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Compound Detail

CHEMBL576982

QUIZARTINIB
💊 Approved Drug
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💊 Approved Drug
CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCOCC5)ccc34)cc2)no1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL576982
Name QUIZARTINIB
Phase Approved
Structure Type MOL
InChI Key CVWXJKQAOSCOAB-UHFFFAOYSA-N
Therapeutic ✓ Yes

Known Names

AC-010220 Ac-220 AC010220 AC220 ASP-2689 Quizartinib
102
Targets
464
Activities
3
Assay Types
30
PK Parameters
20
Publications
6
Known Names
4
Indications
5
Mechanisms

Molecular Properties

560.7
MW (Da)
5.86
ALogP
9
HBA
2
HBD
106.2
PSA (Ų)
0.26
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2023
Availability Prescription
Chirality Achiral

Routes of Administration

Oral

Flags

Black Box Warning Natural Product Chemical Probe
USAN Stem -tinib
USAN Year 2010

Extended Properties

Molecular Formula C29H32N6O4S
MW 560.68
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -2.19

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Macrophage colony stimulating factor receptor inhibitor INHIBITOR Macrophage colony-stimulating factor 1 receptor ✓ ✓
Tyrosine-protein kinase receptor FLT3 inhibitor INHIBITOR Receptor-type tyrosine-protein kinase FLT3 ✓ ✓
Stem cell growth factor receptor inhibitor INHIBITOR Mast/stem cell growth factor receptor Kit ✓ ✓
Platelet-derived growth factor receptor inhibitor INHIBITOR Platelet-derived growth factor receptor ✓ ✓
Tyrosine-protein kinase receptor RET inhibitor INHIBITOR Proto-oncogene tyrosine-protein kinase receptor Ret ✓ ✓

