General Information of the Protein
Protein ID
PT06503
Protein Name
Activated CDC42 kinase 1
Secondarily
Protein Name
Non-receptor protein tyrosine kinase Ack
Tyrosine kinase non-receptor protein 2
Gene Name
TNK2
Secondarily
Gene Name
Ack1
Sequence
MQPEEGTGWLLELLSEVQLQQYFLRLRDDLNITRLSHFEYVKNEDLEKIGMGRPGQRRLWEAVKRRKAMCKRKSWMSKVFSGKRLEAEFPSQHSQSTFRKPSPTPGSLPGEGTLQSLTCLIGEKDLRLLEKLGDGSFGVVRRGEWDAPAGKTVSVAVKCLKPDVLSQPEAMDDFIREVNAMHSLDHRNLIRLYGVVLTLPMKMVTELAPLGSLLDRLRKHQGHFLLGTLSRYAVQVAEGMAYLESKRFIHRDLAARNLLLATRDLVKIGDFGLMRALPQNDDHYVMQEHRKVPFAWCAPESLKTRTFSHASDTWMFGVTLWEMFTYGQEPWIGLNGSQILHKIDKEGERLPRPEDCPQDIYNVMVQCWAHKPEDRPTFVALRDFLLEAQPTDMRALQDFEEPDKLHIQMNDVITVIEGRAENYWWRGQNTRTLCVGPFPRNVVTSVAGLSAQDISQPLQNSFIHTGHGDSDPRHCWGFPDRIDELYLGNPMDPPDLLSVELSTSRPTQHLGRVKREPPPRPPQPAIFTQKTTYDPVSEDPDPLSSDFKRLGLRKPALPRGLWLAKPSARVPGTKADRSSGGEVTLIDFGEEPVVPTPRPCAPSLAQLAMDACSLLDKTPPQSPTRALPRPLHPTPVVDWDARPLPPPPAYDDVAQDEDDFEVCSINSTLVGAGLPAGPSQGETNYAFVPEQAQMPPALEDNLFLPPQGGGKPPSSVQTAEIFQALQQECMRQLQVPTGQLTPSPTPGGDDKPQVPPRVPIPPRPTRPRVELSPAPSGEEETSRWPGPASPPRVPPREPLSPQGSRTPSPLVPPGSSPLPHRLSSSPGKTMPTTQSFASDPKYATPQVIQAPGPRAGPCILPIVRDGRKVSSTHYYLLPERPPYLERYQRFLREAQSPEEPAALPVPPLLPPPSTPAPAAPTATVRPMPQAAPDPKANFSTNNSNPGARPPSLRAAARLPQRGCPGDGQEAARPADKVQMLQAMVHGVTTEECQAALQSHSWSVQRAAQYLKVEQLFGLGLRPRVECHKVLEMFDWNLEQAGCHLLGSCGPAHHKR
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Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Ack family
Function
Non-receptor tyrosine-protein and serine/threonine-protein kinase that is implicated in cell spreading and migration, cell survival, cell growth and proliferation. Transduces extracellular signals to cytosolic and nuclear effectors. Phosphorylates AKT1, AR, MCF2, WASL and WWOX. Implicated in trafficking and clathrin-mediated endocytosis through binding to epidermal growth factor receptor (EGFR) and clathrin. Binds to both poly- and mono-ubiquitin and regulates ligand-induced degradation of EGFR, thereby contributing to the accumulation of EGFR at the limiting membrane of early endosomes. Downstream effector of CDC42 which mediates CDC42-dependent cell migration via phosphorylation of BCAR1. May be involved both in adult synaptic function and plasticity and in brain development. Activates AKT1 by phosphorylating it on 'Tyr-176'. Phosphorylates AR on 'Tyr-267' and 'Tyr-363' thereby promoting its recruitment to androgen-responsive enhancers (AREs). Phosphorylates WWOX on 'Tyr-287'. Phosphorylates MCF2, thereby enhancing its activity as a guanine nucleotide exchange factor (GEF) toward Rho family proteins. Contributes to the control of AXL receptor levels. Confers metastatic properties on cancer cells and promotes tumor growth by negatively regulating tumor suppressor such as WWOX and positively regulating pro-survival factors such as AKT1 and AR.
