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Assay Detail

CHEMBL834320

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

Functional
Concentration required to inhibit tumor cell growth in KB-8-5 cells
ChEMBL ↗
71
Total Activities
70
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

KB (CHEMBL398) ↗
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 71 6.82 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL186081 — — 1 9.00
CHEMBL182319 TALTOBULIN 2.0 1 8.64
CHEMBL189092 — — 1 8.62
CHEMBL364159 — — 1 8.43
CHEMBL188372 — — 1 8.39
CHEMBL364121 — — 1 8.24
CHEMBL189817 — — 1 8.22
CHEMBL186238 — — 1 8.17
CHEMBL181650 — — 1 8.15
CHEMBL361685 — — 1 7.96
CHEMBL188682 — — 1 7.85
CHEMBL189042 — — 1 7.75
CHEMBL364107 — — 1 7.72
CHEMBL189702 — — 1 7.72
CHEMBL363127 — — 1 7.72
CHEMBL189648 — — 1 7.66
CHEMBL454574 — — 1 7.41
CHEMBL186044 — — 1 7.25
CHEMBL188356 — — 1 7.24
CHEMBL362289 — — 1 7.22
CHEMBL365487 — — 1 7.21
CHEMBL364788 — — 1 7.20
CHEMBL189070 — — 1 7.16
CHEMBL186143 — — 1 7.16
CHEMBL186323 — — 1 7.12
CHEMBL362118 — — 1 7.11
CHEMBL189034 — — 1 6.89
CHEMBL186875 — — 1 6.89
CHEMBL427525 — — 1 6.80
CHEMBL188724 — — 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL186081 — IC50 = 1.0 nM 9.00
CHEMBL182319 TALTOBULIN IC50 = 2.3 nM 8.64
CHEMBL189092 — IC50 = 2.4 nM 8.62
CHEMBL364159 — IC50 = 3.7 nM 8.43
CHEMBL188372 — IC50 = 4.1 nM 8.39
CHEMBL364121 — IC50 = 5.7 nM 8.24
CHEMBL189817 — IC50 = 6.0 nM 8.22
CHEMBL186238 — IC50 = 6.8 nM 8.17
CHEMBL181650 — IC50 = 7.1 nM 8.15
CHEMBL361685 — IC50 = 11.0 nM 7.96
CHEMBL188682 — IC50 = 14.0 nM 7.85
CHEMBL189042 — IC50 = 18.0 nM 7.75
CHEMBL363127 — IC50 = 19.1 nM 7.72
CHEMBL189702 — IC50 = 19.0 nM 7.72
CHEMBL364107 — IC50 = 19.0 nM 7.72
CHEMBL189648 — IC50 = 22.0 nM 7.66
CHEMBL454574 — IC50 = 39.0 nM 7.41
CHEMBL186044 — IC50 = 56.0 nM 7.25
CHEMBL188356 — IC50 = 57.0 nM 7.24
CHEMBL362289 — IC50 = 60.0 nM 7.22
CHEMBL365487 — IC50 = 62.0 nM 7.21
CHEMBL364788 — IC50 = 63.0 nM 7.20
CHEMBL189070 — IC50 = 69.0 nM 7.16
CHEMBL186143 — IC50 = 70.0 nM 7.16
CHEMBL186323 — IC50 = 75.0 nM 7.12
CHEMBL362118 — IC50 = 78.0 nM 7.11
CHEMBL186875 — IC50 = 129.0 nM 6.89
CHEMBL189034 — IC50 = 130.0 nM 6.89
CHEMBL427525 — IC50 = 158.0 nM 6.80
CHEMBL188724 — IC50 = 162.0 nM 6.79
CHEMBL362764 — IC50 = 180.0 nM 6.75
CHEMBL185957 — IC50 = 197.0 nM 6.71
CHEMBL186983 — IC50 = 196.0 nM 6.71
CHEMBL362883 — IC50 = 226.0 nM 6.65
CHEMBL184739 — IC50 = 227.0 nM 6.64
CHEMBL362891 — IC50 = 293.0 nM 6.53
CHEMBL186997 — IC50 = 363.0 nM 6.44
CHEMBL363038 — IC50 = 414.0 nM 6.38
CHEMBL185704 — IC50 = 499.0 nM 6.30
CHEMBL185985 — IC50 = 550.0 nM 6.26
CHEMBL359983 — IC50 = 584.0 nM 6.23
CHEMBL187638 — IC50 = 616.0 nM 6.21
CHEMBL188891 — IC50 = 646.0 nM 6.19
CHEMBL425183 — IC50 = 639.0 nM 6.19
CHEMBL363114 — IC50 = 846.0 nM 6.07
CHEMBL189705 — IC50 = 902.0 nM 6.04
CHEMBL188573 — IC50 = 1148.0 nM 5.94
CHEMBL185943 — IC50 = 1148.0 nM 5.94
CHEMBL186118 — IC50 = 1202.0 nM 5.92
CHEMBL186834 — IC50 = 1202.0 nM 5.92