General Information of the Protein
Protein ID
PT03338
Protein Name
Tyrosine-protein kinase ABL1
Secondarily
Protein Name
Abelson murine leukemia viral oncogene homolog 1
Abelson tyrosine-protein kinase 1
Proto-oncogene c-Abl
p150
Gene Name
ABL1
Secondarily
Gene Name
Abl
Sequence
MLEICLKLVGCKSKKGLSSSSSCYLEEALQRPVASDFEPQGLSEAARWNSKENLLAGPSENDPNLFVALYDFVASGDNTLSITKGEKLRVLGYNHNGEWCEAQTKNGQGWVPSNYITPVNSLEKHSWYHGPVSRNAAEYLLSSGINGSFLVRESESSPGQRSISLRYEGRVYHYRINTASDGKLYVSSESRFNTLAELVHHHSTVADGLITTLHYPAPKRNKPTIYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTYGNLLDYLRECNRQEVSAVVLLYMATQISSAMEYLEKKNFIHRDLAARNCLVGENHLVKVADFGLSRLMTGDTYTAHAGAKFPIKWTAPESLAYNKFSIKSDVWAFGVLLWEIATYGMSPYPGIDLSQVYELLEKDYRMERPEGCPEKVYELMRACWQWNPSDRPSFAEIHQAFETMFQESSISDEVEKELGKRGTRGGAGSMLQAPELPTKTRTCRRAAEQKDAPDTPELLHTKGLGESDALDSEPAVSPLLPRKERGPPDGSLNEDERLLPRDRKTNLFSALIKKKKKMAPTPPKRSSSFREMDGQPDRRGASEDDSRELCNGPPALTSDAAEPTKSPKASNGAGVPNGAFREPGNSGFRSPHMWKKSSTLTGSRLAAAEEESGMSSSKRFLRSCSASCMPHGARDTEWRSVTLPRDLPSAGKQFDSSTFGGHKSEKPALPRKRTSESRSEQVAKSTAMPPPRLVKKNEEAAEEGFKDTESSPGSSPPSLTPKLLRRQVTASPSSGLSHKEEATKGSASGMGTPATAEPAPPSNKVGLSKASSEEMRVRRHKHSSESPGRDKGRLAKLKPAPPPPPACTGKAGKPAQSPSQEAGEAGGPTKTKCTSLAMDAVNTDPTKAGPPGEGLRKPVPPSVPKPQSTAKPPGTPTSPVSTPSTAPAPSPLAGDQQPSSAAFIPLISTRVSLRKTRQPPERIASGTITKGVVLDSTEALCLAISRNSEQMASHSAVLEAGKNLYTFCVSYVDSIQQMRNKFAFREAINKLESNLRELQICPATASSGPAATQDFSKLLSSVKEISDIVRR
    Show/Hide
Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Abl family
Function
Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility and adhesion, receptor endocytosis, autophagy, DNA damage response and apoptosis. Coordinates actin remodeling through tyrosine phosphorylation of proteins controlling cytoskeleton dynamics like WASF3 (involved in branch formation); ANXA1 (involved in membrane anchoring); DBN1, DBNL, CTTN, RAPH1 and ENAH (involved in signaling); or MAPT and PXN (microtubule-binding proteins). Phosphorylation of WASF3 is critical for the stimulation of lamellipodia formation and cell migration. Involved in the regulation of cell adhesion and motility through phosphorylation of key regulators of these processes such as BCAR1, CRK, CRKL, DOK1, EFS or NEDD9. Phosphorylates multiple receptor tyrosine kinases and more particularly promotes endocytosis of EGFR, facilitates the formation of neuromuscular synapses through MUSK, inhibits PDGFRB-mediated chemotaxis and modulates the endocytosis of activated B-cell receptor complexes. Other substrates which are involved in endocytosis regulation are the caveolin (CAV1) and RIN1. Moreover, ABL1 regulates the CBL family of ubiquitin ligases that drive receptor down-regulation and actin remodeling. Phosphorylation of CBL leads to increased EGFR stability. Involved in late-stage autophagy by regulating positively the trafficking and function of lysosomal components. ABL1 targets to mitochondria in response to oxidative stress and thereby mediates mitochondrial dysfunction and cell death. In response to oxidative stress, phosphorylates serine/threonine kinase PRKD2 at 'Tyr-717' (By similarity). ABL1 is also translocated in the nucleus where it has DNA-binding activity and is involved in DNA-damage response and apoptosis. Many substrates are