General Information of the Protein
Protein ID
PT06122
Protein Name
Retinoblastoma-associated protein
Secondarily
Protein Name
p105-Rb
p110-RB1
pRb
pp110
Gene Name
RB1
Sequence
MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTALCQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIAAVDLDEMSFTFTELQKNIEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSSISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYKTAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFMNSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDARLFLDHDKTLQTDSIDSFETQRTPRKSNLDEEVNVIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVKDIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDNIFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEGNLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNHTAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYLRLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLKFKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLSPIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFGTSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQKLAEMTSTRTRMQKQKMNDSMDTSNKEEK
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Unclassified protein
Function
Tumor suppressor that is a key regulator of the G1/S transition of the cell cycle (PubMed:10499802). The hypophosphorylated form binds transcription regulators of the E2F family, preventing transcription of E2F-responsive genes (PubMed:10499802). Both physically blocks E2Fs transactivating domain and recruits chromatin-modifying enzymes that actively repress transcription (PubMed:10499802). Cyclin and CDK-dependent phosphorylation of RB1 induces its dissociation from E2Fs, thereby activating transcription of E2F responsive genes and triggering entry into S phase (PubMed:10499802). RB1 also promotes the G0-G1 transition upon phosphorylation and activation by CDK3/cyclin-C (PubMed:15084261). Directly involved in heterochromatin formation by maintaining overall chromatin structure and, in particular, that of constitutive heterochromatin by stabilizing histone methylation. Recruits and targets histone methyltransferases SUV39H1, KMT5B and KMT5C, leading to epigenetic transcriptional repression. Controls histone H4 'Lys-20' trimethylation. Inhibits the intrinsic kinase activity of TAF1. Mediates transcriptional repression by SMARCA4/BRG1 by recruiting a histone deacetylase (HDAC) complex to the c-FOS promoter. In resting neurons, transcription of the c-FOS promoter is inhibited by BRG1-dependent recruitment of a phospho-RB1-HDAC1 repressor complex. Upon calcium influx, RB1 is dephosphorylated by calcineurin, which leads to release of the repressor complex (By similarity).
    Show/Hide
Uniprot ID
Primary ID:
P06400

Secondarily ID:
A8K5E3
P78499
Q5VW46
Q8IZL4
    Show/Hide
Ensembl ID
ENSG00000139687
HGNC ID
HGNC:9884
Subcellular Location
Nucleus
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: CL000111 , MDA-MB-231
Compound ID Compound Name Compound Formula
CP0004106
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
   Show/Hide
C28H26N4O3
 1
1
IC50 = 66 nM
   TI
   LI
   LO
   TS
CP0537202
6-methyl-N-(3-methylcyclopentyl)-2,3,4,9-tetrahydro-1H-carbazol-2-amine
   Show/Hide
C19H26N2
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0565954
N-benzyl-6-methyl-2,3,4,9-tetrahydro-1H-carbazol-2-amine;hydrochloride
   Show/Hide
C20H23ClN2
 1
1
IC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0560340
6-methyl-N-[(4-methylphenyl)methyl]-2,3,4,9-tetrahydro-1H-carbazol-2-amine;hydrochloride
