Protein Information

General Information of the Protein

Protein ID	PT01754
Protein Name	Activated CDC42 kinase 1
Secondarily Protein Name	Tyrosine kinase non-receptor protein 2
Gene Name	TNK2
Secondarily Gene Name	ACK1
Sequence	MQPEEGTGWLLELLSEVQLQQYFLRLRDDLNVTRLSHFEYVKNEDLEKIGMGRPGQRRLWEAVKRRKALCKRKSWMSKVFSGKRLEAEFPPHHSQSTFRKTSPAPGGPAGEGPLQSLTCLIGEKDLRLLEKLGDGSFGVVRRGEWDAPSGKTVSVAVKCLKPDVLSQPEAMDDFIREVNAMHSLDHRNLIRLYGVVLTPPMKMVTELAPLGSLLDRLRKHQGHFLLGTLSRYAVQVAEGMGYLESKRFIHRDLAARNLLLATRDLVKIGDFGLMRALPQNDDHYVMQEHRKVPFAWCAPESLKTRTFSHASDTWMFGVTLWEMFTYGQEPWIGLNGSQILHKIDKEGERLPRPEDCPQDIYNVMVQCWAHKPEDRPTFVALRDFLLEAQPTDMRALQDFEEPDKLHIQMNDVITVIEGRAENYWWRGQNTRTLCVGPFPRNVVTSVAGLSAQDISQPLQNSFIHTGHGDSDPRHCWGFPDRIDELYLGNPMDPPDLLSVELSTSRPPQHLGGVKKPTYDPVSEDQDPLSSDFKRLGLRKPGLPRGLWLAKPSARVPGTKASRGSGAEVTLIDFGEEPVVPALRPCAPSLAQLAMDACSLLDETPPQSPTRALPRPLHPTPVVDWDARPLPPPPAYDDVAQDEDDFEICSINSTLVGAGVPAGPSQGQTNYAFVPEQARPPPPLEDNLFLPPQGGGKPPSSAQTAEIFQALQQECMRQLQAPAGSPAPSPSPGGDDKPQVPPRVPIPPRPTRPHVQLSPAPPGEEETSQWPGPASPPRVPPREPLSPQGSRTPSPLVPPGSSPLPPRLSSSPGKTMPTTQSFASDPKYATPQVIQAPGPRAGPCILPIVRDGKKVSSTHYYLLPERPSYLERYQRFLREAQSPEEPTPLPVPLLLPPPSTPAPAAPTATVRPMPQAALDPKANFSTNNSNPGARPPPPRATARLPQRGCPGDGPEAGRPADKIQMAMVHGVTTEECQAALQCHGWSVQRAAQYLKVEQLFGLGLRPRGECHKVLEMFDWNLEQAGCHLLGSWGPAHHKR Show/Hide
Organism	Homo sapiens, Human
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. Phosphorylates WASP (PubMed:20110370). Show/Hide
Uniprot ID	Primary ID: Q07912 Secondarily ID: Q6ZMQ0 Q8N6U7 Q96H59 Show/Hide
Ensembl ID	ENSG00000061938
HGNC ID	HGNC:19297
Subcellular Location	Cell membrane Nucleus Endosome Cell junction Adherens junction Cytoplasmic vesicle membrane Cytoplasmic vesicle Clathrin-coated vesicle Membrane Clathrin-coated pit Cytoplasm Perinuclear region 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: CL000023 , BTI-Tn-5B1-4

