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Compound Detail

CHEMBL3188267

CAPMATINIB
💊 Approved Drug
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💊 Approved Drug
CNC(=O)c1ccc(-c2cnc3ncc(Cc4ccc5ncccc5c4)n3n2)cc1F
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL3188267
Name CAPMATINIB
Phase Approved
Structure Type MOL
InChI Key LIOLIMKSCNQPLV-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

Capmatinib INC-280 INC280 Incb-28060 INCB-28060 FREE BASE NVP-INC280 NVP-INC280-NX NYP-INC280-NX
5
Targets
9
Activities
2
Assay Types
0
PK Parameters
20
Publications
8
Known Names
12
Indications
1
Mechanisms

Molecular Properties

412.4
MW (Da)
3.43
ALogP
6
HBA
1
HBD
85.1
PSA (Ų)
0.49
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2020
Availability Prescription
Chirality Achiral

Routes of Administration

Oral

Flags

Chemical Probe
USAN Stem -tinib
USAN Year 2016

Extended Properties

Molecular Formula C23H17FN6O
MW 412.43
Aromatic Rings 5
Heavy Atoms 31
NP-Likeness -1.54

Mechanism of Action

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

Indications

Neoplasms Neoplasms Carcinoma, Non-Small-Cell Lung Sarcoma Carcinoma, Hepatocellular Kidney Neoplasms Lung Neoplasms Melanoma Melanoma Breast Neoplasms Glioblastoma Liver Diseases

ATC Classification

L01EX17
capmatinib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS

Activity Summary

IC50 7 meas. best 9.89
Kd 2 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatocyte growth factor receptor
CHEMBL3717
 IC50 9.89 9.7675 0.1 4
Hepatocyte growth factor receptor
CHEMBL3717
 Kd 9.52 9.52 0.3 1
EBC-1
CHEMBL4296411
 IC50 8.92 8.92 1.2 1
NCI-H1993
CHEMBL1075527
 IC50 8.64 8.64 2.3 1
SNU-5
CHEMBL614934
 IC50 8.57 8.57 2.7 1
Cyclin-dependent kinase-like 5
CHEMBL1163112
 Kd 5.69 5.69 2042.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hepatocyte growth factor receptor IC50 = 0.13 nM 9.89 Inhibition of c-Met (unknown origin) 26717201
Hepatocyte growth factor receptor IC50 = 0.13 nM 9.89 Inhibition of c-Met (unknown origin) 35763868
Hepatocyte growth factor receptor IC50 = 0.13 nM 9.89 Inhibition of MET (unknown origin) 37262349
Hepatocyte growth factor receptor Kd = 0.3 nM 9.52 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878
Hepatocyte growth factor receptor IC50 = 0.4 nM 9.4 Inhibition of c-MET (unknown origin) using TK substrate-biotin peptide as substr... 28411455
EBC-1 IC50 = 1.2 nM 8.92 Antiproliferative activity against human EBC-1 cells 38169272
NCI-H1993 IC50 = 2.3 nM 8.64 Growth inhibition of human NCI-H1993 cells after 72 hrs by CCK-8 assay 28411455
SNU-5 IC50 = 2.7 nM 8.57 Growth inhibition of human SNU5 cells after 72 hrs by CCK-8 assay 28411455
Cyclin-dependent kinase-like 5 Kd = 2042.0 nM 5.69 Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... 29191878

Literature References

PubMed DOI Target Context # Activities
29191878 10.1126/science.aan4368 Unchecked 5
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 2
37657268 10.1016/j.ejmech.2023.115758 Replicase polyprotein 1ab 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
29191878 10.1126/science.aan4368 Activin receptor type-1 1
29191878 10.1126/science.aan4368 Beta-adrenergic receptor kinase 1 1
29191878 10.1126/science.aan4368 Adenosine kinase 1
37657268 10.1016/j.ejmech.2023.115758 Spike glycoprotein 1
29191878 10.1126/science.aan4368 AarF domain-containing protein kinase 1 1
29191878 10.1126/science.aan4368 Activin receptor type-1-like 1
29191878 10.1126/science.aan4368 Activin receptor type-2B 1
29191878 10.1126/science.aan4368 Activin receptor type-1B 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 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
29191878 10.1126/science.aan4368 Tyrosine-protein kinase ABL1 1

Data from ChEMBL 36 via Core Engine