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Assay Detail

CHEMBL707201

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

Functional
Inhibition of [3H]spermidine transport into MDA-MB-231 (human breast cancer) cells.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 1 — Organism
Curated By Expert

Target

MDA-MB-231 (CHEMBL400)
Type CELL-LINE
Organism Homo sapiens

Publication

Amino acid/spermine conjugates: polyamine amides as potent spermidine uptake inhibitors.
Burns MR, Carlson CL, Vanderwerf SM, Ziemer JR, Weeks RS, Cai F, Webb HK, Graminski GF.
J Med Chem (2001) 44 : 3632 -3644
PubMed 11606128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.63 7.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406117 GUSPERIMUS 3.0 1 7.09
CHEMBL121187 1 7.07
CHEMBL19612 SPERMIDINE 3.0 1 6.95
CHEMBL25101 1 6.75
CHEMBL313747 JORO SPIDER TOXIN 3 1 6.72
CHEMBL121124 1 6.59
CHEMBL123001 1 6.58
CHEMBL23194 SPERMINE 0.5 1 6.55
CHEMBL121343 1 6.55
CHEMBL120820 1 6.17
CHEMBL46257 PUTRESCINE 3.0 1 5.89
CHEMBL121239 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406117 GUSPERIMUS Ki = 81.0 nM 7.09
CHEMBL121187 Ki = 86.0 nM 7.07
CHEMBL19612 SPERMIDINE Ki = 113.0 nM 6.95
CHEMBL25101 Ki = 178.0 nM 6.75
CHEMBL313747 JORO SPIDER TOXIN 3 Ki = 190.0 nM 6.72
CHEMBL121124 Ki = 256.0 nM 6.59
CHEMBL123001 Ki = 262.0 nM 6.58
CHEMBL23194 SPERMINE Ki = 280.0 nM 6.55
CHEMBL121343 Ki = 284.0 nM 6.55
CHEMBL120820 Ki = 672.0 nM 6.17
CHEMBL46257 PUTRESCINE Ki = 1280.0 nM 5.89
CHEMBL121239 Ki > 1000.0 nM -