known mediators of DNA repair: DDB1, DDB2, ERCC3, ERCC6, RAD9A, RAD51, RAD52 or WRN. Activates the proapoptotic pathway when the DNA damage is too severe to be repaired. Phosphorylates TP73, a primary regulator for this type of damage-induced apoptosis. Phosphorylates the caspase CASP9 on 'Tyr-191' and regulates its processing in the apoptotic response to DNA damage. Phosphorylates PSMA7 that leads to an inhibition of proteasomal activity and cell cycle transition blocks. Regulates T-cell differentiation in a TBX21-dependent manner (PubMed:21690296). Positively regulates chemokine-mediated T-cell migration, polarization, and homing to lymph nodes and immune-challenged tissues, potentially via activation of NEDD9/HEF1 and RAP1 (PubMed:22810897). Phosphorylates TBX21 on tyrosine residues leading to an enhancement of its transcriptional activator activity (PubMed:21690296).
    Show/Hide
Uniprot ID
Primary ID:
P00520

Secondarily ID:
P97896
Q61252
Q61253
Q61254
Q61255
Q61256
Q61257
Q61258
Q61259
Q61260
Q61261
Q6PCM5
Q8C1X4
    Show/Hide
Ensembl ID
ENSG00000097007
Subcellular Location
Cytoplasm
Cytoskeleton
Nucleus
Mitochondrion
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0015544
3-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzamide
   Show/Hide
C18H13F3N4O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0272876
N-(2-hydroxyethyl)-3-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]benzamide
   Show/Hide
C20H17F3N4O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0388540
4-(6-(4-(trifluoromethoxy)phenylamino)pyrimidin-4-yl)benzenesulfonamide
   Show/Hide
C17H13F3N4O3S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0388541
N-[4-[6-[4-(trifluoromethoxy)anilino]pyrimidin-4-yl]phenyl]methanesulfonamide
   Show/Hide
C18H15F3N4O3S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0388542
(4-methylpiperazin-1-yl)(4-(4-(trifluoromethoxy)phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanone
   Show/Hide
C19H18F3N5O2S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0388544
6-(1H-pyrazol-4-yl)-N-(4-(trifluoromethoxy)phenyl)pyrimidin-4-amine
   Show/Hide
C14H10F3N5O
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0388545
1-tert-butyl-N-(4-(trifluoromethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
   Show/Hide
C16H16F3N5O
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0477483
7-(2-morpholinoethyl)-N-(4-(trifluoromethoxy)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
   Show/Hide
C19H20F3N5O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0510287
2-(4-(4-(Trifluoromethoxy)phenylamino)-1H-pyrazolo-[3,4-d]pyrimidin-1-yl)ethanol
   Show/Hide
C14H12F3N5O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
   Show/Hide
C29H31N7O
 2
1
IC50 = 730 nM
   TI
   LI
   LO
   TS
2
IC50 = 20030 nM
   TI
   LI
   LO
   TS
CP0408606
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-2-hydroxyacetamide
   Show/Hide
C24H27ClN6O4
 2
1
IC50 = 1120 nM
   TI
   LI
   LO
   TS
2
IC50 = 1480 nM
   TI
   LI
   LO
   TS
CP0478346
4-(2-azidophenoxy)-5-chloro-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
   Show/Hide
C22H23ClN8O2
 2
1
IC50 = 1330 nM
   TI
   LI
   LO
   TS
2
IC50 = 1450 nM
   TI
