Sunitinib

Details

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Internal ID ed2f12de-43ab-40fc-9fe9-3b8405dad1e8
Taxonomy Organoheterocyclic compounds > Indoles and derivatives > Indolines
IUPAC Name N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
SMILES (Canonical)
SMILES (Isomeric)
InChI InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
InChI Key WINHZLLDWRZWRT-ATVHPVEESA-N
Popularity 15,667 references in papers

Physical and Chemical Properties

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Molecular Formula C22H27FN4O2
Molecular Weight 398.50 g/mol
Exact Mass 398.21180428 g/mol
Topological Polar Surface Area (TPSA) 77.20 Ų
XlogP 2.60
Atomic LogP (AlogP) 3.33
H-Bond Acceptor 3
H-Bond Donor 3
Rotatable Bonds 7

Synonyms

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557795-19-4
SU-11248
SU11248
sunitinibum
Su-011248
N-[2-(diethylamino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide
NSC-750690
SU011248
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
NSC-736511
There are more than 10 synonyms. If you wish to see them all click here.

2D Structure

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2D Structure of Sunitinib

3D Structure

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ADMET Properties (via admetSAR 2)

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Target Value Probability (raw) Probability (%)
Human Intestinal Absorption + 0.9896 98.96%
Caco-2 - 0.6101 61.01%
Blood Brain Barrier + 0.7750 77.50%
Human oral bioavailability + 0.9000 90.00%
Subcellular localzation Mitochondria 0.4405 44.05%
OATP2B1 inhibitior - 1.0000 100.00%
OATP1B1 inhibitior + 0.8543 85.43%
OATP1B3 inhibitior + 0.9330 93.30%
MATE1 inhibitior - 0.7463 74.63%
OCT2 inhibitior - 0.7000 70.00%
BSEP inhibitior + 0.9072 90.72%
P-glycoprotein inhibitior + 0.5899 58.99%
P-glycoprotein substrate + 0.8007 80.07%
CYP3A4 substrate + 0.6352 63.52%
CYP2C9 substrate - 0.8060 80.60%
CYP2D6 substrate - 0.8229 82.29%
CYP3A4 inhibition - 0.5991 59.91%
CYP2C9 inhibition - 0.6437 64.37%
CYP2C19 inhibition - 0.6261 62.61%
CYP2D6 inhibition - 0.6846 68.46%
CYP1A2 inhibition - 0.5626 56.26%
CYP2C8 inhibition - 0.5958 59.58%
CYP inhibitory promiscuity + 0.7032 70.32%
UGT catelyzed - 0.0000 0.00%
Carcinogenicity (binary) - 0.7900 79.00%
Carcinogenicity (trinary) Non-required 0.6085 60.85%
Eye corrosion - 0.9886 98.86%
Eye irritation - 0.9649 96.49%
Skin irritation - 0.7702 77.02%
Skin corrosion - 0.9210 92.10%
Ames mutagenesis + 0.6300 63.00%
Human Ether-a-go-go-Related Gene inhibition + 0.7396 73.96%
Micronuclear + 0.7500 75.00%
Hepatotoxicity + 0.9750 97.50%
skin sensitisation - 0.8414 84.14%
Respiratory toxicity + 0.9333 93.33%
Reproductive toxicity + 0.9333 93.33%
Mitochondrial toxicity + 0.9125 91.25%
Nephrotoxicity - 0.8459 84.59%
Acute Oral Toxicity (c) III 0.5912 59.12%
Estrogen receptor binding + 0.8191 81.91%
Androgen receptor binding + 0.6668 66.68%
Thyroid receptor binding + 0.6869 68.69%
Glucocorticoid receptor binding - 0.4868 48.68%
Aromatase binding + 0.6752 67.52%
PPAR gamma + 0.6872 68.72%
Honey bee toxicity - 0.9131 91.31%
Biodegradation - 0.8500 85.00%
Crustacea aquatic toxicity - 0.6100 61.00%
Fish aquatic toxicity + 0.9596 95.96%

Targets

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Proven Targets:

