Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T51282 Target Info
Target Name Rho-associated protein kinase 1 (ROCK1)
Synonyms
Rok; Rho-associated, coiled-coil containing protein kinase 1; Rho-associated kinase 1; Rho kinase; ROCK1; ROCK; P160ROCK; P160(rock); P160 ROCK-1; Let-502 kinase
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Target Type Successful Target
Gene Name ROCK1
Biochemical Class Kinase
UniProt ID
ROCK1_HUMAN
Co-Targets of This Target  Top
Co-Target Name ERK activator kinase 1 (MEK1) Clinical trial Target
UniProt ID MP2K1_HUMAN
Gene Name MAP2K1
Synonyms
PRKMK1; Mitogen-activated protein kinase kinase 1; MKK1; MEK 1; MAPKK 1; MAPK/ERKkinase 1; MAPK/ERK kinase 1; MAP kinase kinase 1; Dual specificity mitogen-activated protein kinase kinase 1
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Representative Drug(s) CI-1040 Drug Info IC50 = 2 nM Click to Show More [1]
2 CI-1040 Drug Info IC50 = 16 nM [5]
Co-Target Name Rho-associated protein kinase 2 (ROCK2) Successful Target
UniProt ID ROCK2_HUMAN
Gene Name ROCK2
Synonyms
p164 ROCK-2; Rho-associated, coiled-coil-containing protein kinase II; Rho-associated, coiled-coil-containing protein kinase 2; Rho kinase 2; ROCK-II; KIAA0619
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Representative Drug(s) GSK269962A Drug Info IC50 = 4 nM Click to Show More [2]
2 H-1152 Drug Info IC50 = 5 nM [3]
3 Fasudil Drug Info IC50 = 158 nM [7]
Co-Target Name Proto-oncogene c-RAF (c-RAF) Clinical trial Target
UniProt ID RAF1_HUMAN
Gene Name RAF1
Synonyms
cRaf; Raf-1; RAF proto-oncogene serine/threonine-protein kinase; RAF
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Representative Drug(s) CI-1040 Drug Info IC50 = 12 nM [4]
Co-Target Name Casein kinase II alpha (CSNK2A1) Clinical trial Target
UniProt ID CSK21_HUMAN
Gene Name CSNK2A1
Synonyms
Protein kinase CK2; Casein kinase II subunit alpha; CK2A1; CK II alpha; CK II
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Representative Drug(s) CI-1040 Drug Info IC50 = 17 nM [6]
Co-Target Name Casein kinase II (CSNK2) Clinical trial Target
UniProt ID CSK21_HUMAN; CSK22_HUMAN; CSK23_HUMAN; CSK2B_HUMAN
Gene Name NO-GeName
Representative Drug(s) CI-1040 Drug Info EC50 = 100 nM [6]
Co-Target Name Leucine-rich repeat kinase 2 (LRRK2) Clinical trial Target
UniProt ID LRRK2_HUMAN
Gene Name LRRK2
Synonyms
PARK8; Leucine-rich repeat serine/threonine-protein kinase 2; Dardarin
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Representative Drug(s) H-1152 Drug Info IC50 = 244 nM [8]
Co-Target Name RAC-alpha serine/threonine-protein kinase (AKT1) Clinical trial Target
UniProt ID AKT1_HUMAN
Gene Name AKT1
Synonyms
RAC-PK-alpha; RAC; Proto-oncogene c-Akt; Protein kinase B alpha; PKB alpha
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Representative Drug(s) GSK269962A Drug Info IC50 = 955 nM [2]
Co-Target Name Ribosomal protein S6 kinase alpha-5 (RSK5) Patented-recorded Target
UniProt ID KS6A5_HUMAN
Gene Name RPS6KA5
Synonyms
S6K-alpha-5; RSKL; RSK-like protein kinase; Nuclear mitogen- and stress-activated protein kinase 1; MSK1; 90 kDa ribosomal protein S6 kinase 5
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Representative Drug(s) GSK269962A Drug Info IC50 = 49 nM [2]
Co-Target Name Ribosomal protein S6 kinase alpha-1 (RSK1) Patented-recorded Target
UniProt ID KS6A1_HUMAN
Gene Name RPS6KA1
Synonyms
p90S6K; p90RSK1; p90-RSK 1; S6K-alpha-1; Ribosomal S6 kinase 1; RSK-1; MAPKAPK1A; MAPKAPK-1a; MAPKAP kinase 1a; MAPK-activated protein kinase 1a; MAP kinase-activated protein kinase 1a; 90 kDa ribosomal protein S6 kinase 1
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Representative Drug(s) GSK269962A Drug Info IC50 = 132 nM [2]
Co-Target Name Protein kinase N2 (PKN2) Literature-reported Target
UniProt ID PKN2_HUMAN
Gene Name PKN2
Synonyms
Serine/threonine-protein kinase N2; Protein-kinase C-related kinase 2; Protein kinase C-like 2; PRKCL2; PRK2; PKN gamma
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Representative Drug(s) Fasudil Drug Info IC50 = 780 nM [9]
Co-Target Name cAMP-dependent protein kinase (PKA) Co-Target
UniProt ID KAPCA_HUMAN; KAPCB_HUMAN; KAPCG_HUMAN
Gene Name PRKACA; PRKACB; PRKACG
Synonyms
PKA C
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Representative Drug(s) H-1152 Drug Info Ki = 340 nM Click to Show More [10]
2 Fasudil Drug Info Ki = 460 nM [10]
References  Top
REF 1 Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3031-4.
REF 2 Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98.
REF 3 Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4812-7.
REF 4 Pharmacophore identification of Raf-1 kinase inhibitors. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2346-50.
REF 5 4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase. J Med Chem. 2007 Oct 18;50(21):5090-102.
REF 6 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. J Med Chem. 2019 Feb 28;62(4):1817-1836.
REF 7 Advances in the studies of roles of Rho/Rho-kinase in diseases and the development of its inhibitors. Eur J Med Chem. 2013;70:613-22.
REF 8 The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3690-6.
REF 9 Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3235-9.
REF 10 The structure of dimeric ROCK I reveals the mechanism for ligand selectivity. J Biol Chem. 2006 Jan 6;281(1):260-8.

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