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Assay Detail

CHEMBL997155

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

Binding
Inhibition of dynamin 1-mediated endocytosis internalization of Tf-A594 in human U2OS cells pretreated for 30 mins
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dynamin-1 (CHEMBL4958)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibition of dynamin mediated endocytosis by the dynoles--synthesis and functional activity of a family of indoles.
Hill TA, Gordon CP, McGeachie AB, Venn-Brown B, Odell LR, Chau N, Quan A, Mariana A, Sakoff JA, Chircop M, Robinson PJ, McCluskey A.
J Med Chem (2009) 52 : 3762 -3773
PubMed 19459681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.85 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483059 1 5.30
CHEMBL496625 1 4.97
CHEMBL523731 1 4.88
CHEMBL496824 1 4.84
CHEMBL496626 1 4.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483059 IC50 = 5000.0 nM 5.30
CHEMBL496625 IC50 = 10800.0 nM 4.97
CHEMBL523731 IC50 = 13200.0 nM 4.88
CHEMBL496824 IC50 = 14300.0 nM 4.84
CHEMBL496626 IC50 = 58200.0 nM 4.24