Target
5'-AMP-activated protein kinase subunit beta-1/5'-AMP-activated protein kinase subunit gamma-1/Dual specificity protein kinase CLK2
Ligand
BDBM50262685
Substrate
poly(Glu4, Tyr)
Meas. Tech.
in vitro Kinase Assay
IC50
234.6±0.0 nM
Citation
 Hao, JHo, JNLewis, JAKarim, KADaniels, RNGentry, PRHopkins, CRLindsley, CWHong, CC In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. ACS Chem Biol 5:245-53 (2010) [PubMed]  Article 
Target
Name:
5'-AMP-activated protein kinase subunit beta-1/5'-AMP-activated protein kinase subunit gamma-1/Dual specificity protein kinase CLK2
Synonyms:
AMP-activated protein kinase (AMPK)
Type:
PROTEIN
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 3 components.
Component 1
Name:
Dual specificity protein kinase CLK2
Synonyms:
2.7.12.1 | CDC-like kinase 2 | CDC-like kinase 2 (CLK2) | CDC2-like kinase 2 (CLK2) | CLK2 | CLK2_HUMAN
Type:
n/a
Mol. Mass.:
60128.79
Organism:
Homo sapiens (Human)
Description:
P49760
Residue:
499
Sequence:
MPHPRRYHSSERGSRGSYREHYRSRKHKRRRSRSWSSSSDRTRRRRREDSYHVRSRSSYDDRSSDRRVYDRRYCGSYRRNDYSRDRGDAYYDTDYRHSYEYQRENSSYRSQRSSRRKHRRRRRRSRTFSRSSSQHSSRRAKSVEDDAEGHLIYHVGDWLQERYEIVSTLGEGTFGRVVQCVDHRRGGARVALKIIKNVEKYKEAARLEINVLEKINEKDPDNKNLCVQMFDWFDYHGHMCISFELLGLSTFDFLKDNNYLPYPIHQVRHMAFQLCQAVKFLHDNKLTHTDLKPENILFVNSDYELTYNLEKKRDERSVKSTAVRVVDFGSATFDHEHHSTIVSTRHYRAPEVILELGWSQPCDVWSIGCIIFEYYVGFTLFQTHDNREHLAMMERILGPIPSRMIRKTRKQKYFYRGRLDWDENTSAGRYVRENCKPLRRYLTSEAEEHHQLFDLIESMLEYEPAKRLTLGEALQHPFFARLRAEPPNKLWDSSRDISR
  
Component 2
Name:
5'-AMP-activated protein kinase subunit beta-1
Synonyms:
5'-AMP-activated protein kinase subunit beta-1 | AAKB1_HUMAN | AMP-activated protein kinase alpha-2/beta-1/gamma-3 | AMPK | AMPK subunit beta-1 | AMPKb | PRKAB1
Type:
n/a
Mol. Mass.:
30380.94
Organism:
Homo sapiens (Human)
Description:
Q9Y478
Residue:
270
Sequence:
MGNTSSERAALERHGGHKTPRRDSSGGTKDGDRPKILMDSPEDADLFHSEEIKAPEKEEFLAWQHDLEVNDKAPAQARPTVFRWTGGGKEVYLSGSFNNWSKLPLTRSHNNFVAILDLPEGEHQYKFFVDGQWTHDPSEPIVTSQLGTVNNIIQVKKTDFEVFDALMVDSQKCSDVSELSSSPPGPYHQEPYVCKPEERFRAPPILPPHLLQVILNKDTGISCDPALLPEPNHVMLNHLYALSIKDGVMVLSATHRYKKKYVTTLLYKPI
  
Component 3
Name:
5'-AMP-activated protein kinase subunit gamma-1
Synonyms:
5'-AMP-activated protein kinase subunit gamma-1 | AAKG1_HUMAN | AMP-activated protein kinase, gamma-1 subunit | AMPK alpha2/beta2/gamma1 | AMPK gamma-1 | AMPK gamma1 | AMPK subunit gamma-1 | AMPKg | PRKAG1
Type:
n/a
Mol. Mass.:
37581.44
Organism:
Homo sapiens (Human)
Description:
P54619
Residue:
331
Sequence:
METVISSDSSPAVENEHPQETPESNNSVYTSFMKSHRCYDLIPTSSKLVVFDTSLQVKKAFFALVTNGVRAAPLWDSKKQSFVGMLTITDFINILHRYYKSALVQIYELEEHKIETWREVYLQDSFKPLVCISPNASLFDAVSSLIRNKIHRLPVIDPESGNTLYILTHKRILKFLKLFITEFPKPEFMSKSLEELQIGTYANIAMVRTTTPVYVALGIFVQHRVSALPVVDEKGRVVDIYSKFDVINLAAEKTYNNLDVSVTKALQHRSHYFEGVLKCYLHETLETIINRLVEAEVHRLVVVDENDVVKGIVSLSDILQALVLTGGEKKP
  
Inhibitor
Name:
BDBM50262685
Synonyms:
6-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-3-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidine | 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine | CHEMBL478629 | Dorsomorphin | US9040694, Dorsomorphin
Type:
Small organic molecule
Emp. Form.:
C24H25N5O
Mol. Mass.:
399.4882
SMILES:
C(CN1CCCCC1)Oc1ccc(cc1)-c1cnc2c(cnn2c1)-c1ccncc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
poly(Glu4, Tyr)
Synonyms:
n/a
Type:
Random copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA