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Assay Detail

CHEMBL5036176

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Functional
Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 72 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 CWR22R
Confidence 1 — Organism
Curated By Autocuration

Target

CWR22R (CHEMBL612657)
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 6.58 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215078 1 7.36
CHEMBL5087181 1 7.20
CHEMBL5079045 1 6.60
CHEMBL5086339 1 6.50
CHEMBL5075400 1 6.40
CHEMBL4226570 1 6.30
CHEMBL5074720 1 6.20
CHEMBL5081695 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215078 EC50 = 44.0 nM 7.36
CHEMBL5087181 EC50 = 63.1 nM 7.20
CHEMBL5079045 EC50 = 251.19 nM 6.60
CHEMBL5086339 EC50 = 316.23 nM 6.50
CHEMBL5075400 EC50 = 398.11 nM 6.40
CHEMBL4226570 EC50 = 501.19 nM 6.30
CHEMBL5074720 EC50 = 630.96 nM 6.20
CHEMBL5081695 EC50 = 794.33 nM 6.10