Multiforme.
Li Z, Guo M, Gu M, Cai Z, Wu Q, Yu J, Tang M, He C, Wang Y, Sun P, You Q, Wang L.
J Med Chem (2024) 67 : 15691 -15710
PubMed 39136241 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 4.98 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5597580 1 6.05
CHEMBL428650 ENDOTHALL 1 5.51
CHEMBL5596734 1 5.44
CHEMBL5596696 1 5.39
CHEMBL5597886 1 5.27
CHEMBL5596039 1 5.21
CHEMBL5598389 1 5.21
CHEMBL5597987 1 5.17
CHEMBL5597468 1 5.14
CHEMBL5598083 1 5.11
CHEMBL5598075 1 5.11
CHEMBL5597434 1 5.07
CHEMBL5597115 1 4.94
CHEMBL5597001 1 4.76
CHEMBL5596690 1 4.65
CHEMBL5597671 1 4.57
CHEMBL5596676 1 4.39
CHEMBL5598406 1 4.27
CHEMBL5596433 1 4.23
CHEMBL5597836 1 4.11
CHEMBL5596464 1 -
CHEMBL5598044 1 -
CHEMBL5598087 1 -
CHEMBL5597525 1 -
CHEMBL5597048 1 -
CHEMBL5596793 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5597580 IC50 = 900.0 nM 6.05
CHEMBL428650 ENDOTHALL IC50 = 3100.0 nM 5.51
CHEMBL5596734 IC50 = 3600.0 nM 5.44
CHEMBL5596696 IC50 = 4100.0 nM 5.39
CHEMBL5597886 IC50 = 5400.0 nM 5.27
CHEMBL5596039 IC50 = 6100.0 nM 5.21
CHEMBL5598389 IC50 = 6200.0 nM 5.21
CHEMBL5597987 IC50 = 6700.0 nM 5.17
CHEMBL5597468 IC50 = 7200.0 nM 5.14
CHEMBL5598083 IC50 = 7700.0 nM 5.11
CHEMBL5598075 IC50 = 7700.0 nM 5.11
CHEMBL5597434 IC50 = 8500.0 nM 5.07
CHEMBL5597115 IC50 = 11600.0 nM 4.94
CHEMBL5597001 IC50 = 17300.0 nM 4.76
CHEMBL5596690 IC50 = 22500.0 nM 4.65
CHEMBL5597671 IC50 = 27100.0 nM 4.57
CHEMBL5596676 IC50 = 40400.0 nM 4.39
CHEMBL5598406 IC50 = 53200.0 nM 4.27
CHEMBL5596433 IC50 = 58300.0 nM 4.23
CHEMBL5597836 IC50 = 77900.0 nM 4.11
CHEMBL5596464 IC50 > 100000.0 nM -
CHEMBL5598044 IC50 > 100000.0 nM -
CHEMBL5598087 IC50 > 100000.0 nM -
CHEMBL5597525 IC50 > 100000.0 nM -
CHEMBL5597048 IC50 > 100000.0 nM -
CHEMBL5596793 IC50 = 463000.0 nM -