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

CHEMBL4473213

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
CC(C)(C)c1cc(NC(=O)Cc2ccc(-n3cnc4cc(-c5ccc(S(C)(=O)=O)cc5)ccc43)cc2)no1

Basic Information

ChEMBL ID CHEMBL4473213
Phase Preclinical
Structure Type MOL
InChI Key LMFNJXLDISVWLF-UHFFFAOYSA-N
7
Targets
14
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

528.6
MW (Da)
5.56
ALogP
7
HBA
1
HBD
107.1
PSA (Ų)
0.31
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H28N4O4S
MW 528.63
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -1.68

Activity Summary

IC50 14 meas. best 9.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 9.17 8.77 0.7 7
Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET
CHEMBL3430904
IC50 9.17 9.17 0.7 2
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 8.52 8.52 3.0 1
Unchecked
CHEMBL612545
IC50 8.51 8.51 3.1 1
High affinity nerve growth factor receptor
CHEMBL2815
IC50 7.5 7.5 32.0 1
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
IC50 7.34 7.34 46.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.12 5.12 7570.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 0.67 nM 9.17 Inhibition of RET isoform 9 C634W mutant in human TT cells assessed as reduction... 32298114
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 0.67 nM 9.17 Inhibition of RET isoform 9 M918T mutant in human MZ-CRC-1 cells assessed as red... 32298114
Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET IC50 = 0.67 nM 9.17 Inhibition of CCDC6/RET in human TPC1 cells assessed as reduction in cell prolif... 32298114
Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET IC50 = 0.67 nM 9.17 Inhibition of CCDC6/RET in human LC2/ad cells assessed as reduction in cell prol... 32298114
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 1.0 nM 9.0 Inhibition of recombinant human GST-tagged RET cytoplasmic domain (658 to 1114 r... 32298114
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 1.6 nM 8.8 Inhibition of RET isoform 15 M918T mutant (unknown origin) expressed in mouse BA... 32298114
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 1.7 nM 8.77 Inhibition of RET isoform 15 C634R mutant (unknown origin) expressed in mouse BA... 32298114
Vascular endothelial growth factor receptor 2 IC50 = 3.0 nM 8.52 Inhibition of recombinant human His-tagged VEGFR2 cytoplasmic domain (789 to 135... 32298114
Unchecked IC50 = 3.1 nM 8.51 Inhibition of NCOA4/RET isoform 15 (unknown origin) expressed in mouse BAF3 cell... 32298114
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 4.17 nM 8.38 Inhibition of RET isoform 9 C634R mutant (unknown origin) expressed in mouse NIH... 32298114
Proto-oncogene tyrosine-protein kinase receptor Ret IC50 = 8.0 nM 8.1 Inhibition of recombinant human N-terminal GST/His-tagged RET V804M mutant (658 ... 32298114
High affinity nerve growth factor receptor IC50 = 32.0 nM 7.5 Inhibition of recombinant human His-tagged TRKA cytoplasmic domain (441 to 796 r... 32298114
Macrophage colony-stimulating factor 1 receptor IC50 = 46.0 nM 7.34 Inhibition of recombinant human His-tagged CSF1R cytoplasmic domain (538 to 910 ... 32298114
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 7570.0 nM 5.12 Inhibition of human ERG expressed in HEK293 cells by patch clamp assay 32298114

Literature References

PubMed DOI Target Context # Activities
32298114 10.1021/acs.jmedchem.9b01336 Proto-oncogene tyrosine-protein kinase receptor Ret 35
32298114 10.1021/acs.jmedchem.9b01336 Unchecked 15
32298114 10.1021/acs.jmedchem.9b01336 Mus musculus 14
32298114 10.1021/acs.jmedchem.9b01336 ADMET 10
32298114 10.1021/acs.jmedchem.9b01336 Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET 8
32298114 10.1021/acs.jmedchem.9b01336 SHC-transforming protein 1 6
32298114 10.1021/acs.jmedchem.9b01336 GTPase HRas 2
32298114 10.1021/acs.jmedchem.9b01336 Centrosomal protein 43/RET 2
32298114 10.1021/acs.jmedchem.9b01336 High affinity nerve growth factor receptor 2
32298114 10.1021/acs.jmedchem.9b01336 Macrophage colony-stimulating factor 1 receptor 2
32298114 10.1021/acs.jmedchem.9b01336 Vascular endothelial growth factor receptor 2 2
32298114 10.1021/acs.jmedchem.9b01336 NT-3 growth factor receptor 1
32298114 10.1021/acs.jmedchem.9b01336 Voltage-gated inwardly rectifying potassium channel KCNH2 1
32298114 10.1021/acs.jmedchem.9b01336 MAP kinase-interacting serine/threonine-protein kinase 2 1
32298114 10.1021/acs.jmedchem.9b01336 Tyrosine-protein kinase Lyn 1
32298114 10.1021/acs.jmedchem.9b01336 Tyrosine-protein kinase HCK 1
32298114 10.1021/acs.jmedchem.9b01336 BaF3 1
32298114 10.1021/acs.jmedchem.9b01336 BCPAP 1
32298114 10.1021/acs.jmedchem.9b01336 PC-9 1
32298114 10.1021/acs.jmedchem.9b01336 A549 1

Data from ChEMBL 36 via Core Engine