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Assay Detail

CHEMBL833366

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Functional
Inhibitory concentration against S1 cells was evaluated
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type S1
Confidence 1 — Organism
Curated By Autocuration

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 4 7.45 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182319 TALTOBULIN 2.0 1 8.43
CHEMBL188372 1 8.14
CHEMBL428647 PACLITAXEL 4.0 1 7.04
CHEMBL186875 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182319 TALTOBULIN IC50 = 3.7 nM 8.43
CHEMBL188372 IC50 = 7.3 nM 8.14
CHEMBL428647 PACLITAXEL IC50 = 92.0 nM 7.04
CHEMBL186875 IC50 = 657.0 nM 6.18