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Compound Detail

CHEMBL4591082

SR-302
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CS(=O)(=O)N1CCCC(NC(=O)[C@H](CCC2CCCCC2)NC(=O)c2ccc(CNC(=O)c3cnc4ccccn34)cc2)C1

Basic Information

ChEMBL ID CHEMBL4591082
Name SR-302
Phase Preclinical
Structure Type MOL
InChI Key WGMNFJAFXXXRLZ-GEVKEYJPSA-N
4
Targets
24
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

622.8
MW (Da)
3.26
ALogP
7
HBA
3
HBD
142.0
PSA (Ų)
0.30
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C32H42N6O5S
MW 622.79
Aromatic Rings 3
Heavy Atoms 44
NP-Likeness -1.49

Activity Summary

IC50 24 meas. best 9.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Discoidin domain-containing receptor 2
CHEMBL5122
IC50 9.12 8.2067 0.8 6
Mitogen-activated protein kinase 14
CHEMBL260
IC50 8.21 7.3367 6.2 6
Epithelial discoidin domain-containing receptor 1
CHEMBL5319
IC50 7.64 7.5167 23.0 6
Mitogen-activated protein kinase 11
CHEMBL3961
IC50 7.35 6.9233 45.1 6

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Discoidin domain-containing receptor 2 IC50 = 0.75 nM 9.12 Affinity Biochemical interaction (Enzyme kinetic assay (Reaction Biology)) EUB00... -
Discoidin domain-containing receptor 2 IC50 = 0.75 nM 9.12 Enzyme kinetic assay (Reaction Biology) (DDR2) -
Mitogen-activated protein kinase 14 IC50 = 6.2 nM 8.21 Enzyme kinetic assay (Reaction Biology) (MAPK14) -
Mitogen-activated protein kinase 14 IC50 = 6.2 nM 8.21 Affinity Biochemical interaction (Enzyme kinetic assay (Reaction Biology)) EUB00... -
Discoidin domain-containing receptor 2 IC50 = 18.0 nM 7.75 NanoBRET (SGC-Frankfurt) (DDR2) -
Discoidin domain-containing receptor 2 IC50 = 18.0 nM 7.75 Inhibition of DDR2 (unknown origin) expressed in HEK293T cells using NanoBRET Na... 34506142
Discoidin domain-containing receptor 2 IC50 = 18.0 nM 7.75 Cellular target engagement assay with: DDR2 -
Discoidin domain-containing receptor 2 IC50 = 18.0 nM 7.75 Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000... -
Epithelial discoidin domain-containing receptor 1 IC50 = 23.0 nM 7.64 NanoBRET (SGC-Frankfurt) (DDR1) -
Epithelial discoidin domain-containing receptor 1 IC50 = 23.0 nM 7.64 Inhibition of DDR1 (unknown origin) expressed in HEK293T cells using NanoBRET Na... 34506142
Epithelial discoidin domain-containing receptor 1 IC50 = 23.0 nM 7.64 Cellular target engagement assay with: DDR1 -
Epithelial discoidin domain-containing receptor 1 IC50 = 23.0 nM 7.64 Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000... -
Mitogen-activated protein kinase 11 IC50 = 45.1 nM 7.35 Enzyme kinetic assay (Reaction Biology) (MAPK11) -
Mitogen-activated protein kinase 11 IC50 = 45.1 nM 7.35 Affinity Biochemical interaction (Enzyme kinetic assay (Reaction Biology)) EUB00... -
Epithelial discoidin domain-containing receptor 1 IC50 = 53.3 nM 7.27 Enzyme kinetic assay (Reaction Biology) (DDR1) -
Epithelial discoidin domain-containing receptor 1 IC50 = 53.3 nM 7.27 Affinity Biochemical interaction (Enzyme kinetic assay (Reaction Biology)) EUB00... -
Mitogen-activated protein kinase 14 IC50 = 125.0 nM 6.9 NanoBRET (SGC-Frankfurt) (MAPK14) -
Mitogen-activated protein kinase 14 IC50 = 125.0 nM 6.9 Inhibition of p38alpha (unknown origin) expressed in HEK293T cells using NanoBRE... 34506142
Mitogen-activated protein kinase 14 IC50 = 125.0 nM 6.9 Cellular target engagement assay with: MAPK14 -
Mitogen-activated protein kinase 14 IC50 = 125.0 nM 6.9 Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4689842 Fibroblast 1272
- 10.6019/CHEMBL4689842 U2OS 1270
- 10.6019/CHEMBL4689842 HEK-293T 1270
- 10.6019/CHEMBL4507324 Tyrosine-protein kinase ABL1 16
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL4507324 Epidermal growth factor receptor 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL4507324 Receptor-type tyrosine-protein kinase FLT3 11
- 10.6019/CHEMBL4507324 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL4507324 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL4507324 Proto-oncogene tyrosine-protein kinase receptor Ret 4
34506142 10.1021/acs.jmedchem.1c00868 Mitogen-activated protein kinase 14 3
- 10.6019/CHEMBL4507324 Serine/threonine-protein kinase B-raf 3
- 10.6019/CHEMBL4507324 Ribosomal protein S6 kinase alpha-5 3
34506142 10.1021/acs.jmedchem.1c00868 Epithelial discoidin domain-containing receptor 1 3
- 10.6019/CHEMBL4507324 Mitogen-activated protein kinase 14 3
- 10.6019/CHEMBL4507324 Mitogen-activated protein kinase 11 3
- 10.6019/CHEMBL4507324 Discoidin domain-containing receptor 2 3

Data from ChEMBL 36 via Core Engine