   LI
   LO
   TS
CP0905680
N-(2-(5-Chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)-2-benzyloxyacetamide
   Show/Hide
C31H33ClN6O4
 2
1
IC50 = 1370 nM
   TI
   LI
   LO
   TS
2
IC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0472904
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-3-hydroxypropanamide
   Show/Hide
C25H29ClN6O4
 2
1
IC50 = 1390 nM
   TI
   LI
   LO
   TS
2
IC50 = 2070 nM
   TI
   LI
   LO
   TS
CP0429397
N-[4-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-3-phenylmethoxypropanamide
   Show/Hide
C32H35ClN6O4
 2
1
IC50 = 1430 nM
   TI
   LI
   LO
   TS
2
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0518127
4-(3-aminophenoxy)-5-chloro-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
   Show/Hide
C22H25ClN6O2
 2
1
IC50 = 1900 nM
   TI
   LI
   LO
   TS
2
IC50 = 1960 nM
   TI
   LI
   LO
   TS
CP0408607
N-[2-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-2-hydroxyacetamide
   Show/Hide
C24H27ClN6O4
 2
1
IC50 = 2070 nM
   TI
   LI
   LO
   TS
2
IC50 = 4180 nM
   TI
   LI
   LO
   TS
CP0534556
N-[4-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]acetamide
   Show/Hide
C24H27ClN6O3
 2
1
IC50 = 2080 nM
   TI
   LI
   LO
   TS
2
IC50 = 2890 nM
   TI
   LI
   LO
   TS
CP0408613
N-[4-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-2-phenylmethoxyacetamide
   Show/Hide
C31H33ClN6O4
 2
1
IC50 = 2110 nM
   TI
   LI
   LO
   TS
2
IC50 = 3620 nM
   TI
   LI
   LO
   TS
CP0408596
N-[2-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-3-hydroxypropanamide
   Show/Hide
C25H29ClN6O4
 2
1
IC50 = 2120 nM
   TI
   LI
   LO
   TS
2
IC50 = 3860 nM
   TI
   LI
   LO
   TS
CP0408595
N-[2-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide
   Show/Hide
C25H27ClN6O3
 2
1
IC50 = 2370 nM
   TI
   LI
   LO
   TS
2
IC50 = 2920 nM
   TI
   LI
   LO
   TS
CP0408609
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-2-phenylmethoxyacetamide
   Show/Hide
C31H33ClN6O4
 2
1
IC50 = 2440 nM
   TI
   LI
   LO
   TS
2
IC50 = 2870 nM
   TI
   LI
   LO
   TS
CP0472903
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-3-phenylmethoxypropanamide
   Show/Hide
C32H35ClN6O4
 2
1
IC50 = 2470 nM
   TI
   LI
   LO
   TS
2
IC50 = 2490 nM
   TI
   LI
   LO
   TS
CP0471792
N-[4-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-2-hydroxyacetamide
   Show/Hide
C24H27ClN6O4
 2
1
IC50 = 2740 nM
   TI
   LI
   LO
   TS
2
IC50 = 6680 nM
   TI
   LI
   LO
   TS
CP0482008
4-(4-aminophenoxy)-5-chloro-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
   Show/Hide
C22H25ClN6O2
 2
1
IC50 = 2810 nM
   TI
   LI
   LO
   TS
2
IC50 = 5470 nM
   TI
   LI
   LO
   TS
CP0408612
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]acetamide
   Show/Hide
C24H27ClN6O3
 2
1
IC50 = 2910 nM
   TI
   LI
   LO
   TS
2
IC50 = 5560 nM
   TI
   LI
   LO
   TS
CP0905681
N-(2-(5-Chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)-3-benzyloxypropanamide
   Show/Hide
C32H35ClN6O4
 2
1
IC50 = 3060 nM
   TI
   LI
   LO
   TS
2
IC50 = 3120 nM
   TI
   LI
   LO
   TS
CP0408610
N-[4-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-3-hydroxypropanamide
   Show/Hide
C25H29ClN6O4
 2
1
IC50 = 3250 nM
   TI
   LI
   LO
   TS
2
