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Assay Detail

CHEMBL4386830

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

Binding
Inhibition of KIX-RLucN fused CBP (unknown origin) binding to KID-RLucC fused CREB (unknown origin) transfected in human HEK293 cells preincubated with compound 30 mins before before forskolin addition and measured after 90 mins in presence of coelenterazine by split Renilla luciferase complementation assay
12
Total Activities
12
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

SAR optimization studies on modified salicylamides as a potential treatment for acute myeloid leukemia through inhibition of the CREB pathway.
Chae HD, Cox N, Capolicchio S, Lee JW, Horikoshi N, Kam S, Ng AA, Edwards J, Butler TL, Chan J, Lee Y, Potter G, Capece MC, Liu CW, Wakatsuki S, Smith M, Sakamoto KM.
Bioorg Med Chem Lett (2019) 29 : 2307 -2315
PubMed 31253529 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.66 5.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2313117 1 5.91
CHEMBL4589141 1 5.82
CHEMBL1448 NICLOSAMIDE 4.0 1 5.82
CHEMBL4467546 1 5.81
CHEMBL2338696 1 5.60
CHEMBL4551427 1 5.52
CHEMBL584646 1 5.40
CHEMBL65742 1 5.39
CHEMBL4442963 1 -
CHEMBL4533737 1 -
CHEMBL4468001 1 -
CHEMBL4543954 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2313117 IC50 = 1240.0 nM 5.91
CHEMBL4589141 IC50 = 1520.0 nM 5.82
CHEMBL1448 NICLOSAMIDE IC50 = 1530.0 nM 5.82
CHEMBL4467546 IC50 = 1550.0 nM 5.81
CHEMBL2338696 IC50 = 2530.0 nM 5.60
CHEMBL4551427 IC50 = 3030.0 nM 5.52
CHEMBL584646 IC50 = 3990.0 nM 5.40
CHEMBL65742 IC50 = 4030.0 nM 5.39
CHEMBL4442963 IC50 > 7000.0 nM -
CHEMBL4533737 IC50 > 7000.0 nM -
CHEMBL4468001 IC50 > 7000.0 nM -
CHEMBL4543954 IC50 > 7000.0 nM -