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Assay Detail

CHEMBL2175528

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

Binding
Inhibition of TNFalpha-induced human NFkappaB activity in HEK293 cells incubated for 6 hrs followed by compound wash out measured after 5 mins by by luciferase assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification, synthesis, and biological evaluation of the metabolites of 3-amino-6-(3'-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11-(6H)dione (AM6-36), a promising rexinoid lead compound for the development of cancer chemotherapeutic and chemopreventive agents.
Chen L, Conda-Sheridan M, Reddy PV, Morrell A, Park EJ, Kondratyuk TP, Pezzuto JM, van Breemen RB, Cushman M.
J Med Chem (2012) 55 : 5965 -5981
PubMed 22712432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.21 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172205 1 6.40
CHEMBL2172211 1 6.22
CHEMBL2172207 1 6.16
CHEMBL403183 1 5.70
CHEMBL242413 1 5.58
CHEMBL2172209 1 5.43
CHEMBL60718 TPCK 1 5.29
CHEMBL2172300 1 5.14
CHEMBL2172299 1 4.84
CHEMBL2172212 1 4.58
CHEMBL2172206 1 4.49
CHEMBL2172298 1 4.41
CHEMBL2172210 1 4.40
CHEMBL2172217 1 4.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172205 IC50 = 400.0 nM 6.40
CHEMBL2172211 IC50 = 600.0 nM 6.22
CHEMBL2172207 IC50 = 700.0 nM 6.16
CHEMBL403183 IC50 = 2010.0 nM 5.70
CHEMBL242413 IC50 = 2600.0 nM 5.58
CHEMBL2172209 IC50 = 3700.0 nM 5.43
CHEMBL60718 TPCK IC50 = 5100.0 nM 5.29
CHEMBL2172300 IC50 = 7300.0 nM 5.14
CHEMBL2172299 IC50 = 14400.0 nM 4.84
CHEMBL2172212 IC50 = 26300.0 nM 4.58
CHEMBL2172206 IC50 = 32300.0 nM 4.49
CHEMBL2172298 IC50 = 38800.0 nM 4.41
CHEMBL2172210 IC50 = 39800.0 nM 4.40
CHEMBL2172217 IC50 = 49300.0 nM 4.31