IC50 = 3350 nM
   TI
   LI
   LO
   TS
CP0472905
(E)-N-[4-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-4-(dimethylamino)but-2-enamide
   Show/Hide
C28H34ClN7O3
 2
1
IC50 = 3410 nM
   TI
   LI
   LO
   TS
2
IC50 = 4720 nM
   TI
   LI
   LO
   TS
CP0432757
5-chloro-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(4-nitrophenoxy)pyrimidin-2-amine
   Show/Hide
C22H23ClN6O4
 2
1
IC50 = 3480 nM
   TI
   LI
   LO
   TS
2
IC50 = 6890 nM
   TI
   LI
   LO
   TS
CP0408652
4-(3-azidophenoxy)-5-chloro-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
   Show/Hide
C22H23ClN8O2
 2
1
IC50 = 3870 nM
   TI
   LI
   LO
   TS
2
IC50 = 4670 nM
   TI
   LI
   LO
   TS
CP0408611
N-[2-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]acetamide
   Show/Hide
C24H27ClN6O3
 2
1
IC50 = 4730 nM
   TI
   LI
   LO
   TS
2
IC50 = 8490 nM
   TI
   LI
   LO
   TS
CP0408650
5-chloro-4-(3-isothiocyanatophenoxy)-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
   Show/Hide
C23H23ClN6O2S
 2
1
IC50 = 4990 nM
   TI
   LI
   LO
   TS
2
IC50 = 8410 nM
   TI
   LI
   LO
   TS
CP0482004
5-chloro-4-(2-isothiocyanatophenoxy)-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
   Show/Hide
C23H23ClN6O2S
 2
1
IC50 = 5560 nM
   TI
   LI
   LO
   TS
2
IC50 = 8990 nM
   TI
   LI
   LO
   TS
CP0429398
4-(2-aminophenoxy)-5-chloro-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
   Show/Hide
C22H25ClN6O2
 2
1
IC50 = 5740 nM
   TI
   LI
   LO
   TS
2
IC50 = 6730 nM
   TI
   LI
   LO
   TS
CP0511869
(E)-N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-4-(dimethylamino)but-2-enamide
   Show/Hide
C28H34ClN7O3
 2
1
IC50 = 6020 nM
   TI
   LI
   LO
   TS
2
IC50 = 7020 nM
   TI
   LI
   LO
   TS
CP0482007
N-[4-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide
   Show/Hide
C25H27ClN6O3
 2
1
IC50 = 6390 nM
   TI
   LI
   LO
   TS
2
IC50 = 7700 nM
   TI
   LI
   LO
   TS
CP0432729
5-chloro-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(3-nitrophenoxy)pyrimidin-2-amine
   Show/Hide
C22H23ClN6O4
 2
1
IC50 = 6800 nM
   TI
   LI
   LO
   TS
2
IC50 = 9150 nM
   TI
   LI
   LO
   TS
CP0478344
5-chloro-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(2-nitrophenoxy)pyrimidin-2-amine
   Show/Hide
C22H23ClN6O4
 2
1
IC50 = 6810 nM
   TI
   LI
   LO
   TS
2
IC50 = 11570 nM
   TI
   LI
   LO
   TS
CP0494495
5-chloro-4-(4-isothiocyanatophenoxy)-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
   Show/Hide
C23H23ClN6O2S
 2
1
IC50 = 7500 nM
   TI
   LI
   LO
   TS
2
IC50 = 9530 nM
   TI
   LI
   LO
   TS
CP0432728
(E)-N-[2-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]-4-(dimethylamino)but-2-enamide
   Show/Hide
C28H34ClN7O3
 2
1
IC50 = 8120 nM
   TI
   LI
   LO
   TS
2
IC50 = 9100 nM
   TI
   LI
   LO
   TS
CP0059062
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide
   Show/Hide
C25H27ClN6O3
 2
1
IC50 = 9690 nM
   TI
   LI
   LO
   TS
2
IC50 = 16280 nM
   TI
   LI
   LO
   TS
CP0482006
4-(4-azidophenoxy)-5-chloro-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
   Show/Hide
C22H23ClN8O2
 2
1
IC50 = 13060 nM
   TI
   LI
   LO
   TS
2
IC50 = 15130 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
   Show/Hide
C29H31N7O
 1
1 IC50 = 10.8 nM