General Information of the Protein
Protein ID
PT05677
Protein Name
Transforming protein RhoA
Secondarily
Protein Name
Rho cDNA clone 12
Gene Name
RHOA
Secondarily
Gene Name
ARH12
ARHA
RHO12
Sequence
MAAIRKKLVIVGDGACGKTCLLIVFSKDQFPEVYVPTVFENYVADIEVDGKQVELALWDTAGQEDYDRLRPLSYPDTDVILMCFSIDSPDSLENIPEKWTPEVKHFCPNVPIILVGNKKDLRNDEHTRRELAKMKQEPVKPEEGRDMANRIGAFGYMECSAKTKDGVREVFEMATRAALQARRGKKKSGCLVL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Hydrolase
Function
Small GTPase which cycles between an active GTP-bound and an inactive GDP-bound state. Mainly associated with cytoskeleton organization, in active state binds to a variety of effector proteins to regulate cellular responses such as cytoskeletal dynamics, cell migration and cell cycle (PubMed:23871831). Regulates a signal transduction pathway linking plasma membrane receptors to the assembly of focal adhesions and actin stress fibers (PubMed:8910519, PubMed:9121475, PubMed:31570889). Involved in a microtubule-dependent signal that is required for the myosin contractile ring formation during cell cycle cytokinesis (PubMed:16236794, PubMed:12900402). Plays an essential role in cleavage furrow formation. Required for the apical junction formation of keratinocyte cell-cell adhesion (PubMed:20974804, PubMed:23940119). Essential for the SPATA13-mediated regulation of cell migration and adhesion assembly and disassembly (PubMed:19934221). The MEMO1-RHOA-DIAPH1 signaling pathway plays an important role in ERBB2-dependent stabilization of microtubules at the cell cortex. It controls the localization of APC and CLASP2 to the cell membrane, via the regulation of GSK3B activity. In turn, membrane-bound APC allows the localization of the MACF1 to the cell membrane, which is required for microtubule capture and stabilization (PubMed:20937854). Regulates KCNA2 potassium channel activity by reducing its location at the cell surface in response to CHRM1 activation; promotes KCNA2 endocytosis (PubMed:9635436, PubMed:19403695). Acts as an allosteric activator of guanine nucleotide exchange factor ECT2 by binding in its activated GTP-bound form to the PH domain of ECT2 which stimulates the release of PH inhibition and promotes the binding of substrate RHOA to the ECT2 catalytic center (PubMed:31888991). May be an activator of PLCE1 (PubMed:16103226). In neurons, involved in the inhibition of the initial spine growth. Upon activation by CaMKII, modulates dendritic spine structural plasticity by relaying CaMKII transient activation to synapse-specific, long-term signaling (By similarity). Acts as a regulator of platelet alpha-granule release during activation and aggregation of platelets (By similarity).
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Uniprot ID
Primary ID:
P61586

Secondarily ID:
P06749
Q53HM4
Q5U024
Q9UDJ0
Q9UEJ4
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Ensembl ID
ENSG00000067560
HGNC ID
HGNC:667
Subcellular Location
Cell membrane
Cytoplasm
Cytoskeleton
Cleavage furrow
Cytoplasm
Cell cortex
Midbody
Cell projection
Lamellipodium
Cell projection
Dendrite
Nucleus
Cytoplasm
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: CL000048 , PC-3
Compound ID Compound Name Compound Formula
CP0456820
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(3-phenoxyphenyl)piperidine-3-carboxamide
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C27H22F6N2O3
 1
1
IC50 = 1500 nM
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CP0515298
N-(3-benzylphenyl)-1-[3,5-bis(trifluoromethyl)benzoyl]piperidine-3-carboxamide
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C28H24F6N2O2
 1
1
IC50 = 1600 nM
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CP0387745
1-[3,5-bis(trifluoromethyl)benzoyl]-N-[3-(2-pyridin-2-ylethoxy)phenyl]piperidine-3-carboxamide
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C28H25F6N3O3
 1
1
IC50 = 2300 nM
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CP0374941
N-(4-chlorophenyl)-1-(3-thiophen-2-ylbenzoyl)piperidine-3-carboxamide
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C23H21ClN2O2S
 1
1
IC50 = 4700 nM
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CP0465342
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(3-pyrrolidin-1-ylsulfonylphenyl)piperidine-3-carboxamide
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C25H25F6N3O4S
 1
1
IC50 = 5600 nM
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CP0380537
1-[3,5-bis(trifluoromethyl)benzoyl]-N-[3-(2-methyl-1,3-thiazol-4-yl)phenyl]piperidine-3-carboxamide
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C25H21F6N3O2S
 1
1
IC50 = 6100 nM
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CP0404550
N-(4-chlorophenyl)-1-[3-(furan-2-yl)benzoyl]piperidine-3-carboxamide
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C23H21ClN2O3
 1
1
IC50 = 6400 nM
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CP0456317
1-[3,5-bis(trifluoromethyl)benzoyl]-N-[3-(pyridin-2-ylmethoxy)phenyl]piperidine-3-carboxamide
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C27H23F6N3O3
 1
1
IC50 = 7400 nM
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CP0387744
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(3-ethylphenyl)piperidine-3-carboxamide
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C23H22F6N2O2
 1
1
IC50 = 8100 nM
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CP0407139
N-(4-chlorophenyl)-1-[4-(furan-2-yl)benzoyl]piperidine-3-carboxamide
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C23H21ClN2O3
 1
1
IC50 = 9200 nM
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CP0556314
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(4-chlorophenyl)piperidine-3-carboxamide
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C21H17ClF6N2O2
 1
1
IC50 = 9800 nM
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CP0374951
1-(3-benzoylbenzoyl)-N-(4-chlorophenyl)piperidine-3-carboxamide
