Compound Detail

CHEMBL2220486

LUCITANIB

🧪 Phase II

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🧪 Phase II

CNC(=O)c1cccc2cc(Oc3ccnc4cc(OCC5(N)CC5)c(OC)cc34)ccc12

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL2220486
Name	LUCITANIB
Phase	Phase II
Structure Type	MOL
InChI Key	CUDVHEFYRIWYQD-UHFFFAOYSA-N

Known Names

Al-3810 CO-3810 E-3810 Lucitanib S 80881 S-80881 S80881

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Mechanisms

Molecular Properties

443.5

MW (Da)

4.42

ALogP

HBA

HBD

95.7

PSA (Å²)

0.44

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
Chirality	Achiral

Flags

Natural Product

USAN Stem	-anib
USAN Year	2014

Extended Properties

Molecular Formula	C26H25N3O4
MW	443.50
Aromatic Rings	4
Heavy Atoms	33
NP-Likeness	-0.34

Mechanism of Action

Mechanism	Action Type	Target	Direct	Efficacy
Fibroblast growth factor receptor 1 inhibitor	INHIBITOR	Fibroblast growth factor receptor 1	✓	✓
Vascular endothelial growth factor receptor inhibitor	INHIBITOR	Vascular endothelial growth factor receptor	✓	✓
Fibroblast growth factor receptor 2 inhibitor	INHIBITOR	Fibroblast growth factor receptor 2	✓	✓

Indications

Breast Neoplasms Carcinoma, Non-Small-Cell Lung Lung Neoplasms Neoplasms Neoplasms Small Cell Lung Carcinoma Genital Neoplasms, Female

Activity Summary

IC50 21 meas. best 8.15

Kd 8 meas. best 8.3

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041	Kd	8.3	8.3	5.0	1
Vascular endothelial growth factor receptor 1 CHEMBL1868	IC50	8.15	8.15	7.0	4
Vascular endothelial growth factor receptor 3 CHEMBL1955	IC50	8.0	8.0	10.0	3
Epithelial discoidin domain-containing receptor 1 CHEMBL5319	Kd	7.85	7.85	14.0	1
Fibroblast growth factor receptor 1 CHEMBL3650	IC50	7.76	7.76	17.5	4
Vascular endothelial growth factor receptor 2 CHEMBL279	IC50	7.6	7.6	25.0	4
Fibroblast growth factor receptor 2 CHEMBL4142	IC50	7.08	7.08	82.5	4
Discoidin domain-containing receptor 2 CHEMBL5122	Kd	7.03	7.03	94.0	1
Receptor-interacting serine/threonine-protein kinase 2 CHEMBL5014	Kd	6.7	6.7	199.0	1
Fibroblast growth factor receptor 3 CHEMBL2742	IC50	6.62	6.62	237.5	1
Platelet-derived growth factor receptor beta CHEMBL1913	Kd	6.56	6.56	278.0	1
Tyrosine-protein kinase Lyn CHEMBL3905	Kd	5.56	5.56	2764.0	1
Pyridoxal kinase CHEMBL1075181	Kd	4.79	4.79	16404.0	1
B16-F10 CHEMBL612656	IC50	4.79	4.79	16300.0	1
Aurora kinase B CHEMBL2185	Kd	4.64	4.64	22852.0	1

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Proto-oncogene tyrosine-protein kinase receptor Ret	Kd	=	5.0	nM	8.3	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ...	29191878
Vascular endothelial growth factor receptor 1	IC50	=	7.0	nM	8.15	Inhibition of VEGFR1 (unknown origin)	29775937
Vascular endothelial growth factor receptor 1	IC50	=	7.0	nM	8.15	Inhibition of VEGFR1 (unknown origin)	34351741
Vascular endothelial growth factor receptor 1	IC50	=	7.0	nM	8.15	Inhibition of VEGFR1 (unknown origin) in the presence of ATP at Km concentration	33556787
Vascular endothelial growth factor receptor 1	IC50	=	7.0	nM	8.15	Inhibition of VEGFR1 (unknown origin)	27914362
Vascular endothelial growth factor receptor 3	IC50	=	10.0	nM	8.0	Inhibition of VEGFR3 (unknown origin)	27914362
Vascular endothelial growth factor receptor 3	IC50	=	10.0	nM	8.0	Inhibition of VEGFR3 (unknown origin)	34351741
Vascular endothelial growth factor receptor 3	IC50	=	10.0	nM	8.0	Inhibition of VEGFR3 (unknown origin) in the presence of ATP at Km concentration	33556787
Epithelial discoidin domain-containing receptor 1	Kd	=	14.0	nM	7.85	Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ...	29191878
Fibroblast growth factor receptor 1	IC50	=	17.5	nM	7.76	Inhibition of FGFR1 (unknown origin)	27914362
Fibroblast growth factor receptor 1	IC50	=	17.5	nM	7.76	Inhibition of FGFR1 (unknown origin)	29775937
Fibroblast growth factor receptor 1	IC50	=	17.5	nM	7.76	Inhibition of FGFR1 (unknown origin)	34351741
Fibroblast growth factor receptor 1	IC50	=	17.5	nM	7.76	Inhibition of FGFR1 (unknown origin) in the presence of ATP at Km concentration	33556787
Vascular endothelial growth factor receptor 2	IC50	=	25.0	nM	7.6	Inhibition of VEGFR2 (unknown origin) in the presence of ATP at Km concentration	33556787
Vascular endothelial growth factor receptor 2	IC50	=	25.0	nM	7.6	Inhibition of VEGFR2 (unknown origin)	34351741
Vascular endothelial growth factor receptor 2	IC50	=	25.0	nM	7.6	Inhibition of VEGFR2 (unknown origin)	29775937
Vascular endothelial growth factor receptor 2	IC50	=	25.0	nM	7.6	Inhibition of VEGFR2 (unknown origin)	27914362
Fibroblast growth factor receptor 2	IC50	=	82.5	nM	7.08	Inhibition of FGFR2 (unknown origin)	27914362
Fibroblast growth factor receptor 2	IC50	=	82.5	nM	7.08	Inhibition of FGFR2 (unknown origin)	29775937
Fibroblast growth factor receptor 2	IC50	=	82.5	nM	7.08	Inhibition of FGFR2 (unknown origin)	34351741

Literature References

PubMed	DOI	Target Context	# Activities
29191878	10.1126/science.aan4368	Unchecked	4
-	10.6019/CHEMBL4495565	SARS-CoV-2	4
-	10.6019/CHEMBL4495564	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	RAC-alpha serine/threonine-protein kinase	1
29191878	10.1126/science.aan4368	Adenylate kinase 2, mitochondrial	1
29191878	10.1126/science.aan4368	Adenosine kinase	1
29191878	10.1126/science.aan4368	Atypical kinase COQ8A, mitochondrial	1
29191878	10.1126/science.aan4368	AarF domain-containing protein kinase 1	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	Actin-related protein 2	1
29191878	10.1126/science.aan4368	Peroxisomal acyl-coenzyme A oxidase 3	1
38870832	10.1016/j.ejmech.2024.116561	B16-F10	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

Data from ChEMBL 36 via Core Engine