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Assay Detail

CHEMBL5036175

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Functional
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 24 hrs by Celltiter-Glo cell viability assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MV4-11
Confidence 1 — Organism
Curated By Autocuration

Target

MV4-11 (CHEMBL613835)
Type CELL-LINE
Organism Homo sapiens

Publication

Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity.
Klein VG, Bond AG, Craigon C, Lokey RS, Ciulli A.
J Med Chem (2021) 64 : 18082 -18101
PubMed 34881891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.20 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5087181 1 8.40
CHEMBL4215078 1 7.70
CHEMBL5079045 1 7.30
CHEMBL5075400 1 7.00
CHEMBL5086339 1 6.90
CHEMBL4226570 1 6.90
CHEMBL5081695 1 6.70
CHEMBL5074720 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5087181 EC50 = 3.981 nM 8.40
CHEMBL4215078 EC50 = 19.95 nM 7.70
CHEMBL5079045 EC50 = 50.12 nM 7.30
CHEMBL5075400 EC50 = 100.0 nM 7.00
CHEMBL5086339 EC50 = 125.89 nM 6.90
CHEMBL4226570 EC50 = 125.89 nM 6.90
CHEMBL5081695 EC50 = 199.53 nM 6.70
CHEMBL5074720 EC50 = 199.53 nM 6.70