Compound Detail

CHEMBL1289601

LENVATINIB

💊 Approved Drug

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💊 Approved Drug

COc1cc2nccc(Oc3ccc(NC(=O)NC4CC4)c(Cl)c3)c2cc1C(N)=O

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL1289601
Name	LENVATINIB
Phase	Approved
Structure Type	MOL
InChI Key	WOSKHXYHFSIKNG-UHFFFAOYSA-N
Therapeutic	✓ Yes

Known Names

E-7080 ER-203492-00 Kisplyx Lenvatinib

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Molecular Properties

426.9

MW (Da)

4.07

ALogP

HBA

HBD

115.6

PSA (Å²)

0.55

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
First Approval	2015
Availability	Prescription
Chirality	Achiral

Routes of Administration

Oral

Flags

Natural Product

USAN Stem	-tinib
USAN Year	2010

Extended Properties

Molecular Formula	C21H19ClN4O4
MW	426.86
Aromatic Rings	3
Heavy Atoms	30
NP-Likeness	-1.35

Indications

Neoplasms Neoplasms Carcinoma, Hepatocellular Carcinoma, Non-Small-Cell Lung Carcinoma, Renal Cell Carcinoma, Renal Cell Carcinoma, Renal Cell Carcinoma, Renal Cell Carcinoma, Squamous Cell Cholangiocarcinoma Cholangiocarcinoma Colorectal Neoplasms Endometrial Neoplasms Endometrial Neoplasms Endometrial Neoplasms Esophageal Neoplasms Esophageal Neoplasms Melanoma Thyroid Neoplasms Thyroid Neoplasms

ATC Classification

L01EX08

lenvatinib

Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Level 2: ANTINEOPLASTIC AGENTS