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0088957 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-(1,3-dithiolan-2-ylmethyl)-5-phenylfuro[2,3-d]pyrimidin-4-amine Show/Hide	C26H28N4O2S2	1
1	Ki = 0.2 nM Bioactivity Info	TI LI LO TS
CP0044001 Compound Info	N-(1,3-dithiolan-2-ylmethyl)-5-phenyl-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C28H31N5OS2	1
1	Ki = 0.3 nM Bioactivity Info	TI LI LO TS
CP0427768 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-(1,3-dithiolan-2-ylmethyl)-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C26H29N5OS2	1
1	Ki = 0.3 nM Bioactivity Info	TI LI LO TS
CP0375828 Compound Info	N,N-dimethyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]benzenesulfonamide Show/Hide	C25H27N5O3S	1
1	Ki = 2 nM Bioactivity Info	TI LI LO TS
CP0436198 Compound Info	N,N-dimethyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]benzamide Show/Hide	C26H27N5O2	1
1	Ki = 2 nM Bioactivity Info	TI LI LO TS
CP0494810 Compound Info	N-methyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]benzenesulfonamide Show/Hide	C24H25N5O3S	1
1	Ki = 2 nM Bioactivity Info	TI LI LO TS
CP0412467 Compound Info	N-methyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]benzamide Show/Hide	C25H25N5O2	1
1	Ki = 3 nM Bioactivity Info	TI LI LO TS
CP0416244 Compound Info	5-(2-fluorophenyl)-N-[[(2S)-oxolan-2-yl]methyl]-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C29H32FN5O2	1
1	Ki = 4 nM Bioactivity Info	TI LI LO TS
CP0427773 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-(1,3-dithian-2-ylmethyl)-5-phenylfuro[2,3-d]pyrimidin-4-amine Show/Hide	C27H30N4O2S2	1
1	Ki = 4 nM Bioactivity Info	TI LI LO TS
CP0436122 Compound Info	N-methyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenylfuro[2,3-d]pyrimidin-6-yl]benzenesulfonamide Show/Hide	C24H24N4O4S	1
1	Ki = 4 nM Bioactivity Info	TI LI LO TS
CP0436123 Compound Info	6-[4-(2-morpholin-4-ylethoxy)phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-5-phenylfuro[2,3-d]pyrimidin-4-amine Show/Hide	C29H32N4O4	1
1	Ki = 4 nM Bioactivity Info	TI LI LO TS
CP0481030 Compound Info	1-[2-[4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenoxy]ethyl]pyrrolidin-2-one Show/Hide	C29H31N5O3	1
1	Ki = 4 nM Bioactivity Info	TI LI LO TS
CP0514810 Compound Info	1-[2-[4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenylfuro[2,3-d]pyrimidin-6-yl]phenoxy]ethyl]pyrrolidin-2-one Show/Hide	C29H30N4O4	1
1	Ki = 4 nM Bioactivity Info	TI LI LO TS
CP0200044 Compound Info	(S)-6-(4-(2-(dimethylamino)ethoxy)phenyl)-5-phenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine Show/Hide	C27H30N4O3	1
1	Ki = 5 nM Bioactivity Info	TI LI LO TS
CP0544603 Compound Info	6-(4-methoxyphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-5-phenylfuro[2,3-d]pyrimidin-4-amine Show/Hide	C24H23N3O3	1
1	Ki = 5 nM Bioactivity Info	TI LI LO TS
CP0380624 Compound Info	N-[[(2S)-oxolan-2-yl]methyl]-5-phenyl-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C29H33N5O2	1
1	Ki = 6 nM Bioactivity Info	TI LI LO TS
CP0427769 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C27H31N5O2	1
1	Ki = 6 nM Bioactivity Info	TI LI LO TS
CP0436121 Compound Info	6-(4-methoxyphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C24H24N4O2	1
1	Ki = 6 nM Bioactivity Info	TI LI LO TS
CP0481031 Compound Info	morpholin-4-yl-[4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenylfuro[2,3-d]pyrimidin-6-yl]phenyl]methanone Show/Hide	C28H28N4O4	1
1	Ki = 6 nM Bioactivity Info	TI LI LO TS
CP0488094 Compound Info	6-[4-(2-morpholin-4-ylethoxy)phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C29H33N5O3	1
1	Ki = 6 nM Bioactivity Info	TI LI LO TS
CP0544599 Compound Info	N-[[(2S)-oxolan-2-yl]methyl]-5,6-diphenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C23H22N4O	1
1	Ki = 6 nM Bioactivity Info	TI LI LO TS
CP0544604 Compound Info	morpholin-4-yl-[4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]methanone Show/Hide	C28H29N5O3	1
1	Ki = 6 nM Bioactivity Info	TI LI LO TS
CP0375827 Compound Info	6-(4-methylsulfonylphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C24H24N4O3S	1
1	Ki = 7 nM Bioactivity Info	TI LI LO TS
CP0507343 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-5-phenyl-N-(thiolan-2-ylmethyl)furo[2,3-d]pyrimidin-4-amine Show/Hide	C27H30N4O2S	1
1	Ki = 8 nM Bioactivity Info	TI LI LO TS
CP0514809 Compound Info	6-(4-methylsulfonylphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-5-phenylfuro[2,3-d]pyrimidin-4-amine Show/Hide	C24H23N3O4S	1
1	Ki = 8 nM Bioactivity Info	TI LI LO TS
CP0424082 Compound Info	5-(cyclohexen-1-yl)-6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C27H35N5O2	1
1	Ki = 10 nM Bioactivity Info	TI LI LO TS
