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Assay Detail

CHEMBL4030998

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

Binding
Inhibition of mouse GATA4/NKX2-5 transcriptional synergy expressed in African green monkey COS-1 cells measured after 30 hrs by dual luciferase reporter gene assay
ChEMBL ↗
81
Total Activities
80
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GATA4/NKX2-5 (CHEMBL4106137) ↗
Type PROTEIN COMPLEX
Organism Mus musculus

Publication

Discovery of Small Molecules Targeting the Synergy of Cardiac Transcription Factors GATA4 and NKX2-5.
Välimäki MJ, Tölli MA, Kinnunen SM, Aro J, Serpi R, Pohjolainen L, Talman V, Poso A, Ruskoaho HJ.
J Med Chem (2017) 60 : 7781 -7798
PubMed 28858485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 80 4.78 5.52
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361366 — — 2 5.52
CHEMBL4059969 — — 1 5.30
CHEMBL4078483 — — 1 5.30
CHEMBL4099820 — — 1 5.22
CHEMBL4089681 — — 1 5.16
CHEMBL3196347 — — 1 5.16
CHEMBL4061558 — — 1 5.16
CHEMBL4097402 — — 1 5.10
CHEMBL4076746 — — 1 5.10
CHEMBL4095086 — — 1 5.10
CHEMBL4095473 — — 1 5.05
CHEMBL4062678 — — 1 5.00
CHEMBL4081879 — — 1 5.00
CHEMBL4103231 — — 1 5.00
CHEMBL4100136 — — 1 4.96
CHEMBL4085301 — — 1 4.96
CHEMBL1381879 — — 1 4.89
CHEMBL4086394 — — 1 4.89
CHEMBL4083694 — — 1 4.80
CHEMBL4061938 — — 1 4.80
CHEMBL4070567 — — 1 4.77
CHEMBL4073403 — — 1 4.75
CHEMBL4076019 — — 1 4.72
CHEMBL4080486 — — 1 4.70
CHEMBL4098503 — — 1 4.70
CHEMBL1571383 — — 1 4.70
CHEMBL4076171 — — 1 4.70
CHEMBL4099211 — — 1 4.70
CHEMBL4081188 — — 1 4.70
CHEMBL4090632 — — 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361366 — IC50 = 3000.0 nM 5.52
CHEMBL4059969 — IC50 = 5000.0 nM 5.30
CHEMBL4078483 — IC50 = 5000.0 nM 5.30
CHEMBL4099820 — IC50 = 6000.0 nM 5.22
CHEMBL4089681 — IC50 = 7000.0 nM 5.16
CHEMBL3196347 — IC50 = 7000.0 nM 5.16
CHEMBL4061558 — IC50 = 7000.0 nM 5.16
CHEMBL4097402 — IC50 = 8000.0 nM 5.10
CHEMBL4076746 — IC50 = 8000.0 nM 5.10
CHEMBL4095086 — IC50 = 8000.0 nM 5.10
CHEMBL4095473 — IC50 = 9000.0 nM 5.05
CHEMBL4103231 — IC50 = 10000.0 nM 5.00
CHEMBL4081879 — IC50 = 10000.0 nM 5.00
CHEMBL4062678 — IC50 = 10000.0 nM 5.00
CHEMBL4085301 — IC50 = 11000.0 nM 4.96
CHEMBL4100136 — IC50 = 11000.0 nM 4.96
CHEMBL1381879 — IC50 = 13000.0 nM 4.89
CHEMBL4086394 — IC50 = 13000.0 nM 4.89
CHEMBL4083694 — IC50 = 16000.0 nM 4.80
CHEMBL4061938 — IC50 = 16000.0 nM 4.80
CHEMBL4070567 — IC50 = 17000.0 nM 4.77
CHEMBL4073403 — IC50 = 18000.0 nM 4.75
CHEMBL4076019 — IC50 = 19000.0 nM 4.72
CHEMBL1571383 — IC50 = 20000.0 nM 4.70
CHEMBL4078535 — IC50 = 20000.0 nM 4.70
CHEMBL4090632 — IC50 = 20000.0 nM 4.70
CHEMBL4081188 — IC50 = 20000.0 nM 4.70
CHEMBL4076171 — IC50 = 20000.0 nM 4.70
CHEMBL4098503 — IC50 = 20000.0 nM 4.70
CHEMBL4080486 — IC50 = 20000.0 nM 4.70
CHEMBL4099211 — IC50 = 20000.0 nM 4.70
CHEMBL493742 — IC50 = 21000.0 nM 4.68
CHEMBL151 LUTEOLIN IC50 = 22000.0 nM 4.66
CHEMBL4090787 — IC50 = 22000.0 nM 4.66
CHEMBL4069789 — IC50 = 23000.0 nM 4.64
CHEMBL4068091 — IC50 = 23000.0 nM 4.64
CHEMBL28 APIGENIN IC50 = 24000.0 nM 4.62
CHEMBL3193145 — IC50 = 24000.0 nM 4.62
CHEMBL4060038 — IC50 = 26000.0 nM 4.58
CHEMBL4068769 — IC50 = 28000.0 nM 4.55
CHEMBL4096074 — IC50 = 28000.0 nM 4.55
CHEMBL4067647 — IC50 = 30000.0 nM 4.52
CHEMBL3211162 — IC50 = 30000.0 nM 4.52
CHEMBL4060110 — IC50 = 32000.0 nM 4.50
CHEMBL4088348 — IC50 = 33000.0 nM 4.48
CHEMBL4103229 — IC50 = 37000.0 nM 4.43
CHEMBL4105226 — IC50 = 37000.0 nM 4.43
CHEMBL1348312 — IC50 = 38000.0 nM 4.42
CHEMBL4078962 — IC50 = 42000.0 nM 4.38
CHEMBL4079441 — IC50 = 50000.0 nM 4.30