Activity Summary

IC50 31 meas. best 9.15

Kd 23 meas. best 8.68

Ki 3 meas. best 8.82

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Vascular endothelial growth factor receptor 2 CHEMBL279	IC50	9.15	8.4938	0.7	8
Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041	Ki	8.82	8.82	1.5	2
Fibroblast growth factor receptor 4 CHEMBL3973	IC50	8.72	7.615	1.9	2
Vascular endothelial growth factor receptor 2 CHEMBL279	Kd	8.68	8.68	2.1	1
HUVEC CHEMBL613979	IC50	8.52	8.49	3.0	2
BaF3 CHEMBL614524	IC50	8.49	8.49	3.2	1
Vascular endothelial growth factor receptor 3 CHEMBL1955	IC50	8.28	8.28	5.2	4
Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041	Kd	8.05	8.05	9.0	1
Coiled-coil domain-containing protein 6/Tyrosine-protein kinase receptor RET CHEMBL3430904	IC50	8.0	8.0	10.0	1
Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET CHEMBL3430888	IC50	8.0	8.0	10.0	1
Proto-oncogene tyrosine-protein kinase receptor Ret /Nuclear receptor coactivator 4 fusion protein CHEMBL3430877	IC50	8.0	8.0	10.0	1
Receptor-interacting serine/threonine-protein kinase 2 CHEMBL5014	Kd	7.96	7.96	11.0	1
Fibroblast growth factor receptor 2 CHEMBL4142	IC50	7.96	7.96	11.0	1
Vascular endothelial growth factor receptor 1 CHEMBL1868	IC50	7.66	7.66	22.0	3
Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041	IC50	7.46	7.46	35.0	1
Platelet-derived growth factor receptor beta CHEMBL1913	IC50	7.41	7.41	39.0	1
Epithelial discoidin domain-containing receptor 1 CHEMBL5319	Kd	7.34	7.34	46.0	1
Platelet-derived growth factor receptor alpha CHEMBL2007	IC50	7.29	7.29	51.0	1
MAP kinase-activated protein kinase 2 CHEMBL2208	Kd	7.2	7.2	63.0	1
Fibroblast growth factor receptor 1 CHEMBL3650	IC50	7.18	7.18	66.0	1
Carbonic anhydrase 5A, mitochondrial CHEMBL4789	Ki	6.88	6.88	132.7	1
Protein-tyrosine kinase 6 CHEMBL4601	Kd	6.76	6.76	173.0	1
Discoidin domain-containing receptor 2 CHEMBL5122	Kd	6.66	6.66	218.0	1
Mitogen-activated protein kinase 14 CHEMBL260	Kd	6.66	6.66	217.0	1
Platelet-derived growth factor receptor beta CHEMBL1913	Kd	6.5	6.5	316.0	1
Receptor-interacting serine/threonine-protein kinase 3 CHEMBL1795199	Kd	6.5	6.5	316.0	1
TRAF2 and NCK-interacting protein kinase CHEMBL4527	Kd	6.25	6.25	565.0	1
Mitogen-activated protein kinase kinase kinase kinase 2 CHEMBL5330	Kd	6.24	6.24	578.0	1
Hep 3B2 CHEMBL4296437	IC50	6.16	6.16	696.2	1
Serine/threonine-protein kinase 10 CHEMBL3981	Kd	6.1	6.1	793.0	1
Huh-7 CHEMBL614039	IC50	6.07	6.07	850.9	1
Ribosyldihydronicotinamide dehydrogenase [quinone] CHEMBL3959	Kd	5.82	5.82	1523.0	1
Mitogen-activated protein kinase kinase kinase 6 CHEMBL1163123	Kd	5.8	5.8	1575.0	1
Aurora kinase B CHEMBL2185	Kd	5.75	5.75	1781.0	1
Serine/threonine-protein kinase/endoribonuclease IRE1 CHEMBL1163101	Kd	5.65	5.65	2242.0	1
Ferrochelatase, mitochondrial CHEMBL3879831	Kd	5.55	5.55	2806.0	1
Dual specificity mitogen-activated protein kinase kinase 5 CHEMBL4948	Kd	5.54	5.54	2910.0	1
Mitogen-activated protein kinase kinase kinase kinase 5 CHEMBL4852	Kd	5.51	5.51	3117.0	1
Tyrosine-protein kinase ABL1 CHEMBL1862	Kd	5.42	5.42	3771.0	1
STE20-like serine/threonine-protein kinase CHEMBL4202	Kd	5.41	5.41	3851.0	1
Breakpoint cluster region protein CHEMBL5146	Kd	5.39	5.39	4113.0	1
HCCLM3 CHEMBL5465453	IC50	4.56	4.56	27810.0	1

