General Information of the Protein
Protein ID
PT05113
Protein Name
Histone-arginine methyltransferase CARM1
Secondarily
Protein Name
Coactivator-associated arginine methyltransferase 1
Protein arginine N-methyltransferase 4
Gene Name
CARM1
Secondarily
Gene Name
Prmt4
Sequence
MAAAAATAVGPGAGSAGVAGPGGAGPCATVSVFPGARLLTIGDANGEIQRHAEQQALRLEVRAGPDAAGIALYSHEDVCVFKCSVSRETECSRVGRQSFIITLGCNSVLIQFATPHDFCSFYNILKTCRGHTLERSVFSERTEESSAVQYFQFYGYLSQQQNMMQDYVRTGTYQRAILQNHTDFKDKIVLDVGCGSGILSFFAAQAGARKIYAVEASTMAQHAEVLVKSNNLTDRIVVIPGKVEEVSLPEQVDIIISEPMGYMLFNERMLESYLHAKKYLKPSGNMFPTIGDVHLAPFTDEQLYMEQFTKANFWYQPSFHGVDLSALRGAAVDEYFRQPVVDTFDIRILMAKSVKYTVNFLEAKEGDLHRIEIPFKFHMLHSGLVHGLAFWFDVAFIGSIMTVWLSTAPTEPLTHWYQVRCLFQSPLFAKAGDTLSGTCLLIANKRQSYDISIVAQVDQTGSKSSNLLDLKNPFFRYTGTTPSPPPGSHYTSPSENMWNTGSTYNLSSGVAVAGMPTAYDLSSVIAGGSSVGHNNLIPLANTGIVNHTHSRMGSIMSTGIVQGSSGAQGGGGSSSAHYAVNNQFTMGGPAISMASPMSIPTNTMHYGS
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Organism
Mus musculus, Mouse
Protein Classification
Epigenetic regulator
>
Writer
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Protein methyltransferase
>
Protein arginine methyltransferase
Function
Methylates (mono- and asymmetric dimethylation) the guanidino nitrogens of arginyl residues in several proteins involved in DNA packaging, transcription regulation, pre-mRNA splicing, and mRNA stability (PubMed:10381882, PubMed:21138967, PubMed:11341840, PubMed:11997499, PubMed:19897492, PubMed:14966289, PubMed:17218272). Recruited to promoters upon gene activation together with histone acetyltransferases from EP300/P300 and p160 families, methylates histone H3 at 'Arg-17' (H3R17me), forming mainly asymmetric dimethylarginine (H3R17me2a), leading to activates transcription via chromatin remodeling (PubMed:10381882, PubMed:11747826, PubMed:12498683, PubMed:11751582, PubMed:11341840, PubMed:11997499, PubMed:15339660, PubMed:15616592). During nuclear hormone receptor activation and TCF7L2/TCF4 activation, acts synergically with EP300/P300 and either one of the p160 histone acetyltransferases NCOA1/SRC1, NCOA2/GRIP1 and NCOA3/ACTR or CTNNB1/beta-catenin to activate transcription (PubMed:11997499, PubMed:16322096, PubMed:17882261, PubMed:19843527). During myogenic transcriptional activation, acts together with NCOA3/ACTR as a coactivator for MEF2C (PubMed:11713257). During monocyte inflammatory stimulation, acts together with EP300/P300 as a coactivator for NF-kappa-B (PubMed:11983685). Acts as a coactivator for PPARG, promotes adipocyte differentiation and the accumulation of brown fat tissue (PubMed:18188184). Plays a role in the regulation of pre-mRNA alternative splicing by methylation of splicing factors (PubMed:21138967). Also seems to be involved in p53/TP53 transcriptional activation (PubMed:15186775). Methylates EP300/P300, both at 'Arg-2142', which may loosen its interaction with NCOA2/GRIP1, and at 'Arg-580' and 'Arg-604' in the KIX domain, which impairs its interaction with CREB and inhibits CREB-dependent transcriptional activation (PubMed:11701890). Also methylates arginine residues in RNA-binding proteins PABPC1, ELAVL1 and ELAV4, which may affect their mRNA-stabilizing properties and the half-life of their target mRNAs (PubMed:11850402, PubMed:12756295, PubMed:12237300). Acts as a transcriptional coactivator of ACACA/acetyl-CoA carboxylase by enriching H3R17 methylation at its promoter, thereby positively regulating fatty acid synthesis (PubMed:30366907). Independently of its methyltransferase activity, involved in replication fork progression: promotes PARP1 recruitment to replication forks, leading to poly-ADP-ribosylation of chromatin at replication forks and reduced fork speed (By similarity).
