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Assay Detail

CHEMBL841753

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Binding
Binding affinity towards tubulin
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Tubulin beta-1 chain (CHEMBL1915)
Type SINGLE PROTEIN
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
Kd 7 5.95 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182319 TALTOBULIN 2.0 1 6.58
CHEMBL188372 1 6.16
CHEMBL181650 1 6.16
CHEMBL365487 1 6.00
CHEMBL364121 1 5.92
CHEMBL363127 1 5.40
CHEMBL185704 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182319 TALTOBULIN Kd = 260.0 nM 6.58
CHEMBL188372 Kd = 700.0 nM 6.16
CHEMBL181650 Kd = 700.0 nM 6.16
CHEMBL365487 Kd = 1000.0 nM 6.00
CHEMBL364121 Kd = 1200.0 nM 5.92
CHEMBL363127 Kd = 4000.0 nM 5.40
CHEMBL185704 Kd = 4000.0 nM 5.40