CHEMBL ID UniProt ID Name Min activity Assay type Source
CHEMBL3830 Q2M2I8 Adaptor-associated kinase 11 nM
Kd
via Super-PRED
CHEMBL4247 Q9UM73 ALK tyrosine kinase receptor 170 nM
Kd
via Super-PRED
CHEMBL4045 Q13131 AMP-activated protein kinase, alpha-1 subunit 19 nM
Kd
via Super-PRED
CHEMBL4522 Q9NSY1 BMP-2-inducible protein kinase 5.5 nM
Kd
via Super-PRED
CHEMBL5073 Q8IU85 CaM kinase I delta 510 nM
Kd
via Super-PRED
CHEMBL4147 Q9UQM7 CaM kinase II alpha 80 nM
Kd
via Super-PRED
CHEMBL3829 Q13555 CaM kinase II gamma 690 nM
Kd
via Super-PRED
CHEMBL2828 P48730 Casein kinase I delta 15 nM
Kd
via Super-PRED
CHEMBL4937 P49674 Casein kinase I epsilon 13 nM
Kd
via Super-PRED
CHEMBL5084 Q9Y6M4 Casein kinase I isoform gamma-3 240 nM
Kd
via Super-PRED
CHEMBL3629 P68400 Casein kinase II alpha 81 nM
Kd
via Super-PRED
CHEMBL4070 P19784 Casein kinase II alpha (prime) 370 nM
Kd
via Super-PRED
CHEMBL3055 P50613 Cyclin-dependent kinase 7 330 nM
Kd
via Super-PRED
CHEMBL2558 P53355 Death-associated protein kinase 1 120 nM
Kd
via Super-PRED
CHEMBL2468 O43293 Death-associated protein kinase 3 22 nM
Kd
via Super-PRED
CHEMBL3587 Q02750 Dual specificity mitogen-activated protein kinase kinase 1 130 nM
Kd
via Super-PRED
CHEMBL2964 P36507 Dual specificity mitogen-activated protein kinase kinase 2 110 nM
Kd
via Super-PRED
CHEMBL4225 P49760 Dual specificity protein kinase CLK2 20 nM
Kd
via Super-PRED
CHEMBL4224 P49759 Dual specificty protein kinase CLK1 22 nM
Kd
via Super-PRED
CHEMBL4526 Q9UF33 Ephrin type-A receptor 6 960 nM
Kd
via Super-PRED
CHEMBL3650 P11362 Fibroblast growth factor receptor 1 520 nM
Kd
via Super-PRED
CHEMBL2742 P22607 Fibroblast growth factor receptor 3 290 nM
Kd
via Super-PRED
CHEMBL240 Q12809 HERG 500 nM
IC50
via Super-PRED
CHEMBL3529 Q14164 Inhibitor of nuclear factor kappa B kinase epsilon subunit 620 nM
Kd
via Super-PRED
CHEMBL5785 P19525 Interferon-induced, double-stranded RNA-activated protein kinase 670 nM
Kd
via Super-PRED
CHEMBL1075104 Q5S007 Leucine-rich repeat serine/threonine-protein kinase 2 15 nM
IC50
via Super-PRED
CHEMBL1844 P07333 Macrophage colony stimulating factor receptor 2 nM
Kd
via Super-PRED
CHEMBL3831 Q7KZI7 MAP/microtubule affinity-regulating kinase 2 310 nM
Kd
via Super-PRED
CHEMBL4578 Q14680 Maternal embryonic leucine zipper kinase 350 nM
Kd
via Super-PRED
CHEMBL5432 Q8IVH8 Mitogen-activated protein kinase kinase kinase kinase 3 180 nM
Kd
via Super-PRED
CHEMBL6166 O95819 Mitogen-activated protein kinase kinase kinase kinase 4 140 nM
Kd
via Super-PRED
CHEMBL4852 Q9Y4K4 Mitogen-activated protein kinase kinase kinase kinase 5 41 nM
Kd
via Super-PRED
CHEMBL2815 P04629 Nerve growth factor receptor Trk-A 100 nM
Kd
via Super-PRED
CHEMBL4898 Q16620 Neurotrophic tyrosine kinase receptor type 2 590 nM
Kd
via Super-PRED
