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

CHEMBL496102

AMG-208
🧪 Phase II
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
🧪 Phase II
COc1ccc2c(OCc3nnc4ccc(-c5ccccc5)nn34)ccnc2c1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL496102
Name AMG-208
Phase Phase II
Structure Type MOL
InChI Key HEAIZQNMNCHNFD-UHFFFAOYSA-N

Known Names

Amg 208 Amg-208 Amg208
3
Targets
12
Activities
2
Assay Types
6
PK Parameters
20
Publications
3
Known Names
3
Indications
1
Mechanisms

Molecular Properties

383.4
MW (Da)
3.93
ALogP
7
HBA
0
HBD
74.4
PSA (Ų)
0.46
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Flags

Natural Product

Extended Properties

Molecular Formula C22H17N5O2
MW 383.41
Aromatic Rings 5
Heavy Atoms 29
NP-Likeness -1.70

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Hepatocyte growth factor receptor inhibitor INHIBITOR Hepatocyte growth factor receptor ✓ ✓

Indications

Prostatic Neoplasms, Castration-Resistant Neoplasms Neoplasms

Activity Summary

IC50 10 meas. best 8.05
Kd 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cAMP-dependent protein kinase catalytic subunit gamma
CHEMBL2743
 Kd 8.7 8.7 2.0 1
Hepatocyte growth factor receptor
CHEMBL3717
 IC50 8.05 7.8725 9.0 8
Hepatocyte growth factor receptor
CHEMBL3717
 Kd 7.55 7.55 28.0 1
Cytochrome P450 3A4
CHEMBL340
 IC50 5.39 4.945 4100.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 2517.0 ng.hr.mL-1 Rattus norvegicus
CL 131.0 mL.min-1.g-1 Rattus norvegicus
CL 122.0 mL.min-1.g-1 Mus musculus
CL 6.167 mL.min-1.kg-1 Rattus norvegicus
F 43.0 % Rattus norvegicus
T1/2 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
cAMP-dependent protein kinase catalytic subunit gamma Kd = 2.0 nM 8.7 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878
Hepatocyte growth factor receptor IC50 = 9.0 nM 8.05 Inhibition of c-Met by HTRF assay 18426196
Hepatocyte growth factor receptor IC50 = 9.0 nM 8.05 Inhibition of c-Met by HTRF assay 19819693
Hepatocyte growth factor receptor IC50 = 9.0 nM 8.05 Inhibition of human c-MET 21641696
Hepatocyte growth factor receptor IC50 = 9.0 nM 8.05 Inhibition of recombinant c-Met kinase domain (unknown origin) incubated for 30 ... 25699405
Hepatocyte growth factor receptor IC50 = 9.0 nM 8.05 Inhibition of c-Met (unknown origin) 26717201
Hepatocyte growth factor receptor IC50 = 9.0 nM 8.05 Inhibition of c-Met (unknown origin) using poly(Glu-Tyr) at 4:1 ratio as substra... 29157685
Hepatocyte growth factor receptor Kd = 28.0 nM 7.55 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878
Hepatocyte growth factor receptor IC50 = 46.0 nM 7.34 Inhibition of HGF-mediated c-Met phosphorylation in serum-starved human PC2 cell... 18426196
Hepatocyte growth factor receptor IC50 = 46.0 nM 7.34 Inhibition of HGF-mediated human c-Met autophosphorylation expressed in human PC... 19819693
Cytochrome P450 3A4 IC50 = 4100.0 nM 5.39 Inhibition of human CYP3A4 in human liver microsomes preincubated with NADPH 19819693
Cytochrome P450 3A4 IC50 = 32000.0 nM 4.5 Inhibition of human CYP3A4 19819693

Literature References

PubMed DOI Target Context # Activities
18426196 10.1021/jm800043g Rattus norvegicus 5
29191878 10.1126/science.aan4368 Unchecked 4
19819693 10.1016/j.bmcl.2009.09.096 Cytochrome P450 3A4 3
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
19819693 10.1016/j.bmcl.2009.09.096 Hepatocyte growth factor receptor 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
18426196 10.1021/jm800043g Hepatocyte growth factor receptor 2
29191878 10.1126/science.aan4368 Tyrosine-protein kinase ABL1 1
29191878 10.1126/science.aan4368 Actin-related protein 2 1
29191878 10.1126/science.aan4368 Long-chain-fatty-acid--CoA ligase 5 1
29191878 10.1126/science.aan4368 Peroxisomal acyl-coenzyme A oxidase 1 1
29191878 10.1126/science.aan4368 Very long-chain specific acyl-CoA dehydrogenase, mitochondrial 1
29191878 10.1126/science.aan4368 Acyl-CoA dehydrogenase family member 11 1
29191878 10.1126/science.aan4368 Acyl-CoA dehydrogenase family member 10 1
29191878 10.1126/science.aan4368 Tyrosine-protein kinase ABL2 1
29157685 10.1016/j.ejmech.2017.08.044 Hepatocyte growth factor receptor 1
26717201 10.1016/j.ejmech.2015.12.016 Hepatocyte growth factor receptor 1
25699405 10.1021/jm501913a Hepatocyte growth factor receptor 1
21641696 10.1016/j.ejmech.2011.05.031 Hepatocyte growth factor receptor 1
18426196 10.1021/jm800043g ADMET 1

Data from ChEMBL 36 via Core Engine