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Uniprot ID
Primary ID:
Q9WVG6

Secondarily ID:
Q3TYB9
Q8K1Y5
Q91W24
Q99KX8
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Ensembl ID
ENSG00000142453
Subcellular Location
Nucleus
Cytoplasm
Chromosome
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: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0238111
1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-3-yl)-N-[(2-methoxyphenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C21H22F3N5O3S
 1
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
CP0417920
1-(3-{[(2S)-2-aminopropanamido]methyl}phenyl)-N-[(2-methoxyphenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C23H24F3N5O3
 1
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
CP0538577
N-[(2-methoxyphenyl)methyl]-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C23H26F3N5O2
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0453810
1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-3-yl)-N-benzyl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C20H20F3N5O2S
 1
1
IC50 = 220 nM
   TI
   LI
   LO
   TS
CP0467352
1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-2-yl)-N-benzyl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C20H20F3N5O2S
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0423665
1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-3-yl)-N-[(2-methylphenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C21H22F3N5O2S
 1
1
IC50 = 260 nM
   TI
   LI
   LO
   TS
CP0467351
1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-2-yl)-N-[(2-methoxyphenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C21H22F3N5O3S
 1
1
IC50 = 300 nM
   TI
   LI
   LO
   TS
CP0479925
1-(3-((2-(methylamino)ethylamino)methyl)phenyl)-N-(naphthalen-1-ylmethyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C26H26F3N5O
 1
1
IC50 = 320 nM
   TI
   LI
   LO
   TS
CP0423666
1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-3-yl)-N-[(3-methoxyphenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C21H22F3N5O3S
 1
1
IC50 = 370 nM
   TI
   LI
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   TS
CP0400377
N-(2,3-dihydro-1,4-benzodioxin-5-ylmethyl)-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C24H26F3N5O3
 1
1
IC50 = 710 nM
   TI
   LI
   LO
   TS
CP0535291
N-[(5-fluoro-2-methoxyphenyl)methyl]-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C23H25F4N5O2
 1
1
IC50 = 710 nM
   TI
   LI
   LO
   TS
CP0453811
methyl 2-({[1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-3-yl)-3-(trifluoromethyl)-1H-pyrazol-5-yl]formamido}methyl)benzoate
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C22H22F3N5O4S
 1
1
IC50 = 770 nM
   TI
   LI
   LO
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CP0462670
1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-3-yl)-N-[(2-fluorophenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C20H19F4N5O2S
 1
1
IC50 = 790 nM
   TI
   LI
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CP0504601
N-[(2-ethoxyphenyl)methyl]-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C24H28F3N5O2
 1
1
IC50 = 900 nM
   TI
   LI
   LO
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CP0373511
1-(3-((2-aminoethylamino)methyl)phenyl)-N-(2-methoxybenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C22H24F3N5O2
 1
1
IC50 = 1000 nM
   TI
   LI
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CP0527167
N-[(2-ethylphenyl)methyl]-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C24H28F3N5O
 1
1
IC50 = 1610 nM
   TI
   LI
   LO
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CP0463717
N-[2-(1H-indol-3-yl)ethyl]-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C25H27F3N6O
 1
1
IC50 = 1800 nM
   TI
   LI
   LO
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CP0502096
1-(4-{[(2S)-2-aminopropanamido]methyl}-1,3-thiazol-2-yl)-N-[(2-methoxyphenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C20H21F3N6O3S
 1
1
IC50 = 2200 nM
   TI
   LI
   LO
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CP0372953
1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-2-yl)-N-[(2-fluorophenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C20H19F4N5O2S
 1
1
IC50 = 2310 nM
   TI
   LI
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CP0547533
1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-2-yl)-N-{[2-(propan-2-yloxy)phenyl]methyl}-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C23H26F3N5O3S
 1
1
IC50 = 2920 nM
   TI
   LI
   LO
   TS
CP0502097
1-(6-{[(2S)-2-aminopropanamido]methyl}pyridin-2-yl)-N-[(2-methoxyphenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C22H23F3N6O3
 1
1
IC50 = 3050 nM
   TI
   LI
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   TS
CP0896438
(S)-1-(5-((2-aminopropanamido)methyl)thiophen-2-yl)-N-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C19H19F3N6O2S
 1
1
IC50 = 3350 nM
   TI
   LI
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   TS
CP0463718
N-[(2-methoxynaphthalen-1-yl)methyl]-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C27H28F3N5O2
 1
1
IC50 = 3350 nM
   TI
   LI
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CP0536411
N-(cyclohexylmethyl)-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C22H30F3N5O
 1
1
IC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0372892
1-(4-{[(2S)-2-aminopropanamido]methyl}pyridin-2-yl)-N-[(2-methoxyphenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C22H23F3N6O3
