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Assay Detail

CHEMBL706282

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

Functional
In vitro concentration required to kill 50% of LNCaP human prostate cancer cell line
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type LNCaP
Confidence 1 — Organism
Curated By Intermediate

Target

LNCaP (CHEMBL612518)
Type CELL-LINE
Organism Homo sapiens

Publication

Design and synthesis of a pro-drug of vinblastine targeted at treatment of prostate cancer with enhanced efficacy and reduced systemic toxicity.
Brady SF, Pawluczyk JM, Lumma PK, Feng DM, Wai JM, Jones R, DeFeo-Jones D, Wong BK, Miller-Stein C, Lin JH, Oliff A, Freidinger RM, Garsky VM.
J Med Chem (2002) 45 : 4706 -4715
PubMed 12361397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 5.56 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL142678 1 7.00
CHEMBL357171 1 6.52
CHEMBL378544 VINBLASTINE SULFATE 4.0 1 6.30
CHEMBL413081 1 6.00
CHEMBL266634 1 5.80
CHEMBL383912 1 5.40
CHEMBL412869 1 5.03
CHEMBL384108 1 4.80
CHEMBL439254 1 4.40
CHEMBL265312 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL142678 EC50 = 100.0 nM 7.00
CHEMBL357171 EC50 = 300.0 nM 6.52
CHEMBL378544 VINBLASTINE SULFATE EC50 = 500.0 nM 6.30
CHEMBL413081 EC50 = 1000.0 nM 6.00
CHEMBL266634 EC50 = 1600.0 nM 5.80
CHEMBL383912 EC50 = 4000.0 nM 5.40
CHEMBL412869 EC50 = 9300.0 nM 5.03
CHEMBL384108 EC50 = 16000.0 nM 4.80
CHEMBL439254 EC50 = 40000.0 nM 4.40
CHEMBL265312 EC50 = 48000.0 nM 4.32