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Compound Detail

CHEMBL4580220

BAY-3827
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CCc1ccccc1C(=O)Nc1n[nH]c2c(C)c(F)c(C3C(C#N)=C(C)N(C)C(C)=C3C#N)cc12

Basic Information

ChEMBL ID CHEMBL4580220
Name BAY-3827
Phase Preclinical
Structure Type MOL
InChI Key OZFFKOSQNBBYCA-UHFFFAOYSA-N
14
Targets
32
Activities
3
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

468.5
MW (Da)
5.45
ALogP
5
HBA
2
HBD
108.6
PSA (Ų)
0.53
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C27H25FN6O
MW 468.54
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.14

Activity Summary

IC50 22 meas. best 8.85
Ki 9 meas. best 6.66
EC50 1 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5'-AMP-activated protein kinase catalytic subunit alpha-1
CHEMBL4045
IC50 8.85 7.7429 1.4 7
5'-AMP-activated protein kinase catalytic subunit alpha-2
CHEMBL2116
IC50 8.15 8.15 7.0 1
Ribosomal protein S6 kinase alpha-1
CHEMBL2553
IC50 8.05 8.0433 9.0 3
Ribosomal protein S6 kinase alpha-2
CHEMBL3906
IC50 7.62 7.62 24.0 2
Ribosomal protein S6 kinase alpha-6
CHEMBL4924
IC50 7.44 7.44 36.0 1
Ribosomal protein S6 kinase alpha-5
CHEMBL4237
IC50 7.37 7.37 43.0 2
Ribosomal protein S6 kinase alpha-3
CHEMBL2345
IC50 7.28 7.28 52.0 2
Serine/threonine-protein kinase 24
CHEMBL5082
IC50 7.03 7.03 94.0 2
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 6.91 6.91 124.0 1
5'-AMP-activated protein kinase catalytic subunit alpha-1
CHEMBL4045
EC50 6.82 6.82 150.0 1
Unchecked
CHEMBL612545
Ki 6.66 6.655 218.8 2
4-aminobutyrate aminotransferase, mitochondrial
CHEMBL2044
Ki 6.65 6.65 222.4 1
Aurora kinase A
CHEMBL4722
IC50 6.32 6.32 480.0 1
D(1A) dopamine receptor
CHEMBL2056
Ki 6.2 6.2 631.0 3
Sigma intracellular receptor 2
CHEMBL4105907
Ki 5.55 5.55 2818.4 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5'-AMP-activated protein kinase catalytic subunit alpha-1 IC50 = 1.4 nM 8.85 Biochemical PRKAA1 assay with 10 µM ATP (Bayer in house) -
5'-AMP-activated protein kinase catalytic subunit alpha-2 IC50 = 7.0 nM 8.15 AMPKalpha2(h) Eurofins kinase panel -
5'-AMP-activated protein kinase catalytic subunit alpha-1 IC50 = 7.0 nM 8.15 Eurofins kinase panel (PRKAA1) -
5'-AMP-activated protein kinase catalytic subunit alpha-1 IC50 = 7.0 nM 8.15 Affinity Biochemical interaction: (Enzymatic inhibition assay) EUB0000311b PRKAA... -
Ribosomal protein S6 kinase alpha-1 IC50 = 9.0 nM 8.05 Rsk1(h) Eurofins kinase panel -
Ribosomal protein S6 kinase alpha-1 IC50 = 9.1 nM 8.04 Eurofins kinase panel (RPS6KA1) -
Ribosomal protein S6 kinase alpha-1 IC50 = 9.1 nM 8.04 Affinity Biochemical interaction: (Enzymatic inhibition assay) EUB0000311b RPS6K... -
5'-AMP-activated protein kinase catalytic subunit alpha-1 IC50 = 10.0 nM 8.0 AMPKalpha1(h) Eurofins kinase panel -
5'-AMP-activated protein kinase catalytic subunit alpha-1 IC50 = 15.0 nM 7.82 Biochemical PRKAA1 assay with 2 mM ATP (Bayer in house) -
Ribosomal protein S6 kinase alpha-2 IC50 = 24.0 nM 7.62 Rsk3(h) Eurofins kinase panel -
Ribosomal protein S6 kinase alpha-2 IC50 = 24.0 nM 7.62 Selectivity interaction (Kinase panel (Eurofins, enzymatic assay)) EUB0000311b R... -
Ribosomal protein S6 kinase alpha-6 IC50 = 36.0 nM 7.44 Selectivity interaction (Kinase panel (Eurofins, enzymatic assay)) EUB0000311b R... -
Ribosomal protein S6 kinase alpha-5 IC50 = 43.0 nM 7.37 MSK1(h) Eurofins kinase panel -
Ribosomal protein S6 kinase alpha-5 IC50 = 43.0 nM 7.37 Selectivity interaction (Kinase panel (Eurofins, enzymatic assay)) EUB0000311b R... -
Ribosomal protein S6 kinase alpha-3 IC50 = 52.0 nM 7.28 Selectivity interaction (Kinase panel (Eurofins, enzymatic assay)) EUB0000311b R... -
Ribosomal protein S6 kinase alpha-3 IC50 = 52.0 nM 7.28 Rsk2(h) Eurofins kinase panel -
Serine/threonine-protein kinase 24 IC50 = 94.0 nM 7.03 MST3(h) Eurofins kinase panel -
Serine/threonine-protein kinase 24 IC50 = 94.0 nM 7.03 Selectivity interaction (Kinase panel (Eurofins, enzymatic assay)) EUB0000311b S... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 124.0 nM 6.91 Selectivity interaction (Kinase panel (Eurofins, enzymatic assay)) EUB0000311b F... -
5'-AMP-activated protein kinase catalytic subunit alpha-1 EC50 = 150.0 nM 6.82 Affinity Phenotypic Cellular interaction: (Cellular mechanistic pACC assay using... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4507319 Tyrosine-protein kinase ABL1 16
- 10.6019/CHEMBL4507319 Epidermal growth factor receptor 13
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL4507319 Receptor-type tyrosine-protein kinase FLT3 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL4507319 Unchecked 11
- 10.6019/CHEMBL4507319 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL5465560 Receptor-type tyrosine-protein kinase FLT3 10
- 10.6019/CHEMBL4507319 Mast/stem cell growth factor receptor Kit 10
- 10.6019/CHEMBL4507319 5'-AMP-activated protein kinase catalytic subunit alpha-1 8
- 10.6019/CHEMBL5303304 HEK-293T 7
- 10.6019/CHEMBL5303304 U2OS 7
- 10.6019/CHEMBL5058564 Fibroblast 6
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.6019/CHEMBL5058564 HEK-293T 5
- 10.6019/CHEMBL4507319 Proto-oncogene tyrosine-protein kinase receptor Ret 5
- 10.6019/CHEMBL4507319 Ribosomal protein S6 kinase alpha-1 5
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL4507319 Hepatocyte growth factor receptor 4
- 10.6019/CHEMBL4507319 ALK tyrosine kinase receptor 4

Data from ChEMBL 36 via Core Engine