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Assay Detail

CHEMBL4700533

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

Functional
Inhibition of LPS-induced TNFalpha production in human THP-1 cells incubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 1 — Organism
Curated By Autocuration

Target

THP-1 (CHEMBL614245)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis and biological screening of a library of macamides as TNF-alpha inhibitors
Tena Perez, Victor, Apaza Ticona, Luis, Serban, Andreea Madalina, Acero Gomez, Javier, Rumbero SAnchez, Angel
RSC Med Chem (2020) 11 : 1196 -1209
PubMed 33479624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 5.58 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4741016 1 8.05
CHEMBL4744906 1 7.30
CHEMBL4780964 1 7.22
CHEMBL4760560 1 7.10
CHEMBL4786583 1 6.96
CHEMBL4744685 1 6.48
CHEMBL4791162 1 6.27
CHEMBL4787109 1 6.21
CHEMBL4778317 1 6.15
CHEMBL4795304 1 6.13
CHEMBL4749337 1 6.11
CHEMBL4743882 1 6.11
CHEMBL4782222 1 6.01
CHEMBL4798906 1 6.00
CHEMBL4754239 1 5.92
CHEMBL4757432 1 5.82
CHEMBL4747955 1 5.80
CHEMBL4762818 1 5.77
CHEMBL4752695 1 5.75
CHEMBL4778391 1 5.74
CHEMBL250711 OLEOYL DOPAMINE 1 5.45
CHEMBL4749287 1 5.28
CHEMBL64379 MALINAMIDE 1 5.28
CHEMBL4796598 1 5.19
CHEMBL4780445 1 5.08
CHEMBL4749407 1 5.05
CHEMBL4749194 1 4.88
CHEMBL2415106 1 4.85
CHEMBL1223510 1 4.82
CHEMBL4749954 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4741016 IC50 = 9.0 nM 8.05
CHEMBL4744906 IC50 = 50.0 nM 7.30
CHEMBL4780964 IC50 = 60.0 nM 7.22
CHEMBL4760560 IC50 = 80.0 nM 7.10
CHEMBL4786583 IC50 = 110.0 nM 6.96
CHEMBL4744685 IC50 = 330.0 nM 6.48
CHEMBL4791162 IC50 = 540.0 nM 6.27
CHEMBL4787109 IC50 = 620.0 nM 6.21
CHEMBL4778317 IC50 = 710.0 nM 6.15
CHEMBL4795304 IC50 = 740.0 nM 6.13
CHEMBL4743882 IC50 = 780.0 nM 6.11
CHEMBL4749337 IC50 = 780.0 nM 6.11
CHEMBL4782222 IC50 = 970.0 nM 6.01
CHEMBL4798906 IC50 = 1000.0 nM 6.00
CHEMBL4754239 IC50 = 1210.0 nM 5.92
CHEMBL4757432 IC50 = 1520.0 nM 5.82
CHEMBL4747955 IC50 = 1600.0 nM 5.80
CHEMBL4762818 IC50 = 1710.0 nM 5.77
CHEMBL4752695 IC50 = 1770.0 nM 5.75
CHEMBL4778391 IC50 = 1840.0 nM 5.74
CHEMBL250711 OLEOYL DOPAMINE IC50 = 3540.0 nM 5.45
CHEMBL4749287 IC50 = 5300.0 nM 5.28
CHEMBL64379 MALINAMIDE IC50 = 5200.0 nM 5.28
CHEMBL4796598 IC50 = 6400.0 nM 5.19
CHEMBL4780445 IC50 = 8300.0 nM 5.08
CHEMBL4749407 IC50 = 8900.0 nM 5.05
CHEMBL4749194 IC50 = 13100.0 nM 4.88
CHEMBL2415106 IC50 = 14200.0 nM 4.85
CHEMBL1223510 IC50 = 15200.0 nM 4.82
CHEMBL4749954 IC50 = 15700.0 nM 4.80
CHEMBL2415104 IC50 = 16600.0 nM 4.78
CHEMBL4799813 IC50 = 19700.0 nM 4.71
CHEMBL4762255 IC50 = 21000.0 nM 4.68
CHEMBL4763119 IC50 = 23800.0 nM 4.62
CHEMBL2415102 IC50 = 43100.0 nM 4.37
CHEMBL4776118 IC50 = 56800.0 nM 4.25
CHEMBL4782107 IC50 = 58700.0 nM 4.23
CHEMBL1836706 IC50 = 78400.0 nM 4.11
CHEMBL8659 OLEIC ACID IC50 = 79000.0 nM 4.10