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Uniprot ID
Primary ID:
O54967

Secondarily ID:
Q0Z844
Q8C2U0
Q8K0K4
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Ensembl ID
ENSG00000061938
Subcellular Location
Cell membrane
Nucleus
Endosome
Cell junction
Adherens junction
Cytoplasmic vesicle membrane
Cytoplasmic vesicle
Clathrin-coated vesicle
Membrane
Clathrin-coated pit
Cytoplasm
Cytosol
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: CL000421 , C8 [Human colon adenocarcinoma]
Compound ID Compound Name Compound Formula
CP0427768
6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-(1,3-dithiolan-2-ylmethyl)-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C26H29N5OS2
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0044001
N-(1,3-dithiolan-2-ylmethyl)-5-phenyl-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C28H31N5OS2
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0088957
6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-(1,3-dithiolan-2-ylmethyl)-5-phenylfuro[2,3-d]pyrimidin-4-amine
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C26H28N4O2S2
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0427769
6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C27H31N5O2
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0436198
N,N-dimethyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]benzamide
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C26H27N5O2
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0481030
1-[2-[4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenoxy]ethyl]pyrrolidin-2-one
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C29H31N5O3
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0544604
morpholin-4-yl-[4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]methanone
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C28H29N5O3
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0200044
(S)-6-(4-(2-(dimethylamino)ethoxy)phenyl)-5-phenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine
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C27H30N4O3
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0412467
N-methyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]benzamide
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C25H25N5O2
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0416244
5-(2-fluorophenyl)-N-[[(2S)-oxolan-2-yl]methyl]-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C29H32FN5O2
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0494810
N-methyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]benzenesulfonamide
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C24H25N5O3S
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0380624
N-[[(2S)-oxolan-2-yl]methyl]-5-phenyl-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C29H33N5O2
 1
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
CP0488094
6-[4-(2-morpholin-4-ylethoxy)phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C29H33N5O3
 1
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
CP0375828
N,N-dimethyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]benzenesulfonamide
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C25H27N5O3S
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0375827
6-(4-methylsulfonylphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C24H24N4O3S
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0436123
6-[4-(2-morpholin-4-ylethoxy)phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-5-phenylfuro[2,3-d]pyrimidin-4-amine
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C29H32N4O4
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0533374
5-(3-methoxyphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C30H35N5O3
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0544601
5-(2-methylphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C30H35N5O2
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0544600
N,N-dimethyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenylfuro[2,3-d]pyrimidin-6-yl]benzamide
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C26H26N4O3
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0481031
morpholin-4-yl-[4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenylfuro[2,3-d]pyrimidin-6-yl]phenyl]methanone
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C28H28N4O4
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0514810
1-[2-[4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenylfuro[2,3-d]pyrimidin-6-yl]phenoxy]ethyl]pyrrolidin-2-one
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C29H30N4O4
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0540569
5-(cyclopenten-1-yl)-6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C26H33N5O2
 1
1
IC50 = 240 nM
   TI
   LI
   LO
   TS
CP0514809
6-(4-methylsulfonylphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-5-phenylfuro[2,3-d]pyrimidin-4-amine
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C24H23N3O4S
 1
1
IC50 = 250 nM
   TI
   LI
   LO
   TS
CP0436122
N-methyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenylfuro[2,3-d]pyrimidin-6-yl]benzenesulfonamide
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C24H24N4O4S
 1
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0436121
6-(4-methoxyphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C24H24N4O2
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0507342
N-[[(2S)-oxolan-2-yl]methyl]-5-pyridin-3-yl-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C28H32N6O2
 1
1
IC50 = 390 nM
   TI
   LI
   LO
   TS
CP0544602
(1R,2S)-2-[[[6-[4-[2-(dimethylamino)ethoxy]phenyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]methyl]cyclobutan-1-ol
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C27H31N5O2
 1
1
IC50 = 410 nM
   TI
   LI
   LO
   TS
CP0544605
6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(1S,2R)-2-methoxycyclobutyl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C28H33N5O2
 1
1
IC50 = 420 nM
   TI
   LI
   LO
   TS
CP0436125
(1R,2R)-2-[[[6-[4-[2-(dimethylamino)ethoxy]phenyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]methyl]cyclopentan-1-ol
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C28H33N5O2
 1
1
IC50 = 460 nM
   TI
   LI
   LO
   TS
CP0424082
5-(cyclohexen-1-yl)-6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C27H35N5O2
 1
1
IC50 = 500 nM
   TI
   LI
   LO
   TS
CP0427773
6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-(1,3-dithian-2-ylmethyl)-5-phenylfuro[2,3-d]pyrimidin-4-amine
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C27H30N4O2S2
 1
1
IC50 = 550 nM
   TI
   LI
   LO
   TS
CP0544603
6-(4-methoxyphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-5-phenylfuro[2,3-d]pyrimidin-4-amine
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C24H23N3O3
 1
1
IC50 = 550 nM
   TI
   LI
   LO
   TS
CP0544599
N-[[(2S)-oxolan-2-yl]methyl]-5,6-diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C23H22N4O
 1
1
IC50 = 620 nM
   TI
   LI
   LO
   TS
CP0416245
6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(1R,2R)-2-methoxycyclopentyl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C29H35N5O2
 1
1
IC50 = 780 nM
   TI
   LI
   LO
   TS
CP0494811
6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(1S,2R)-2-methoxycyclopentyl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C29H35N5O2
 1
1
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0436124
6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-(1,3-dioxolan-2-ylmethyl)-5-phenylfuro[2,3-d]pyrimidin-4-amine
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C26H28N4O4
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0530374
N-methyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenylfuro[2,3-d]pyrimidin-6-yl]benzamide
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C25H24N4O3
 1
1
IC50 = 2050 nM
   TI
   LI
   LO
   TS
CP0507343
6-[4-[2-(dimethylamino)ethoxy]phenyl]-5-phenyl-N-(thiolan-2-ylmethyl)furo[2,3-d]pyrimidin-4-amine
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C27H30N4O2S
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0344507
2,3-Diarylfuro[2,3-b]pyridine-4-amine, 6
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C24H22N2O2
 1
1
IC50 = 5600 nM
   TI
   LI
   LO
   TS
CP0375829
6-[4-[2-(dimethylamino)ethoxy]phenyl]-5-phenyl-N-[[(2S)-thian-2-yl]methyl]furo[2,3-d]pyrimidin-4-amine
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C28H32N4O2S
 1
1
IC50 = 7160 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01754 Activated CDC42 kinase 1 Homo sapiens, Human