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Assay Detail

CHEMBL4275887

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

Functional
Antiproliferative activity against human HEMC-SS cells treated for 24 hrs under hypoxic condition followed by compound wash-out and incubated under normoxic condition for 48 hrs by alamar blue assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type H-EMC-SS
Confidence 1 — Organism
Curated By Intermediate

Target

H-EMC-SS (CHEMBL1075451)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-activity relationship study of hypoxia-activated prodrugs for proteoglycan-targeted chemotherapy in chondrosarcoma.
Ghedira D, Voissière A, Peyrode C, Kraiem J, Gerard Y, Maubert E, Vivier M, Miot-Noirault E, Chezal JM, Farhat F, Weber V.
Eur J Med Chem (2018) 158 : 51 -67
PubMed 30199705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.87 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260046 EVOFOSFAMIDE 3.0 1 6.89
CHEMBL4294007 1 6.40
CHEMBL4278857 1 6.10
CHEMBL4289535 1 5.96
CHEMBL4282724 1 5.85
CHEMBL4283062 1 5.82
CHEMBL4279260 1 5.82
CHEMBL4284207 1 5.77
CHEMBL4286107 1 5.75
CHEMBL4292087 1 5.68
CHEMBL4290926 1 5.62
CHEMBL4287185 1 5.62
CHEMBL4290602 1 5.55
CHEMBL4277694 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260046 EVOFOSFAMIDE IC50 = 130.0 nM 6.89
CHEMBL4294007 IC50 = 400.0 nM 6.40
CHEMBL4278857 IC50 = 800.0 nM 6.10
CHEMBL4289535 IC50 = 1100.0 nM 5.96
CHEMBL4282724 IC50 = 1400.0 nM 5.85
CHEMBL4283062 IC50 = 1500.0 nM 5.82
CHEMBL4279260 IC50 = 1500.0 nM 5.82
CHEMBL4284207 IC50 = 1700.0 nM 5.77
CHEMBL4286107 IC50 = 1800.0 nM 5.75
CHEMBL4292087 IC50 = 2100.0 nM 5.68
CHEMBL4290926 IC50 = 2400.0 nM 5.62
CHEMBL4287185 IC50 = 2400.0 nM 5.62
CHEMBL4290602 IC50 = 2800.0 nM 5.55
CHEMBL4277694 IC50 = 4300.0 nM 5.37