Indications

Leukemia, Myeloid, Acute Neoplasms Liver Diseases Myelodysplastic Syndromes

ATC Classification

L01EX11
quizartinib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS

Activity Summary

Kd 261 meas. best 9.24
IC50 200 meas. best 10.42
EC50 3 meas. best 9.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NOMO-1
CHEMBL2366198
 IC50 10.42 10.42 0.0 1
OPM-2
CHEMBL2366353
 IC50 10.25 10.25 0.1 1
KG-1
CHEMBL612264
 IC50 9.8 7.135 0.2 2
L-363
CHEMBL2366267
 IC50 9.74 9.74 0.2 1
RPMI-8226
CHEMBL614882
 IC50 9.73 9.73 0.2 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
 IC50 9.7 7.6388 0.2 77
MV4-11
CHEMBL613835
 IC50 9.68 8.9513 0.2 16
NON-PROTEIN TARGET
CHEMBL3879801
 IC50 9.52 9.52 0.3 1
BaF3
CHEMBL614524
 IC50 9.42 7.4861 0.4 23
ML-2
CHEMBL614356
 IC50 9.38 9.38 0.4 1
Unchecked
CHEMBL612545
 IC50 9.3 8.215 0.5 10
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
 Kd 9.24 8.308 0.6 45
Cyclin-dependent kinase 7/ cyclin H
CHEMBL2111288
 IC50 9.21 9.21 0.6 3
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
 EC50 9.07 9.07 0.9 1
MOLM-13
CHEMBL3706572
 IC50 8.96 7.5438 1.1 8
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
 Kd 8.8 7.975 1.6 8
Platelet-derived growth factor receptor beta
CHEMBL1913
 Kd 8.8 8.2138 1.6 8
Mast/stem cell growth factor receptor Kit
CHEMBL1936
 Kd 8.8 7.9612 1.6 25
Platelet-derived growth factor receptor alpha
CHEMBL2007
 Kd 8.8 8.025 1.6 8
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
 Kd 8.8 8.0772 1.6 18
Interleukin-1 receptor-associated kinase 4
CHEMBL3778
 IC50 8.69 8.69 2.1 2
Unchecked
CHEMBL612545
 Kd 8.15 7.3325 7.0 4
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
 IC50 7.86 7.86 13.8 2
U-266
CHEMBL2366315
 IC50 7.71 7.71 19.6 1
Tyrosine-protein kinase Blk
CHEMBL2250
 IC50 7.68 7.68 20.7 2
SKM-1
CHEMBL2366085
 IC50 7.52 7.52 30.0 1
OCI-AML2
CHEMBL2366220
 IC50 7.52 6.935 30.0 2
KMOE-2
CHEMBL2366347
 IC50 7.52 7.52 30.0 1
HL-60
CHEMBL383
 IC50 7.52 6.815 30.0 2
KG-1a
CHEMBL4296453
 IC50 7.52 7.52 30.0 1
OCI-AML-5
CHEMBL4523576
 IC50 7.52 7.52 30.0 1
TF-1
CHEMBL612552
 IC50 7.52 7.52 30.0 1
NB-4
CHEMBL614188
 IC50 7.52 7.52 30.0 1
THP-1
CHEMBL614245
 IC50 7.52 7.11 30.0 2
IM-9
CHEMBL614584
 IC50 7.52 7.52 30.0 1
Platelet-derived growth factor receptor beta
CHEMBL1913
 IC50 7.42 7.42 37.8 2
Vascular endothelial growth factor receptor 3
CHEMBL1955
 Kd 7.42 7.395 38.0 6
Vascular endothelial growth factor receptor 1
CHEMBL1868
 Kd 7.39 7.3183 41.0 6
Platelet-derived growth factor receptor alpha
CHEMBL2007
 IC50 7.38 7.38 42.0 2
Tyrosine-protein kinase Lck
CHEMBL258
 IC50 7.24 7.24 57.8 2
Epithelial discoidin domain-containing receptor 1
CHEMBL5319
 Kd 7.09 7.0683 81.0 6
Mast/stem cell growth factor receptor Kit
CHEMBL1936
 IC50 7.08 7.08 82.6 1
Vascular endothelial growth factor receptor 2
CHEMBL279
 Kd 7.06 7.05 87.0 5
BDNF/NT-3 growth factors receptor
CHEMBL4898
 Kd 6.96 6.3975 110.0 4
Interleukin-1 receptor-associated kinase 1
CHEMBL3357
 IC50 6.94 6.94 116.0 2
Discoidin domain-containing receptor 2
CHEMBL5122
 Kd 6.75 6.238 180.0 5
HT-22
CHEMBL614316
 EC50 6.71 6.71 193.6 1
NT-3 growth factor receptor
CHEMBL5608
 Kd 6.7 6.37 200.0 4
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
 Kd 6.66 5.85 220.0 4
U-937
CHEMBL612794
 IC50 6.6 5.835 251.2 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 11583.65 ng.hr.mL-1 Rattus norvegicus
AUC 19646.23 ng.hr.mL-1 Mus musculus
AUC 19623.8 ng.hr.mL-1 Mus musculus
AUC 1928.0 ng.hr.mL-1 Rattus norvegicus
AUC 14467.0 ng.hr.mL-1 Rattus norvegicus
AUC 1973.0 ng.hr.mL-1 Rattus norvegicus
AUC 14970.0 ng.hr.mL-1 Rattus norvegicus
CL 7.11 mL.min-1.kg-1 Rattus norvegicus
CL 9.35 mL.min-1.kg-1 Rattus norvegicus
CL 12.6 mL.min-1.kg-1 Rattus norvegicus
Cmax 2160.0 nM Rattus norvegicus
Cmax 3800.0 nM Mus musculus
Cmax 3800.0 nM Mus musculus
Cmax 1298.42 nM Rattus norvegicus
Cmax 2036.81 nM Rattus norvegicus
F 48.0 % Rattus norvegicus
F 40.0 % Rattus norvegicus
F 75.9 % Rattus norvegicus
MRT 5.83 hr Rattus norvegicus
MRT 10.11 hr Rattus norvegicus
T1/2 5.5 hr Rattus norvegicus
T1/2 3.6 hr Mus musculus
T1/2 4.38 hr Rattus norvegicus
T1/2 3.73 hr Rattus norvegicus
T1/2 4.3 hr Rattus norvegicus
Tmax 1.5 uM Mus musculus
Tmax 1.5 hr Mus musculus
Tmax 0.03 hr Rattus norvegicus
Tmax 8.0 hr Rattus norvegicus
Vd 3.532 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NOMO-1 IC50 = 0.038 nM 10.42 Cytotoxicity against human NOMO-1 cells assessed as reduction in cell viability ... 32199135
OPM-2 IC50 = 0.056 nM 10.25 Cytotoxicity against human OPM-2 cells assessed as reduction in cell viability a... 32199135
KG-1 IC50 = 0.16 nM 9.8 Cytotoxicity against human KG-1 cells assessed as reduction in cell viability af... 32199135
L-363 IC50 = 0.181 nM 9.74 Cytotoxicity against human L-363 cells assessed as reduction in cell viability a... 32199135
RPMI-8226 IC50 = 0.184 nM 9.73 Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viabili... 32199135
Receptor-type tyrosine-protein kinase FLT3 IC50 = 0.2 nM 9.7 Affinity Phenotypic Cellular interaction: (CellTiter-Glo 2.0 Assay (Promega, cel... -
MV4-11 IC50 = 0.21 nM 9.68 Antiproliferative activity against human MV4-11 cells assessed as inhibition of ... 36638621
Receptor-type tyrosine-protein kinase FLT3 IC50 = 0.236 nM 9.63 HotSpot Assay: Table 3 and 4: The HotSpot kinase profiling and screening assays ... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 0.236 nM 9.63 IC50 Kinase Assays: Table 8-10: Compounds were tested in 10-dose IC50 mode with ... -
MV4-11 IC50 = 0.24 nM 9.62 Antiproliferative activity against human MV4-11 cells assessed as reduction in c... 37584545
NON-PROTEIN TARGET IC50 = 0.3 nM 9.52 Cytotoxicity against human AML cells isolated from relapsed acute myeloid leukem... 19654408
MV4-11 IC50 = 0.31 nM 9.51 Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mu... 38389894
BaF3 IC50 = 0.38 nM 9.42 Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD mutant a... 38389894
Receptor-type tyrosine-protein kinase FLT3 IC50 = 0.4 nM 9.4 Affinity Phenotypic Cellular interaction: (CellTiter-Glo 2.0 Assay (Promega, cel... -
ML-2 IC50 = 0.419 nM 9.38 Cytotoxicity against human ML-2 cells assessed as reduction in cell viability af... 32199135
MV4-11 IC50 = 0.452 nM 9.35 Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant ... 30939008
MV4-11 IC50 = 0.5 nM 9.3 Antiproliferative activity against human MV4-11 cells assessed as reduction in c... 34583130
Unchecked IC50 = 0.497 nM 9.3 Cytotoxicity against human MOLP-2 cells assessed as reduction in cell viability ... 32199135
MV4-11 IC50 = 0.56 nM 9.25 Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer... 19754199
MV4-11 IC50 = 0.56 nM 9.25 Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay 19654408

