Compound Detail

CHEMBL477772

PAZOPANIB

💊 Approved Drug

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💊 Approved Drug

Cc1ccc(Nc2nccc(N(C)c3ccc4c(C)n(C)nc4c3)n2)cc1S(N)(=O)=O

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL477772
Name	PAZOPANIB
Phase	Approved
Structure Type	MOL
InChI Key	CUIHSIWYWATEQL-UHFFFAOYSA-N
Therapeutic	✓ Yes

Known Names

GW-786034 GW786034 NSC-752782 Pazopanib Votrient

465

Targets

995

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Molecular Properties

437.5

MW (Da)

3.14

ALogP

HBA

HBD

119.0

PSA (Å²)

0.49

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
First Approval	2009
Availability	Prescription
Chirality	Achiral

Routes of Administration

Oral

Flags

Black Box Warning Natural Product

USAN Stem	-anib
USAN Year	2005

Extended Properties

Molecular Formula	C21H23N7O2S
MW	437.53
Aromatic Rings	4
Heavy Atoms	31
NP-Likeness	-1.70

Indications

Carcinoma, Renal Cell Carcinoma, Renal Cell Neoplasms Neoplasms Ovarian Neoplasms Ovarian Neoplasms Sarcoma Sarcoma Breast Neoplasms Breast Neoplasms Carcinoma, Non-Small-Cell Lung Carcinoma, Squamous Cell Central Nervous System Neoplasms Chondrosarcoma Dermatofibrosarcoma Fallopian Tube Neoplasms Gastrointestinal Stromal Tumors Gliosarcoma Hemangiosarcoma Kidney Neoplasms

ATC Classification

L01EX03

pazopanib

Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Level 2: ANTINEOPLASTIC AGENTS