Pharmacokinetic Data

Parameter	Value	Units	Species
CL	74.1	mL.min-1.g-1	Homo sapiens
T1/2	0.3733	hr	Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Vascular endothelial growth factor receptor 2	IC50	=	0.7	nM	9.15	Inhibition of human N-terminal GST-tagged VEGFR2 cytoplasmic domain (790 to 1356...	31096155
Proto-oncogene tyrosine-protein kinase receptor Ret	Ki	=	1.5	nM	8.82	Binding affinity to full length human recombinant RET assessed as inhibition con...	38484122
Proto-oncogene tyrosine-protein kinase receptor Ret	Ki	=	1.5	nM	8.82	Inhibition of RET (unknown origin)	25625428
Fibroblast growth factor receptor 4	IC50	=	1.9	nM	8.72	Inhibition of FGFR4 (unknown origin) incubated for 10 mins followed by substrate...	37335602
Vascular endothelial growth factor receptor 2	Kd	=	2.1	nM	8.68	Binding affinity to VEGFR2 (unknown origin) by proteros reporter displacement as...	25589937
HUVEC	IC50	=	3.0	nM	8.52	Inhibition of VEGF-induced cell proliferation of HUVEC incubated for 72 hrs by b...	31096155
BaF3	IC50	=	3.23	nM	8.49	Antiproliferative activity against VEGFR2-transformed mouse BaF3 cells assessed ...	37429211
HUVEC	IC50	=	3.47	nM	8.46	Antiproliferative activity against VEGF-stimulated HUVEC assessed as inhibition ...	37429211
Vascular endothelial growth factor receptor 2	IC50	=	4.0	nM	8.4	Inhibition of VEGFR2 (unknown origin)	34351741
Vascular endothelial growth factor receptor 2	IC50	=	4.0	nM	8.4	Inhibition of human recombinant VEGFR2 (805 to 1356 residues) in presence of ATP...	39026631
Vascular endothelial growth factor receptor 2	IC50	=	4.0	nM	8.4	Inhibition of VEGFR2 (unknown origin)	33429247
Vascular endothelial growth factor receptor 2	IC50	=	4.0	nM	8.4	Inhibition of VEGFR2 (unknown origin)	31306818
Vascular endothelial growth factor receptor 2	IC50	=	4.0	nM	8.4	Inhibition of human VEGFR2	29189002
Vascular endothelial growth factor receptor 2	IC50	=	4.0	nM	8.4	Inhibition of VEGFR2	23098265
Vascular endothelial growth factor receptor 2	IC50	=	4.0	nM	8.4	Inhibition of recombinant VEGFR2 after 1 hr by fluorescence polarization assay	20869793
Vascular endothelial growth factor receptor 3	IC50	=	5.2	nM	8.28	Inhibition of VEGFR3	23098265
Vascular endothelial growth factor receptor 3	IC50	=	5.2	nM	8.28	Inhibition of VEGFR3 (unknown origin)	34351741
Vascular endothelial growth factor receptor 3	IC50	=	5.2	nM	8.28	Inhibition of VEGFR3 (unknown origin)	31306818
Vascular endothelial growth factor receptor 3	IC50	=	5.2	nM	8.28	Inhibition of VEGFR3 (unknown origin)	33429247
Proto-oncogene tyrosine-protein kinase receptor Ret	Kd	=	9.0	nM	8.05	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ...	29191878

Literature References

PubMed	DOI	Target Context	# Activities
39136667	10.1021/acs.jnatprod.4c00406	Lenvatinib-resistant Huh7/Len	9
38919032	10.1021/acs.jmedchem.4c00242	MHCC97H	9
38919032	10.1021/acs.jmedchem.4c00242	HCCLM3	9
39136667	10.1021/acs.jnatprod.4c00406	ADMET	8
29191878	10.1126/science.aan4368	Unchecked	5
39136667	10.1021/acs.jnatprod.4c00406	Lenvatinib-resistant Hep3B/Len	5
39136667	10.1021/acs.jnatprod.4c00406	Lenvatinib-resistant HCC/Len	4
-	10.6019/CHEMBL4495565	SARS-CoV-2	4
37335602	10.1021/acs.jmedchem.3c00455	ADMET	3
-	10.6019/CHEMBL4808148	Histone deacetylase 6	2
-	10.6019/CHEMBL4651402	SARS-CoV-2	2
25589937	10.1021/ml500394m	Vascular endothelial growth factor receptor 2	2
37468498	10.1038/s41467-023-40064-9	Prostaglandin G/H synthase 1	2
37468498	10.1038/s41467-023-40064-9	Alpha-1A adrenergic receptor	2
37468498	10.1038/s41467-023-40064-9	Thromboxane A2 receptor	2
37335602	10.1021/acs.jmedchem.3c00455	Fibroblast growth factor receptor 4	2
37468498	10.1038/s41467-023-40064-9	Muscarinic acetylcholine receptor M1	2
-	10.6019/CHEMBL4495564	Replicase polyprotein 1ab	2
25625428	10.1021/jm501464c	Proto-oncogene tyrosine-protein kinase receptor Ret	1
29191878	10.1126/science.aan4368	Acyl-CoA dehydrogenase family member 10	1

Data from ChEMBL 36 via Core Engine