CHEMBL5784 O60285 NUAK family SNF1-like kinase 1 48 nM
Kd
via Super-PRED
CHEMBL2349 P15735 Phosphorylase kinase gamma subunit 2 5.9 nM
Kd
via Super-PRED
CHEMBL2007 P16234 Platelet-derived growth factor receptor alpha 0.79 nM
Kd
via Super-PRED
CHEMBL2595 O94806 Protein kinase C nu 280 nM
Kd
via Super-PRED
CHEMBL5331 Q12866 Proto-oncogene tyrosine-protein kinase MER 26 nM
Kd
via Super-PRED
CHEMBL2553 Q15418 Ribosomal protein S6 kinase alpha 1 140 nM
Kd
via Super-PRED
CHEMBL2345 P51812 Ribosomal protein S6 kinase alpha 3 55 nM
Kd
via Super-PRED
CHEMBL4237 O75582 Ribosomal protein S6 kinase alpha 5 28 nM
Kd
via Super-PRED
CHEMBL3981 O94804 Serine/threonine-protein kinase 10 19 nM
Kd
via Super-PRED
CHEMBL4525 Q9UEE5 Serine/threonine-protein kinase 17A 1 nM
Kd
via Super-PRED
CHEMBL4202 Q9H2G2 Serine/threonine-protein kinase 2 56 nM
Kd
via Super-PRED
CHEMBL2185 Q96GD4 Serine/threonine-protein kinase Aurora-B 380 nM
Kd
via Super-PRED
CHEMBL5600 P27448 Serine/threonine-protein kinase c-TAK1 410 nM
Kd
via Super-PRED
CHEMBL4630 O14757 Serine/threonine-protein kinase Chk1 300 nM
Kd
via Super-PRED
CHEMBL4900 Q9BZL6 Serine/threonine-protein kinase D2 380 nM
Kd
via Super-PRED
CHEMBL4355 O14976 Serine/threonine-protein kinase GAK 20 nM
Kd
via Super-PRED
CHEMBL6167 O95835 Serine/threonine-protein kinase LATS1 630 nM
Kd
via Super-PRED
CHEMBL4598 Q13043 Serine/threonine-protein kinase MST1 19 nM
Kd
via Super-PRED
CHEMBL4708 Q13188 Serine/threonine-protein kinase MST2 56 nM
Kd
via Super-PRED
CHEMBL4311 Q9NQU5 Serine/threonine-protein kinase PAK6 500 nM
Ki
via Super-PRED
CHEMBL1936 P10721 Stem cell growth factor receptor 0.21 nM
Kd
via Super-PRED
CHEMBL2250 P51451 Tyrosine-protein kinase BLK 65 nM
Kd
via Super-PRED
CHEMBL3234 P08631 Tyrosine-protein kinase HCK 880 nM
Kd
via Super-PRED
CHEMBL2959 Q08881 Tyrosine-protein kinase ITK/TSK 13 nM
Kd
via Super-PRED
CHEMBL2835 P23458 Tyrosine-protein kinase JAK1 9.2 nM
Kd
via Super-PRED
CHEMBL258 P06239 Tyrosine-protein kinase LCK 230 nM
Kd
via Super-PRED
CHEMBL3905 P07948 Tyrosine-protein kinase Lyn 270 nM
Kd
via Super-PRED
CHEMBL1974 P36888 Tyrosine-protein kinase receptor FLT3 0.22 nM
Kd
via Super-PRED
CHEMBL2041 P07949 Tyrosine-protein kinase receptor RET 5.8 nM
Kd
via Super-PRED
CHEMBL5314 Q06418 Tyrosine-protein kinase receptor TYRO3 49 nM
Kd
via Super-PRED
CHEMBL4895 P30530 Tyrosine-protein kinase receptor UFO 9 nM
Kd
via Super-PRED
CHEMBL2073 P07947 Tyrosine-protein kinase YES 120 nM
Kd
via Super-PRED
CHEMBL4105933 Q6ZSR9 Uncharacterized protein FLJ45252 431 nM
Kd
via Super-PRED
CHEMBL1868 P17948 Vascular endothelial growth factor receptor 1 1.8 nM
Kd
via Super-PRED
CHEMBL279 P35968 Vascular endothelial growth factor receptor 2 0.23 nM
Kd
via Super-PRED
CHEMBL1955 P35916 Vascular endothelial growth factor receptor 3 17 nM
Ki
via Super-PRED