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C26H23ClN2O3
 1
1
IC50 = 9900 nM
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CP0387743
1-[3-(furan-2-yl)benzoyl]-N-(3-methylsulfanylphenyl)piperidine-3-carboxamide
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C24H24N2O3S
 1
1
IC50 = 10000 nM
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CP0525715
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(3-pyridin-2-yloxyphenyl)piperidine-3-carboxamide
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C26H21F6N3O3
 1
1
IC50 = 10000 nM
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CP0527472
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(3-ethenylphenyl)piperidine-3-carboxamide
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C23H20F6N2O2
 1
1
IC50 = 11000 nM
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CP0374945
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(3-methylsulfanylphenyl)piperidine-3-carboxamide
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C22H20F6N2O2S
 1
1
IC50 = 12000 nM
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CP0374946
1-[3,5-bis(trifluoromethyl)benzoyl]-N-[3-(1,3-oxazol-5-yl)phenyl]piperidine-3-carboxamide
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C24H19F6N3O3
 1
1
IC50 = 12000 nM
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CP0407138
1-[3,5-bis(trifluoromethyl)benzoyl]-N-[3-(furan-2-yl)phenyl]piperidine-3-carboxamide
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C25H20F6N2O3
 1
1
IC50 = 21000 nM
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CP0387741
methyl 3-[[1-[3,5-bis(trifluoromethyl)benzoyl]piperidine-3-carbonyl]amino]benzoate
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C23H20F6N2O4
 1
1
IC50 = 26000 nM
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CP0465341
N-(4-chlorophenyl)-1-[3-(3,3-dimethylbutanoylamino)benzoyl]piperidine-3-carboxamide
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C25H30ClN3O3
 1
1
IC50 = 26000 nM
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CP0374950
N-(4-chlorophenyl)-1-[3-(1,3-thiazol-2-yl)benzoyl]piperidine-3-carboxamide
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C22H20ClN3O2S
 1
1
IC50 = 27000 nM
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CP0374949
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(3-methoxyphenyl)piperidine-3-carboxamide
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C22H20F6N2O3
 1
1
IC50 = 30000 nM
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CP0396493
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(6-chloropyridin-3-yl)piperidine-3-carboxamide
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C20H16ClF6N3O2
 1
1
IC50 = 31000 nM
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CP0374944
1-[3,5-bis(trifluoromethyl)benzoyl]-N-[3-(morpholin-4-ylmethyl)phenyl]piperidine-3-carboxamide
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C26H27F6N3O3
 1
1
IC50 = 32000 nM
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CP0433692
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(3-cyanophenyl)piperidine-3-carboxamide
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C22H17F6N3O2
 1
1
IC50 = 32000 nM
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CP0387742
N-(4-chlorophenyl)-1-[3-(2-methyl-1,3-thiazol-4-yl)benzoyl]piperidine-3-carboxamide
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C23H22ClN3O2S
 1
1
IC50 = 33000 nM
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CP0456819
N-(4-chlorophenyl)-1-(3-ethenylbenzoyl)piperidine-3-carboxamide
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C21H21ClN2O2
 1
1
IC50 = 33000 nM
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CP0515297
N-(4-chlorophenyl)-1-(3-methylsulfanylbenzoyl)piperidine-3-carboxamide
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C20H21ClN2O2S
 1
1
IC50 = 35000 nM
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CP0525714
N-(4-chlorophenyl)-1-(3-methylbenzoyl)piperidine-3-carboxamide
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C20H21ClN2O2
 1
1
IC50 = 35000 nM
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CP0396492
N-(4-chlorophenyl)-1-[3-(1,3-oxazol-5-yl)benzoyl]piperidine-3-carboxamide
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C22H20ClN3O3
 1
1
IC50 = 43000 nM
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CP0374947
N-(4-chlorophenyl)-1-[3-(diethylsulfamoyl)benzoyl]piperidine-3-carboxamide
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C23H28ClN3O4S
 1
1
IC50 = 51000 nM
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CP0374943
1-[3,5-bis(trifluoromethyl)benzoyl]-N-(3-nitrophenyl)piperidine-3-carboxamide
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C21H17F6N3O4
 1
1
IC50 = 66000 nM
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CP0387746
methyl 3-[3-[(4-chlorophenyl)carbamoyl]piperidine-1-carbonyl]benzoate
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C21H21ClN2O4
 1
1
IC50 = 67000 nM
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CP0374948
N-(3-acetylphenyl)-1-[3,5-bis(trifluoromethyl)benzoyl]piperidine-3-carboxamide
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C23H20F6N2O3
 1
1
IC50 = 76000 nM
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CP0396491
N-(4-chlorophenyl)-1-[3-(5-methyl-1,2,4-oxadiazol-3-yl)benzoyl]piperidine-3-carboxamide
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C22H21ClN4O3
 1
1
IC50 = 78000 nM
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Clinical Information about the Protein
Target 1 ( Transforming protein RhoA (RHOA) )
Target Type Discontinued Target
Disease 1 Target-related Disease  1
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Discontinued Drug(s) 1 Discontinued Drug  1
1 ES-285 Discontinued in Phase 1
Solid tumour/cancer
Target 2 ( RhoA messenger RNA (RHOA mRNA) )
Target Type Literature-reported Target