CP0533374 Compound Info	5-(3-methoxyphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C30H35N5O3	1
1	Ki = 10 nM Bioactivity Info	TI LI LO TS
CP0544600 Compound Info	N,N-dimethyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenylfuro[2,3-d]pyrimidin-6-yl]benzamide Show/Hide	C26H26N4O3	1
1	Ki = 10 nM Bioactivity Info	TI LI LO TS
CP0436124 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-(1,3-dioxolan-2-ylmethyl)-5-phenylfuro[2,3-d]pyrimidin-4-amine Show/Hide	C26H28N4O4	1
1	Ki = 13 nM Bioactivity Info	TI LI LO TS
CP0530374 Compound Info	N-methyl-4-[4-[[(2S)-oxolan-2-yl]methylamino]-5-phenylfuro[2,3-d]pyrimidin-6-yl]benzamide Show/Hide	C25H24N4O3	1
1	Ki = 13 nM Bioactivity Info	TI LI LO TS
CP0540569 Compound Info	5-(cyclopenten-1-yl)-6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C26H33N5O2	1
1	Ki = 20 nM Bioactivity Info	TI LI LO TS
CP0544601 Compound Info	5-(2-methylphenyl)-N-[[(2S)-oxolan-2-yl]methyl]-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C30H35N5O2	1
1	Ki = 20 nM Bioactivity Info	TI LI LO TS
CP0544605 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(1S,2R)-2-methoxycyclobutyl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C28H33N5O2	1
1	Ki = 20 nM Bioactivity Info	TI LI LO TS
CP0544602 Compound Info	(1R,2S)-2-[[[6-[4-[2-(dimethylamino)ethoxy]phenyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]methyl]cyclobutan-1-ol Show/Hide	C27H31N5O2	1
1	Ki = 30 nM Bioactivity Info	TI LI LO TS
CP0436125 Compound Info	(1R,2R)-2-[[[6-[4-[2-(dimethylamino)ethoxy]phenyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]methyl]cyclopentan-1-ol Show/Hide	C28H33N5O2	1
1	Ki = 40 nM Bioactivity Info	TI LI LO TS
CP0507342 Compound Info	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 Show/Hide	C28H32N6O2	1
1	Ki = 40 nM Bioactivity Info	TI LI LO TS
CP0416245 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(1R,2R)-2-methoxycyclopentyl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C29H35N5O2	1
1	Ki = 50 nM Bioactivity Info	TI LI LO TS
CP0494811 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(1S,2R)-2-methoxycyclopentyl]methyl]-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C29H35N5O2	1
1	Ki = 50 nM Bioactivity Info	TI LI LO TS
CP0375829 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-5-phenyl-N-[[(2S)-thian-2-yl]methyl]furo[2,3-d]pyrimidin-4-amine Show/Hide	C28H32N4O2S	1
1	Ki = 69 nM Bioactivity Info	TI LI LO TS
CP0344507 Compound Info	2,3-Diarylfuro[2,3-b]pyridine-4-amine, 6 Show/Hide	C24H22N2O2	1
1	Ki = 70 nM Bioactivity Info	TI LI LO TS
CP0541375 Compound Info	N-[[(2S)-oxolan-2-yl]methyl]-6,7-diphenylimidazo[1,2-a][1,3,5]triazin-4-amine Show/Hide	C22H21N5O	1
1	Ki = 1800 nM Bioactivity Info	TI LI LO TS
CP0416243 Compound Info	5-cyclopropyl-6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-[[(2S)-oxolan-2-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C24H31N5O2	1
1	Ki = 1980 nM Bioactivity Info	TI LI LO TS
CP0412608 Compound Info	N-[[(2S)-oxolan-2-yl]methyl]-7,8-diphenylpurin-6-amine Show/Hide	C22H21N5O	1
1	Ki = 7300 nM Bioactivity Info	TI LI LO TS
CP0514806 Compound Info	N-[[(2S)-oxolan-2-yl]methyl]-5,6-diphenylthieno[2,3-d]pyrimidin-4-amine Show/Hide	C23H21N3OS	1
1	Ki > 10000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0187287 Compound Info	3-N-(2,6-dimethylphenyl)-1-(3-methoxy-3-methylbutyl)-6-N-phenylpyrazolo[3,4-d]pyrimidine-3,6-diamine Show/Hide	C25H30N6O	1
1	IC50 = 2 nM
CP0044001 Compound Info	N-(1,3-dithiolan-2-ylmethyl)-5-phenyl-6-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine Show/Hide	C28H31N5OS2	1
1	IC50 = 10 nM
CP0200044 Compound Info	(S)-6-(4-(2-(dimethylamino)ethoxy)phenyl)-5-phenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine Show/Hide	C27H30N4O3	1
1	IC50 = 11 nM
CP0035505 Compound Info	3-N-(2,6-dimethylphenyl)-6-N-[3-fluoro-4-(2-pyrrolidin-1-ylethoxy)phenyl]-1-(3-methoxy-3-methylbutyl)pyrazolo[3,4-d]pyrimidine-3,6-diamine Show/Hide	C31H40FN7O2	1
1	IC50 = 20 nM
CP0493899 Compound Info	3-N-(2,6-dimethylphenyl)-1-(3-methoxy-3-methylbutyl)-6-N-(4-piperazin-1-ylphenyl)pyrazolo[3,4-d]pyrimidine-3,6-diamine Show/Hide	C29H38N8O	1
1	IC50 = 20 nM
CP0344507 Compound Info	2,3-Diarylfuro[2,3-b]pyridine-4-amine, 6 Show/Hide	C24H22N2O2	1
1	IC50 = 110 nM
CP0088957 Compound Info	6-[4-[2-(dimethylamino)ethoxy]phenyl]-N-(1,3-dithiolan-2-ylmethyl)-5-phenylfuro[2,3-d]pyrimidin-4-amine Show/Hide	C26H28N4O2S2	1
1	Ki = 0.3 nM

Clinical Information about the Protein

Target 1 ( Activated CDC42 kinase 1 (ACK-1) )

Target Type	Patented-recorded Target

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT06503	Activated CDC42 kinase 1	Mus musculus, Mouse	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han