Predicted Targets (via Super-PRED):

CHEMBL ID UniProt ID Name Probability Model accuracy
CHEMBL1913 P09619 Platelet-derived growth factor receptor beta 99.64% 95.70%
CHEMBL2581 P07339 Cathepsin D 98.39% 98.95%
CHEMBL1907602 P06493 Cyclin-dependent kinase 1/cyclin B1 96.87% 91.24%
CHEMBL3251 P19838 Nuclear factor NF-kappa-B p105 subunit 96.07% 96.09%
CHEMBL4145 Q9UKV0 Histone deacetylase 9 95.63% 85.49%
CHEMBL5845 P23415 Glycine receptor subunit alpha-1 93.33% 90.71%
CHEMBL2535 P11166 Glucose transporter 93.16% 98.75%
CHEMBL2563 Q9UQL6 Histone deacetylase 5 93.15% 89.67%
CHEMBL5469 Q14289 Protein tyrosine kinase 2 beta 92.65% 91.03%
CHEMBL255 P29275 Adenosine A2b receptor 92.21% 98.59%
CHEMBL4685 P14902 Indoleamine 2,3-dioxygenase 91.99% 96.38%
CHEMBL1907605 P24864 Cyclin-dependent kinase 2/cyclin E1 91.31% 92.88%
CHEMBL1293267 Q9HC97 G-protein coupled receptor 35 91.05% 89.34%
CHEMBL1907600 Q00535 Cyclin-dependent kinase 5/CDK5 activator 1 90.81% 93.03%
CHEMBL3108638 O15164 Transcription intermediary factor 1-alpha 90.36% 95.56%
CHEMBL5979 P05186 Alkaline phosphatase, tissue-nonspecific isozyme 89.96% 85.40%
CHEMBL3492 P49721 Proteasome Macropain subunit 87.98% 90.24%
CHEMBL1806 P11388 DNA topoisomerase II alpha 87.50% 89.00%
CHEMBL3922 P50579 Methionine aminopeptidase 2 86.96% 97.28%
CHEMBL4581 P52732 Kinesin-like protein 1 86.92% 93.18%
CHEMBL3880 P07900 Heat shock protein HSP 90-alpha 86.76% 96.21%
CHEMBL3038477 P67870 Casein kinase II alpha/beta 85.22% 99.23%
CHEMBL2288 Q13526 Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 85.09% 91.71%
CHEMBL2111367 P27986 PI3-kinase p110-alpha/p85-alpha 84.64% 94.33%
CHEMBL3145 P42338 PI3-kinase p110-beta subunit 84.59% 98.75%
CHEMBL4208 P20618 Proteasome component C5 84.46% 90.00%
CHEMBL1075317 P61964 WD repeat-containing protein 5 84.35% 96.33%
CHEMBL3401 O75469 Pregnane X receptor 82.54% 94.73%
CHEMBL5619 P27695 DNA-(apurinic or apyrimidinic site) lyase 82.40% 91.11%
CHEMBL4203 Q9HAZ1 Dual specificity protein kinase CLK4 80.34% 94.45%
CHEMBL1075094 Q16236 Nuclear factor erythroid 2-related factor 2 80.30% 96.00%
CHEMBL224 P28223 Serotonin 2a (5-HT2a) receptor 80.06% 91.43%

Plants that contains it

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Below are displayed all the plants proven (via scientific papers) to contain this compound!
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There are no matching plants.

Cross-Links

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PubChem 5329102
LOTUS LTS0010688
wikiData Q417542