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Target
Sequence
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Ki
IC50
Kd
EC50
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ΔG°
ΔH°
-TΔS°
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IC50
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rcsb
for Protein arginine N-methyltransferase 5
4GQB
: crystal structure of the human prmt5:mep50 complex (
10.1073/PNAS.1209814109
)
4X60
: crystal structure of prmt5:mep50 with epz015666 and sinefungin (
10.1038/NCHEMBIO.1810
)
4X61
: crystal structure of prmt5:mep50 with epz015666 and sam (
10.1038/NCHEMBIO.1810
)
4X63
: crystal structure of prmt5:mep50 with epz015666 and sah (
10.1038/NCHEMBIO.1810
)
5C9Z
: crystal structure of prmt5:mep50 with epz015866 and sinefungin
5EMJ
: crystal structure of prmt5:mep50 with compound 8 and sinefungin (
10.1021/ACSMEDCHEMLETT.5B00380
)
5EMK
: crystal structure of prmt5:mep50 with compound 9 and sinefungin (
10.1021/ACSMEDCHEMLETT.5B00380
)
5EML
: crystal structure of prmt5:mep50 with compound 10 and sam (
10.1021/ACSMEDCHEMLETT.5B00380
)
5EMM
: crystal structure of prmt5:mep50 with compound 15 and sinefungin (
10.1021/ACSMEDCHEMLETT.5B00380
)
5FA5
: crystal structure of prmt5:mep50 in complex with mta and h4 peptide (
10.1126/SCIENCE.AAD5944
)
6CKC
: structure of prmt5:mep50 in complex with lly-283, a potent and selective inhibitor of prmt5, with antitumor activity (
10.1021/ACSMEDCHEMLETT.8B00014
)
6K1S
: discovery of potent and selective covalent protein arginine methyltransferase (prmt5) inhibitors (
10.1021/ACSMEDCHEMLETT.9B00074
)
6RLL
: crystal structure of the human prmt5:mep50 complex with jnj44064146
6RLQ
: crystal structure of the human prmt5:mep50 complex with jnj45031882
6UGH
: cryo-em structure of the apo form of human prmt5:mep50 complex at a resolution of 3.4 angstrom
6UXX
: prmt5:mep50 complexed with allosteric inhibitor compound 1a (
10.1021/ACSMEDCHEMLETT.9B00525
)
6UXY
: prmt5:mep50 complexed with allosteric inhibitor compound 8 (
10.1021/ACSMEDCHEMLETT.9B00525
)
6V0N
: prmt5 bound to pbm peptide from riok1 (
10.1101/2020.08.22.256347.
)
6V0O
: prmt5 bound to the pbm peptide from picln (
10.1101/2020.08.22.256347.
)
6V0P
: prmt5 complex bound to covalent pbm inhibitor brd6711
7BOC
: crystal structure of the prmt5 tim barrel domain in complex with riok1 peptide (
10.1002/CBIC.202100079
)
7KIB
: prmt5:mep50 complexed with 5,5-bicyclic inhibitor compound 4 (
10.1021/ACS.JMEDCHEM.0C02083
)
7KIC
: prmt5:mep50 complexed with 5,5-bicyclic inhibitor compound 34 (
10.1021/ACS.JMEDCHEM.0C02083
)
7KID
: prmt5:mep50 complexed with 5,5-bicyclic inhibitor compound 72 (
10.1021/ACS.JMEDCHEM.0C02083
)
7L1G
: prmt5-mep50 complexed with sam (
10.1021/ACS.JOC.0C02969
)
7M05
: cryoem structure of prmt5 bound to covalent pbm-site inhibitor brd- 6988 (
10.1101/2021.02.03.429644
)
7MX7
: prmt5:mep50 complexed with inhibitor pf-06939999 (
10.1158/1535-7163.MCT-21-0620
)
7MXA
: prmt5:mep50 complexed with inhibitor pf-06855800 (
10.1158/1535-7163.MCT-21-0620
)
7MXC
: prmt5:mep50 complexed with adenosine (
10.1158/1535-7163.MCT-21-0620
)
7MXG
: prmt5(m420t mutant):mep50 complexed with inhibitor pf-06855800 (
10.1158/1535-7163.MCT-21-0620
)
7MXN
: prmt5(m420t mutant):mep50 complexed with inhibitor pf-06939999 (
10.1158/1535-7163.MCT-21-0620
)