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724801 U2OS 304
- 10.6019/CHEMBL5058577 HEK-293T 304
- 10.6019/CHEMBL5058577 U2OS 304
- 10.6019/CHEMBL5724801 Fibroblast 304
- 10.6019/CHEMBL5724801 HEK-293T 304
- 10.6019/CHEMBL5058577 Fibroblast 304
28956923 10.1021/acs.jmedchem.7b00840 BaF3 22
28956923 10.1021/acs.jmedchem.7b00840 Rattus norvegicus 17
- 10.6019/CHEMBL5444388 Receptor-type tyrosine-protein kinase FLT3 17
22037378 10.1038/nbt.1990 Tyrosine-protein kinase ABL1 15
33797247 10.1021/acs.jmedchem.0c02247 MOLM-13 14
35124201 10.1016/j.bmcl.2022.128603 MV4-11 13
30939008 10.1021/acs.jmedchem.9b00223 Receptor-type tyrosine-protein kinase FLT3 13
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
22037378 10.1038/nbt.1990 Epidermal growth factor receptor 12
- 10.6019/CHEMBL5465560 Epidermal growth factor receptor 12
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
29672049 10.1021/acs.jmedchem.7b01529 Receptor-type tyrosine-protein kinase FLT3 10
19654408 10.1182/blood-2009-05-222034 Receptor-type tyrosine-protein kinase FLT3 10
19754199 10.1021/jm9007533 MV4-11 10

Data from ChEMBL 36 via Core Engine