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Compound Detail

CHEMBL3334567

SAVOLITINIB
🧪 Phase III
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🧪 Phase III
C[C@@H](c1ccc2nccn2c1)n1nnc2ncc(-c3cnn(C)c3)nc21
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL3334567
Name SAVOLITINIB
Phase Phase III
Structure Type MOL
InChI Key XYDNMOZJKOGZLS-NSHDSACASA-N

Known Names

Azd-6094 AZD6094 HMPL-504 Savolitinib Volitinib
4
Targets
8
Activities
2
Assay Types
6
PK Parameters
20
Publications
5
Known Names
14
Indications
1
Mechanisms

Molecular Properties

345.4
MW (Da)
1.88
ALogP
9
HBA
0
HBD
91.6
PSA (Ų)
0.50
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer

Flags

Natural Product
USAN Stem -tinib
USAN Year 2016

Extended Properties

Molecular Formula C17H15N9
MW 345.37
Aromatic Rings 5
Heavy Atoms 26
NP-Likeness -2.19

Mechanism of Action

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

Indications

Carcinoma, Non-Small-Cell Lung Carcinoma, Renal Cell Carcinoma, Renal Cell Urogenital Neoplasms Carcinoma Lung Neoplasms Prostatic Neoplasms, Castration-Resistant Pulmonary Disease, Chronic Obstructive Rectal Neoplasms Stomach Neoplasms Stomach Neoplasms Colorectal Neoplasms Neoplasms Neoplasms

Activity Summary

IC50 7 meas. best 8.7
Kd 1 meas. best 6.69

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatocyte growth factor receptor
CHEMBL3717
 IC50 8.7 8.002 2.0 5
MHCC97H
CHEMBL4296470
 IC50 8.61 8.61 2.5 1
NCI-H441
CHEMBL1075542
 IC50 8.22 8.22 6.0 1
Ribosyldihydronicotinamide dehydrogenase [quinone]
CHEMBL3959
 Kd 6.69 6.69 206.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 5594.0 ng.hr.mL-1 Mus musculus
CL 11.0 mL.min-1.kg-1 Mus musculus
Cmax 14323.77 nM Mus musculus
F 27.2 % Mus musculus
T1/2 1.7 hr Mus musculus
Vd 1.2 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hepatocyte growth factor receptor IC50 = 1.995 nM 8.7 Inhibition of c-Met phosphorylation at Tyr 1234/Tyr1235 residues in human NCI-H1... 31531204
MHCC97H IC50 = 2.46 nM 8.61 Antiproliferative activity against human MHCC97H cells assessed as reduction in ... 38086189
Hepatocyte growth factor receptor IC50 = 3.0 nM 8.52 Inhibition of c-Met autophosphorylation in human NCI-H441 cells for 1 hr by ELIS... 25148209
Hepatocyte growth factor receptor IC50 = 4.77 nM 8.32 Inhibition of c-Met (unknown origin) preincubated for 10 mins followed by substr... 38086189
Hepatocyte growth factor receptor IC50 = 5.0 nM 8.3 Inhibition of c-Met (unknown origin) using Poly E4Y substrate and ATP incubated ... 25148209
NCI-H441 IC50 = 6.0 nM 8.22 Antiproliferative activity against human NCI-H441 cells assessed as HGF-induced ... 25148209
Ribosyldihydronicotinamide dehydrogenase [quinone] Kd = 206.0 nM 6.69 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878
Hepatocyte growth factor receptor IC50 = 676.08 nM 6.17 Inhibition of N-terminal NH-tagged and avi-tagged dephosphorylated c-MET D1228V ... 31531204

Literature References

PubMed DOI Target Context # Activities
25148209 10.1021/jm500510f Mus musculus 8
31531204 10.1021/acsmedchemlett.9b00276 Hepatocyte growth factor receptor 8
29191878 10.1126/science.aan4368 Unchecked 4
25148209 10.1021/jm500510f NON-PROTEIN TARGET 4
25148209 10.1021/jm500510f ADMET 4
38086189 10.1016/j.ejmech.2023.116025 MHCC97H 3
31531204 10.1021/acsmedchemlett.9b00276 NCI-H1993 3
25148209 10.1021/jm500510f No relevant target 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
31531204 10.1021/acsmedchemlett.9b00276 Unchecked 2
25148209 10.1021/jm500510f Hepatocyte growth factor receptor 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
29191878 10.1126/science.aan4368 Very long-chain specific acyl-CoA dehydrogenase, mitochondrial 1
38086189 10.1016/j.ejmech.2023.116025 L02 1
29191878 10.1126/science.aan4368 Long-chain-fatty-acid--CoA ligase 5 1
29191878 10.1126/science.aan4368 Peroxisomal acyl-coenzyme A oxidase 3 1
29191878 10.1126/science.aan4368 Peroxisomal acyl-coenzyme A oxidase 1 1
29191878 10.1126/science.aan4368 Tyrosine-protein kinase ABL2 1
29191878 10.1126/science.aan4368 Tyrosine-protein kinase ABL1 1

Data from ChEMBL 36 via Core Engine