Activity Summary

IC50 719 meas. best 10.54

Kd 244 meas. best 8.74

Ki 30 meas. best 9.05

EC50 2 meas. best 6.59

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
EOL1 CHEMBL614489	IC50	10.54	10.54	0.0	1
Carbonic anhydrase 12 CHEMBL3242	Ki	9.05	9.05	0.9	1
Mast/stem cell growth factor receptor Kit CHEMBL1936	Kd	8.74	7.698	1.8	15
Platelet-derived growth factor receptor beta CHEMBL1913	Kd	8.7	7.9233	2.0	3
Vascular endothelial growth factor receptor 2 CHEMBL279	Ki	8.5	8.5	3.2	1
Platelet-derived growth factor receptor beta CHEMBL1913	Ki	8.4	8.4	4.0	1
Platelet-derived growth factor receptor alpha CHEMBL2007	Kd	8.31	8.31	4.9	2
Vascular endothelial growth factor receptor 2 CHEMBL279	IC50	8.3	7.615	5.0	12
Macrophage colony-stimulating factor 1 receptor CHEMBL1844	Kd	8.1	8.1	7.9	2
Carbonic anhydrase 9 CHEMBL3594	Ki	8.04	8.04	9.1	2
AN3-CA CHEMBL1075392	IC50	8.0	8.0	10.1	1
Vascular endothelial growth factor receptor 1 CHEMBL1868	IC50	8.0	7.7525	10.0	4
Carbonic anhydrase 1 CHEMBL261	Ki	7.92	7.92	12.1	1
Vascular endothelial growth factor receptor 1 CHEMBL1868	Kd	7.85	7.85	14.0	2
Vascular endothelial growth factor receptor 2 CHEMBL279	Kd	7.85	7.85	14.0	2
Vascular endothelial growth factor receptor 1 CHEMBL1868	Ki	7.8	7.8	15.8	1
Macrophage colony-stimulating factor 1 receptor CHEMBL1844	Ki	7.7	7.7	19.9	1
HUVEC CHEMBL613979	IC50	7.68	6.3867	21.0	3
Vascular endothelial growth factor receptor 3 CHEMBL1955	Kd	7.57	7.57	27.0	2
Carbonic anhydrase 2 CHEMBL205	Ki	7.49	7.49	32.4	1
CGTH-W-1 CHEMBL2366300	IC50	7.4	7.4	40.0	1
Serine/threonine-protein kinase TAO3 CHEMBL5701	Kd	7.35	7.35	45.0	1
Vascular endothelial growth factor receptor 3 CHEMBL1955	IC50	7.34	7.3325	46.0	4
Unchecked CHEMBL612545	IC50	7.33	5.4025	46.5	8
Discoidin domain-containing receptor 2 CHEMBL5122	IC50	7.3	7.295	50.0	2
Discoidin domain-containing receptor 2 CHEMBL5122	Kd	7.24	6.905	57.0	6
Epithelial discoidin domain-containing receptor 1 CHEMBL5319	Kd	7.24	7.12	57.0	3
Platelet-derived growth factor receptor alpha CHEMBL2007	IC50	7.15	7.15	71.0	1
Mast/stem cell growth factor receptor Kit CHEMBL1936	IC50	7.13	7.0633	74.0	3
Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041	Ki	7.1	7.1	79.4	1
Ephrin type-B receptor 6 CHEMBL5836	Kd	7.09	7.09	81.0	1
Platelet-derived growth factor receptor beta CHEMBL1913	IC50	7.08	7.08	83.0	3
Serine/threonine-protein kinase 10 CHEMBL3981	Kd	7.08	7.08	84.0	2
GDM-1 CHEMBL2366157	IC50	6.98	6.98	104.0	1
A204 CHEMBL614514	IC50	6.96	6.96	109.1	1
Fibroblast growth factor receptor 1 CHEMBL3650	IC50	6.85	6.83	140.0	3
Fibroblast growth factor receptor 2 CHEMBL4142	IC50	6.85	6.85	140.0	1
Macrophage colony-stimulating factor 1 receptor CHEMBL1844	IC50	6.84	6.7	146.0	2
Dual specificity protein kinase TTK CHEMBL3983	Kd	6.82	6.82	150.0	2
Fibroblast growth factor receptor 1 CHEMBL3650	Ki	6.8	6.8	158.5	1
Cyclin-G-associated kinase CHEMBL4355	Kd	6.7	6.7	200.0	2
Fibroblast growth factor receptor 2 CHEMBL4142	Kd	6.68	6.68	210.0	2
STE20-like serine/threonine-protein kinase CHEMBL4202	Kd	6.62	6.62	240.0	1
Serine/threonine-protein kinase TAO1 CHEMBL5261	Kd	6.62	6.62	240.0	1
Jurkat CHEMBL397	EC50	6.59	6.59	254.0	1
Receptor-interacting serine/threonine-protein kinase 1 CHEMBL5464	Kd	6.58	6.58	260.0	3
Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041	Kd	6.57	6.2243	270.0	7
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma CHEMBL1770034	Kd	6.55	6.55	280.0	1
Mitogen-activated protein kinase kinase kinase 9 CHEMBL2872	Kd	6.54	6.54	290.0	2
Serine/threonine-protein kinase PLK4 CHEMBL3788	Kd	6.54	6.54	290.0	2

Pharmacokinetic Data

Parameter	Value	Units	Species
AUC	220000.0	ng.hr.mL-1	Mus musculus
AUC	657000.0	ng.hr.mL-1	Mus musculus
AUC	1141000.0	ng.hr.mL-1	Mus musculus
AUC	1037011.73	ng.hr.mL-1	Homo sapiens
AUC	279.5	-	Chlorocebus sabaeus
CL	1.4	mL.min-1.kg-1	Rattus norvegicus
CL	1.4	mL.min-1.kg-1	Canis lupus familiaris
CL	1.4	mL.min-1.kg-1	Macaca mulatta
F	72.0	%	Rattus norvegicus
F	47.0	%	Canis lupus familiaris
F	65.0	%	Macaca mulatta