 1
1
IC50 = 4200 nM
   TI
   LI
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CP0535292
N-(1H-benzimidazol-2-ylmethyl)-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C23H24F3N7O
 1
1
IC50 = 4300 nM
   TI
   LI
   LO
   TS
CP0502098
1-(5-{[(2S)-2-aminopropanamido]methyl}thiophen-2-yl)-3-(trifluoromethyl)-N-{[2-(trifluoromethyl)phenyl]methyl}-1H-pyrazole-5-carboxamide
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C21H19F6N5O2S
 1
1
IC50 = 4480 nM
   TI
   LI
   LO
   TS
CP0526348
(S)-1-(3-((2-aminopropanethioamido)methyl)phenyl)-N-(2-methoxybenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C23H24F3N5O2S
 1
1
IC50 = 4500 nM
   TI
   LI
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CP0526349
2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-N-[(1-methylbenzimidazol-2-yl)methyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C24H26F3N7O
 1
1
IC50 = 4700 nM
   TI
   LI
   LO
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CP0463719
1-(4-fluoro-3-((2-(methylamino)ethylamino)methyl)phenyl)-N-(2-methoxybenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C23H25F4N5O2
 1
1
IC50 = 5600 nM
   TI
   LI
   LO
   TS
CP0496143
1-(3-((2-(methylamino)ethylamino)methyl)phenyl)-N-(2-(trifluoromethoxy)benzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C23H23F6N5O2
 1
1
IC50 = 6500 nM
   TI
   LI
   LO
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CP0415272
1-(3-((2-(ethylamino)ethylamino)methyl)phenyl)-N-(2-methoxybenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C24H28F3N5O2
 1
1
IC50 = 7700 nM
   TI
   LI
   LO
   TS
CP0485284
1-(3-((2-(dimethylamino)ethylamino)methyl)phenyl)-N-(2-methoxybenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C24H28F3N5O2
 1
1
IC50 = 7900 nM
   TI
   LI
   LO
   TS
CP0447507
N-[(2-methoxyphenyl)methyl]-2-[4-methyl-3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C24H28F3N5O2
 1
1
IC50 = 7940 nM
   TI
   LI
   LO
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CP0462669
1-(2-{[(2S)-2-aminopropanamido]methyl}-1-benzofuran-7-yl)-N-[(2-methoxyphenyl)methyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C25H24F3N5O4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
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CP0899698
1-(2-(((S)-2-aminopropanamido)methyl)isoindolin-4-yl)-N-(2-methoxybenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C25H27F3N6O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
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CP0485293
5-(2-methoxybenzyl)-8-((2-(methylamino)ethylamino)methyl)-2-(trifluoromethyl)pyrazolo[1,5-a]quinoxalin-4(5H)-one
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C23H24F3N5O2
 1
1
IC50 > 10000 nM
   TI
   LI
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CP0506470
N-benzyl-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C22H24F3N5O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
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CP0527168
N-[(2-aminophenyl)methyl]-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C22H25F3N6O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0536410
1-(3-((2-(methylamino)ethylamino)methyl)phenyl)-N-(2-methylbenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C23H26F3N5O
 1
1
IC50 = 13100 nM
   TI
   LI
   LO
   TS
CP0383682
(S)-1-(3-((2-hydroxypropanamido)methyl)phenyl)-N-(2-methoxybenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C23H23F3N4O4
 1
1
IC50 > 20000 nM
   TI
   LI
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CP0383685
N-[(2-methoxyphenyl)methyl]-2-[3-[2-(methylamino)ethylcarbamoyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C23H24F3N5O3
 1
1
IC50 > 20000 nM
   TI
   LI
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   TS
CP0463716
(S)-1-(3-(2-(2-aminopropanamido)ethyl)phenyl)-N-(2-methoxybenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C24H26F3N5O3
 1
1
IC50 > 20000 nM
   TI
   LI
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CP0479923
(S)-1-(3-(5-(1-aminoethyl)-1H-1,2,4-triazol-3-yl)phenyl)-N-(2-methoxybenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C23H22F3N7O2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
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CP0479926
N-[(2-methoxyphenyl)methyl]-2-[3-[[2-(methylamino)ethylamino]methyl]-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C24H25F6N5O2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
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CP0490953
N-[(2-methoxyphenyl)methyl]-2-[3-[(pyrrolidin-3-ylamino)methyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C24H26F3N5O2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0501460
(S)-1-(3-(5-(1-aminoethyl)-1,2,4-oxadiazol-3-yl)phenyl)-N-(2-methoxybenzyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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C23H21F3N6O3
 1
1
IC50 > 20000 nM
   TI
   LI
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CP0479924
N-[(2-methoxyphenyl)methyl]-2-[3-[1-[2-(methylamino)ethylamino]ethyl]phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide
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C24H28F3N5O2
 1
1
IC50 = 21000 nM
   TI
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Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02533 Histone-arginine methyltransferase CARM1 Homo sapiens, Human