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Compound Detail

CHEMBL2323775

MK-8033
Phase I
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Phase I
Cn1cc(-c2cnc3ccc4ccc(CS(=O)(=O)NCc5ccccn5)cc4c(=O)c3c2)cn1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL2323775
Name MK-8033
Phase Phase I
Structure Type MOL
InChI Key VMJFTOSOFDEKTM-UHFFFAOYSA-N

Known Names

Mk-8033 MK8033
7
Targets
22
Activities
2
Assay Types
6
PK Parameters
20
Publications
2
Known Names
1
Indications
2
Mechanisms

Molecular Properties

471.5
MW (Da)
3.16
ALogP
7
HBA
1
HBD
106.8
PSA (Ų)
0.41
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Flags

Chemical Probe

Extended Properties

Molecular Formula C25H21N5O3S
MW 471.54
Aromatic Rings 5
Heavy Atoms 34
NP-Likeness -1.77

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Hepatocyte growth factor receptor inhibitor INHIBITOR Hepatocyte growth factor receptor ✓ ✓
Macrophage-stimulating protein receptor inhibitor INHIBITOR Macrophage-stimulating protein receptor ✓ ✓

Indications

Neoplasms

Activity Summary

IC50 17 meas. best 9.22
Kd 5 meas. best 8.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatocyte growth factor receptor
CHEMBL3717
 IC50 9.22 8.5378 0.6 9
Hepatocyte growth factor receptor
CHEMBL3717
 Kd 8.49 7.7533 3.2 3
Macrophage-stimulating protein receptor
CHEMBL2689
 IC50 8.15 8.15 7.0 3
Macrophage-stimulating protein receptor
CHEMBL2689
 Kd 6.02 6.02 956.0 1
Mus musculus
CHEMBL375
 IC50 5.89 5.83 1300.0 2
Cytochrome P450 3A4
CHEMBL340
 IC50 4.94 4.94 11580.0 1
Cytochrome P450 2C9
CHEMBL3397
 IC50 4.83 4.83 14730.0 1
Ferrochelatase, mitochondrial
CHEMBL3879831
 Kd 4.49 4.49 32640.0 1
Cytochrome P450 2D6
CHEMBL289
 IC50 4.34 4.34 46170.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3.1 mL.min-1.kg-1 Canis lupus familiaris
CL 20.0 mL.min-1.kg-1 Rattus norvegicus
F 33.0 % Canis lupus familiaris
F 35.0 % Rattus norvegicus
T1/2 3.1 hr Canis lupus familiaris
T1/2 0.8 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hepatocyte growth factor receptor IC50 = 0.6 nM 9.22 Inhibition of c-MET Y1230H mutant (unknown origin) 23379595
Hepatocyte growth factor receptor IC50 = 0.6 nM 9.22 Inhibition of c-MET Y1235D mutant (unknown origin) 23379595
Hepatocyte growth factor receptor IC50 = 1.0 nM 9.0 Inhibition of c-MET Y1230C mutant (unknown origin) 23379595
Hepatocyte growth factor receptor IC50 = 1.0 nM 9.0 Inhibition of c-MET (unknown origin)-catalyzed N-biotinylated EQEDEPEGDYFEWLECON... 23379595
Hepatocyte growth factor receptor IC50 = 1.0 nM 9.0 Inhibition of c-Met (unknown origin) 35763868
Hepatocyte growth factor receptor IC50 = 1.2 nM 8.92 Inhibition of c-MET M1250T mutant (unknown origin) 23379595
Hepatocyte growth factor receptor IC50 = 2.0 nM 8.7 Inhibition of c-MET N1100Y mutant (unknown origin) 23379595
Hepatocyte growth factor receptor Kd = 3.2 nM 8.49 Binding affinity to phosphorylated c-MET kinase domain (unknown origin) 23379595
Macrophage-stimulating protein receptor IC50 = 7.0 nM 8.15 Inhibition of RON (unknown origin) by TR-FRET assay 23379595
Macrophage-stimulating protein receptor IC50 = 7.0 nM 8.15 Inhibition of RON (unknown origin) 30530193
Macrophage-stimulating protein receptor IC50 = 7.0 nM 8.15 Inhibition of RON (unknown origin) 35763868
Hepatocyte growth factor receptor Kd = 10.4 nM 7.98 Binding affinity to unphosphorylated c-MET kinase domain (unknown origin) 23379595
Hepatocyte growth factor receptor IC50 = 29.0 nM 7.54 Inhibition of HGF-stimulated c-MET (unknown origin) autophosphorylation at tyros... 23379595
Hepatocyte growth factor receptor Kd = 161.0 nM 6.79 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878
Hepatocyte growth factor receptor IC50 = 582.0 nM 6.24 Inhibition of c-MET (unknown origin) expressed in human GTL16 cells assessed as ... 23379595
Macrophage-stimulating protein receptor Kd = 956.0 nM 6.02 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878
Mus musculus IC50 = 1300.0 nM 5.89 In vivo inhibition of c-MET phosphorylation at tyrosine Y1349 in human GTL16 cel... 23379595
Mus musculus IC50 = 1700.0 nM 5.77 In vivo inhibition of c-MET phosphorylation at tyrosine Y1349 in human GTL16 cel... 23379595
Cytochrome P450 3A4 IC50 = 11580.0 nM 4.94 Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate b... 23379595
Cytochrome P450 2C9 IC50 = 14730.0 nM 4.83 Inhibition of CYP2C9 (unknown origin) 23379595

Literature References

PubMed DOI Target Context # Activities
23379595 10.1021/jm301619u Hepatocyte growth factor receptor 14
- 10.6019/CHEMBL5303304 HEK-293T 8
- 10.6019/CHEMBL5303304 U2OS 6
23379595 10.1021/jm301619u NON-PROTEIN TARGET 6
29191878 10.1126/science.aan4368 Unchecked 5
23379595 10.1021/jm301619u Cytochrome P450 3A4 4
23379595 10.1021/jm301619u Canis familiaris 4
23379595 10.1021/jm301619u Rattus norvegicus 4
- 10.6019/CHEMBL5303304 Fibroblast 4
23379595 10.1021/jm301619u Mus musculus 4
23379595 10.1021/jm301619u Macrophage-stimulating protein receptor 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
23379595 10.1021/jm301619u Vascular endothelial growth factor receptor 3 1
23379595 10.1021/jm301619u Fibroblast growth factor receptor 3 1
23379595 10.1021/jm301619u Tyrosine-protein kinase Mer 1
23379595 10.1021/jm301619u Cytochrome P450 2D6 1
23379595 10.1021/jm301619u Cytochrome P450 2C9 1
35763868 10.1016/j.ejmech.2022.114561 Macrophage-stimulating protein receptor 1
29191878 10.1126/science.aan4368 Acyl-CoA dehydrogenase family member 10 1

Data from ChEMBL 36 via Core Engine