Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4734095

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

Binding
Activation of NF-KappaB (unknown origin) expressed in SH-SY5Y cells co-transfected with pNFkappaB-Luc/pEF6 measured after 24 hrs by Bright-Glo luciferase assay
ChEMBL ↗
102
Total Activities
102
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-SY5Y
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Structure-activity relationship (SAR) studies of N-(3-methylpyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine (SRI-22819) as NF-ҡB activators for the treatment of ALS.
Mathew B,Ruiz P,Dutta S,Entrekin JT,Zhang S,Patel KD,Simmons MS,Augelli-Szafran CE,Cowell RM,Suto MJ
Eur J Med Chem (2021) 210 : 112952 -112952
PubMed 33139114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 102 5.58 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4535691 — — 1 6.80
CHEMBL4791573 — — 1 6.75
CHEMBL4750736 — — 1 6.60
CHEMBL4743351 — — 1 6.54
CHEMBL490592 — — 1 6.46
CHEMBL4796053 — — 1 6.43
CHEMBL4465283 — — 1 6.40
CHEMBL2441195 — — 1 6.32
CHEMBL4797891 — — 1 6.31
CHEMBL2441361 — — 1 6.14
CHEMBL1190223 — — 1 6.10
CHEMBL4788678 — — 1 6.05
CHEMBL4777602 — — 1 6.05
CHEMBL4745272 — — 1 6.03
CHEMBL4763340 — — 1 5.98
CHEMBL256997 ATALUREN 4.0 1 5.96
CHEMBL4749814 — — 1 5.92
CHEMBL4743018 — — 1 5.92
CHEMBL4572792 — — 1 5.92
CHEMBL4745119 — — 1 5.89
CHEMBL4474207 — — 1 5.88
CHEMBL4763195 — — 1 5.85
CHEMBL567009 — — 1 5.82
CHEMBL4752042 — — 1 5.82
CHEMBL4749314 — — 1 5.80
CHEMBL4588896 — — 1 5.80
CHEMBL4746376 — — 1 5.80
CHEMBL4753363 — — 1 5.71
CHEMBL4746431 — — 1 5.70
CHEMBL4799655 — — 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4535691 — EC50 = 160.0 nM 6.80
CHEMBL4791573 — EC50 = 180.0 nM 6.75
CHEMBL4750736 — EC50 = 250.0 nM 6.60
CHEMBL4743351 — EC50 = 290.0 nM 6.54
CHEMBL490592 — EC50 = 350.0 nM 6.46
CHEMBL4796053 — EC50 = 370.0 nM 6.43
CHEMBL4465283 — EC50 = 400.0 nM 6.40
CHEMBL2441195 — EC50 = 480.0 nM 6.32
CHEMBL4797891 — EC50 = 490.0 nM 6.31
CHEMBL2441361 — EC50 = 730.0 nM 6.14
CHEMBL1190223 — EC50 = 800.0 nM 6.10
CHEMBL4788678 — EC50 = 900.0 nM 6.05
CHEMBL4777602 — EC50 = 900.0 nM 6.05
CHEMBL4745272 — EC50 = 940.0 nM 6.03
CHEMBL4763340 — EC50 = 1050.0 nM 5.98
CHEMBL256997 ATALUREN EC50 = 1100.0 nM 5.96
CHEMBL4572792 — EC50 = 1200.0 nM 5.92
CHEMBL4743018 — EC50 = 1210.0 nM 5.92
CHEMBL4749814 — EC50 = 1200.0 nM 5.92
CHEMBL4745119 — EC50 = 1300.0 nM 5.89
CHEMBL4474207 — EC50 = 1310.0 nM 5.88
CHEMBL4763195 — EC50 = 1400.0 nM 5.85
CHEMBL567009 — EC50 = 1500.0 nM 5.82
CHEMBL4752042 — EC50 = 1500.0 nM 5.82
CHEMBL4749314 — EC50 = 1590.0 nM 5.80
CHEMBL4588896 — EC50 = 1580.0 nM 5.80
CHEMBL4746376 — EC50 = 1600.0 nM 5.80
CHEMBL4753363 — EC50 = 1930.0 nM 5.71
CHEMBL4746431 — EC50 = 1980.0 nM 5.70
CHEMBL4784893 — EC50 = 2060.0 nM 5.69
CHEMBL4799655 — EC50 = 2050.0 nM 5.69
CHEMBL4743340 — EC50 = 2160.0 nM 5.67
CHEMBL576027 — EC50 = 2500.0 nM 5.60
CHEMBL4790033 — EC50 = 2500.0 nM 5.60
CHEMBL4739954 — EC50 = 2550.0 nM 5.59
CHEMBL4744297 — EC50 = 2590.0 nM 5.59
CHEMBL4763868 — EC50 = 2580.0 nM 5.59
CHEMBL4741962 — EC50 = 2920.0 nM 5.54
CHEMBL4760473 — EC50 = 3080.0 nM 5.51
CHEMBL4756962 — EC50 = 3060.0 nM 5.51
CHEMBL4743522 — EC50 = 3270.0 nM 5.49
CHEMBL4476647 — EC50 = 3270.0 nM 5.49
CHEMBL4797085 — EC50 = 3410.0 nM 5.47
CHEMBL4777330 — EC50 = 3500.0 nM 5.46
CHEMBL4776755 — EC50 = 3600.0 nM 5.44
CHEMBL4745335 — EC50 = 3710.0 nM 5.43
CHEMBL4752470 — EC50 = 4080.0 nM 5.39
CHEMBL4758990 — EC50 = 4190.0 nM 5.38
CHEMBL4747843 — EC50 = 4230.0 nM 5.37
CHEMBL4760540 — EC50 = 4400.0 nM 5.36