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
EOL1	IC50	=	0.02889	nM	10.54	SANGER: Inhibition of human EoL-1-cell cell growth in a cell viability assay.	-
Carbonic anhydrase 12	Ki	=	0.9	nM	9.05	Inhibition of human CA12 assessed as inhibition constant preincubated for 15 min...	38810335
Mast/stem cell growth factor receptor Kit	Kd	=	1.8	nM	8.74	Binding constant for KIT(L576P) kinase domain	22037378
Platelet-derived growth factor receptor beta	Kd	=	2.0	nM	8.7	Binding constant for PDGFRB kinase domain	22037378
Platelet-derived growth factor receptor beta	Kd	=	2.0	nM	8.7	Binding constant for PDGFRB kinase domain	18183025
Mast/stem cell growth factor receptor Kit	Kd	=	2.3	nM	8.64	Binding constant for KIT(V559D) kinase domain	22037378
Mast/stem cell growth factor receptor Kit	Kd	=	2.3	nM	8.64	Binding constant for KIT(V559D) kinase domain	18183025
Mast/stem cell growth factor receptor Kit	Kd	=	2.8	nM	8.55	Binding constant for KIT kinase domain	22037378
Mast/stem cell growth factor receptor Kit	Kd	=	2.8	nM	8.55	Binding affinity to human KIT incubated for 1 hr by kinase binding assay	21429632
Mast/stem cell growth factor receptor Kit	Kd	=	2.8	nM	8.55	Binding constant for KIT kinase domain	18183025
Vascular endothelial growth factor receptor 2	Ki	=	3.162	nM	8.5	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na...	-
Platelet-derived growth factor receptor beta	Ki	=	3.981	nM	8.4	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na...	-
Platelet-derived growth factor receptor alpha	Kd	=	4.9	nM	8.31	Binding constant for PDGFRA kinase domain	22037378
Platelet-derived growth factor receptor alpha	Kd	=	4.9	nM	8.31	Binding constant for PDGFRA kinase domain	18183025
Vascular endothelial growth factor receptor 2	IC50	=	5.012	nM	8.3	Inhibition of KDR (unknown origin)	23937569
Mast/stem cell growth factor receptor Kit	Kd	=	6.5	nM	8.19	Binding constant for KIT(V559D,T670I) kinase domain	22037378
Mast/stem cell growth factor receptor Kit	Kd	=	6.5	nM	8.19	Binding constant for KIT(V559D,T670I) kinase domain	18183025
Vascular endothelial growth factor receptor 2	IC50	=	8.0	nM	8.1	Inhibition of VEGF-induced VEGFR2 phosphorylation in HUVEC	18620382
Macrophage colony-stimulating factor 1 receptor	Kd	=	7.9	nM	8.1	Binding constant for CSF1R kinase domain	18183025
Macrophage colony-stimulating factor 1 receptor	Kd	=	7.9	nM	8.1	Binding constant for CSF1R kinase domain	22037378

Literature References

PubMed	DOI	Target Context	# Activities
37616488	10.1021/acs.jmedchem.3c00640	MDA-MB-231	42
37616488	10.1021/acs.jmedchem.3c00640	MCF7	26
22037378	10.1038/nbt.1990	Tyrosine-protein kinase ABL1	15
22037378	10.1038/nbt.1990	Epidermal growth factor receptor	12
18620382	10.1021/jm800566m	Mus musculus	10
22037378	10.1038/nbt.1990	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	10
18183025	10.1038/nbt1358	Epidermal growth factor receptor	10
26254279	10.18632/oncotarget.4214	Unchecked	9
22037378	10.1038/nbt.1990	Mast/stem cell growth factor receptor Kit	8
18183025	10.1038/nbt1358	Tyrosine-protein kinase ABL1	7
22037378	10.1038/nbt.1990	Receptor-type tyrosine-protein kinase FLT3	7
25101911	10.1021/jm501177w	HepG2	6
38810335	10.1016/j.ejmech.2024.116527	Unchecked	5
18183025	10.1038/nbt1358	Receptor-type tyrosine-protein kinase FLT3	5
37616488	10.1021/acs.jmedchem.3c00640	Vascular endothelial growth factor receptor 2	5
18183025	10.1038/nbt1358	Mast/stem cell growth factor receptor Kit	5
29191878	10.1126/science.aan4368	Unchecked	5
22037378	10.1038/nbt.1990	Proto-oncogene tyrosine-protein kinase receptor Ret	4
18620382	10.1021/jm800566m	HT-29	4
18620382	10.1021/jm800566m	NON-PROTEIN TARGET	4

Data from ChEMBL 36 via Core Engine