   Show/Hide
C21H25ClN2
 1
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
CP0547874
9-methyl-N-[(4-methylphenyl)methyl]-1,2,3,4-tetrahydrocarbazol-2-amine
   Show/Hide
C21H24N2
 1
1
IC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0946127
6-methyl-N-(3-methylcyclopentyl)-2,3,4,9-tetrahydro-1H-carbazol-2-amine hydrochloride
   Show/Hide
C19H27ClN2
 1
1
IC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0446917
N-[(4-methylphenyl)methyl]-2,3,4,9-tetrahydro-1H-carbazol-2-amine
   Show/Hide
C20H22N2
 1
1
IC50 = 4100 nM
   TI
   LI
   LO
   TS
CP0546788
N-(3-methylcyclopentyl)-6-nitro-2,3,4,9-tetrahydro-1H-carbazol-1-amine
   Show/Hide
C18H23N3O2
 1
1
IC50 = 4810 nM
   TI
   LI
   LO
   TS
CP0561534
N-benzyl-2,3,4,9-tetrahydro-1H-carbazol-2-amine
   Show/Hide
C19H20N2
 1
1
IC50 = 6920 nM
   TI
   LI
   LO
   TS
CP0560338
N-(3-methylcyclopentyl)-2,3,4,9-tetrahydro-1H-carbazol-1-amine
   Show/Hide
C18H24N2
 1
1
IC50 = 9000 nM
   TI
   LI
   LO
   TS
CP0565950
4-fluoro-N-(2,3,4,9-tetrahydro-1H-carbazol-1-yl)benzenesulfonamide
   Show/Hide
C18H17FN2O2S
 1
1
IC50 = 9200 nM
   TI
   LI
   LO
   TS
CP0546786
4-fluoro-N-(2,3,4,9-tetrahydro-1H-carbazol-2-yl)benzenesulfonamide
   Show/Hide
C18H17FN2O2S
 1
1
IC50 = 9500 nM
   TI
   LI
   LO
   TS
CP0560339
N-cyclopentyl-2,3,4,9-tetrahydro-1H-carbazol-2-amine
   Show/Hide
C17H22N2
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0565948
N-cyclopentyl-2,3,4,9-tetrahydro-1H-carbazol-1-amine
   Show/Hide
C17H22N2
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0432817
N-cyclohexyl-2,3,4,9-tetrahydro-1H-carbazol-2-amine
   Show/Hide
C18H24N2
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0546784
N-cyclohexyl-2,3,4,9-tetrahydro-1H-carbazol-1-amine;hydrochloride
   Show/Hide
C18H25ClN2
 1
1
IC50 = 15000 nM
   TI
   LI
   LO
   TS
CP0963229
N-(3-methylcyclopentyl)-2,3,4,9-tetrahydro-1H-carbazol-1-amine hydrochloride
   Show/Hide
C18H25ClN2
 1
1
IC50 = 15000 nM
   TI
   LI
   LO
   TS
CP0921983
N-cyclopentyl-2,3,4,9-tetrahydro-1H-carbazol-1-amine hydrochloride
   Show/Hide
C17H23ClN2
 1
1
IC50 = 16000 nM
   TI
   LI
   LO
   TS
CP0558653
N-(3-methylcyclopentyl)-2,3,4,9-tetrahydro-1H-carbazol-2-amine;hydrochloride
   Show/Hide
C18H25ClN2
 1
1
IC50 = 17300 nM
   TI
   LI
   LO
   TS
CP0537201
N-(2,3,4,9-tetrahydro-1H-carbazol-2-yl)pyridine-3-sulfonamide
   Show/Hide
C17H17N3O2S
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0546785
N-(oxan-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-2-amine;hydrochloride
   Show/Hide
C17H23ClN2O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0546787
2-fluoro-N-(2,3,4,9-tetrahydro-1H-carbazol-2-yl)benzamide
   Show/Hide
C19H17FN2O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0558652
4-cyano-N-(2,3,4,9-tetrahydro-1H-carbazol-1-yl)benzenesulfonamide
   Show/Hide
C19H17N3O2S
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0558654
4-cyano-N-(2,3,4,9-tetrahydro-1H-carbazol-2-yl)benzenesulfonamide
   Show/Hide
C19H17N3O2S
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0558655
3-fluoro-N-(2,3,4,9-tetrahydro-1H-carbazol-2-yl)benzamide
   Show/Hide
C19H17FN2O
 1
1
IC50 = 100000 nM
   TI
   LI
   LO
   TS
CP0565949
N-(2,3,4,9-tetrahydro-1H-carbazol-1-yl)pyridine-3-sulfonamide
   Show/Hide
C17H17N3O2S
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0565952
3-methoxy-N-(2,3,4,9-tetrahydro-1H-carbazol-2-yl)benzamide
   Show/Hide
C20H20N2O2
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS