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Assay Detail

CHEMBL833406

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Functional
Inhibitory concentration against Lox melanoma cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type LOX IMVI
Confidence 1 — Organism
Curated By Expert

Target

LOX IMVI (CHEMBL614096)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).
Zask A, Birnberg G, Cheung K, Kaplan J, Niu C, Norton E, Suayan R, Yamashita A, Cole D, Tang Z, Krishnamurthy G, Williamson R, Khafizova G, Musto S, Hernandez R, Annable T, Yang X, Discafani C, Beyer C, Greenberger LM, Loganzo F, Ayral-Kaloustian S.
J Med Chem (2004) 47 : 4774 -4786
PubMed 15341492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.91 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188372 1 8.96
CHEMBL182319 TALTOBULIN 2.0 1 8.85
CHEMBL181650 1 8.52
CHEMBL188682 1 8.20
CHEMBL186044 1 8.00
CHEMBL185704 1 7.86
CHEMBL428647 PACLITAXEL 4.0 1 7.76
CHEMBL189034 1 7.64
CHEMBL454574 1 7.43
CHEMBL425183 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188372 IC50 = 1.1 nM 8.96
CHEMBL182319 TALTOBULIN IC50 = 1.4 nM 8.85
CHEMBL181650 IC50 = 3.0 nM 8.52
CHEMBL188682 IC50 = 6.3 nM 8.20
CHEMBL186044 IC50 = 10.0 nM 8.00
CHEMBL185704 IC50 = 13.9 nM 7.86
CHEMBL428647 PACLITAXEL IC50 = 17.3 nM 7.76
CHEMBL189034 IC50 = 23.0 nM 7.64
CHEMBL454574 IC50 = 37.0 nM 7.43
CHEMBL425183 IC50 = 1380.0 nM 5.86