SGC | Annotated Phylogenetic Trees

ASH1L

AS-99
IC50: 790 µM
Pubmed IDs: 33990599

CARM1

compound 9 (ref 1); compound 1b (ref 2) IC50: 100.1 µM Pubmed IDs: 17458842,18348515	compound 10 (ref 1); compound 1c (ref 2) IC50: 40.8 µM Pubmed IDs: 17458842,18348515	compound 4 (ref 1); compound 1a (ref 2) IC50: 52.7 µM Pubmed IDs: 17458842,18348515
compound 8 IC50: 35.7 µM Pubmed IDs: 17458842	patent by Purandare et al. (Bristol-Myers Squibb), Oct. 2006	patent by Wahhab et al. (Methylgene Inc), Sept. 2008
therrien09_2b IC50: 0.06 µM Pubmed IDs: 19836951	therrien09_12 IC50: 0.2 µM Pubmed IDs: 19836951	therrien09_23d IC50: 0.9 µM Pubmed IDs: 19836951
therrien09_23m IC50: 0.32 µM Pubmed IDs: 19836951	wan09_1 IC50: 0.04 µM Pubmed IDs: 19632837	wan09_17b IC50: 0.07 µM Pubmed IDs: 19632837
TBDD IC50: 25 µM Pubmed IDs: 20022955 patent by Kundu et al. Jan. 2008	Bonham10_C4 IC50: 2.7 µM Pubmed IDs: 20345902	pyrazole inhibitor IC50: 0.04 µM Pubmed IDs: 19632837
benzo[d]imidazole related analog_2 IC50: 0.84 µM Pubmed IDs: 19632837	benzo[d]imidazole related analog_5 IC50: 17 µM Pubmed IDs: 19632837	benzo[d]imidazole related analog_8 IC50: 1.2 µM Pubmed IDs: 19632837
benzo[d]imidazole related analog_9 IC50: 2.9 µM Pubmed IDs: 19632837	benzo[d]imidazole related analog_14 IC50: 0.7 µM Pubmed IDs: 19632837	benzo[d]imidazole related analog_17a IC50: 0.41 µM Pubmed IDs: 19632837
benzo[d]imidazole related analog_17b IC50: 0.07 µM Pubmed IDs: 19632837	benzo[d]imidazole related analog_17c IC50: 0.26 µM Pubmed IDs: 19632837	benzo[d]imidazole related analog_17d IC50: 0.12 µM Pubmed IDs: 19632837
benzo[d]imidazole related analog_17e IC50: 4.6 µM Pubmed IDs: 19632837	cheng_cmpd_7g IC50: 8.6 µM Pubmed IDs: 21612300	kung15_cpd27 IC50: 0.03 µM Pubmed IDs: 25746813
MS023 IC50: 0.083 µM Pubmed IDs: 26598975	ferreira16_cmpd7 IC50: 1 µM Pubmed IDs: 26824386	MS049 IC50: 0.034 µM Pubmed IDs: 27584694
TP-064 IC50: 0.01 µM http://www.thesgc.org/chemical-probes/TP-064	EZM2302 IC50: 0.006 µM Pubmed IDs: 29269946,29894694	GSK3368715 IC50: 1.15 µM Pubmed IDs: 31257072
guo19_cmpd49 IC50: 0.021 µM Pubmed IDs: 31117515	SKI-73 IC50: 0.043 µM Pubmed IDs: 31657716

DOT1L

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EPZ004777 IC50: 0.0004 µM Pubmed IDs: 21741596	yao11_cmpd_4 IC50: 0.038 µM Pubmed IDs: 21936531	yao11_cmpd_2 IC50: 1.1 µM Pubmed IDs: 21936531
SGC0946 IC50: 0.0003 µM Pubmed IDs: 23250418	EPZ-5676 IC50: 0.00008 µM Pubmed IDs: 23801631	SYC-522 IC50: 0.0005 µM Pubmed IDs: 25359765
chen16_cmpd12 IC50: 0.0014 µM http://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.6b00167	Massonianoside B IC50: 0.4 µM Pubmed IDs: 30951287

EHMT1/GLP

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BIX-01294 IC50: 0.7 µM Pubmed IDs: 18800048,17289593	Chang10_E67 IC50: 0.273 µM Pubmed IDs: 20434463	Chang10_E70 IC50: 1.3 µM Pubmed IDs: 20434463
Chang10_E72 IC50: 0.1 µM Pubmed IDs: 20434463	UNC0224 IC50: 0.05 µM Pubmed IDs: 19891491	UNC0638 IC50: 0.019 µM Pubmed IDs: 21743462
UNC0642 IC50: 0.0025 µM Pubmed IDs: 24102134	devkota14_4d IC50: 1.5 µM Devkota et al. (2014) ACS Med. Chem. Lett. - DOI: 10.1021/ml4002503	A-366 IC50: 0.038 µM ACS Med. Chem. Lett. (2014), DOI: 10.1021/ml400496h
CM-272 IC50: 0.002 µM Pubmed IDs: 28548080

EHMT2/G9a

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BIX-01294 IC50: 1.9 µM Pubmed IDs: 18800048,17289593	UNC0224 IC50: 0.015 µM Pubmed IDs: 19891491	UNC0638 IC50: 0.015 µM Pubmed IDs: 21743462
BRD9539 IC50: 6.3 µM Pubmed IDs: 22536950	BIX-01338 IC50: 4.7 µM Pubmed IDs: 17289593	UNC0642 IC50: 0.0037 µM Pubmed IDs: 24102134
A-366 IC50: 0.0033 µM ACS Med. Chem. Lett. (2014), DOI: 10.1021/ml400496h	devkota14_4d IC50: 1.6 µM Devkota et al. (2014) ACS Med. Chem. Lett. - DOI: 10.1021/ml4002503	Setin-1 IC50: 26 µM Pubmed IDs: 24650704
DCG066 IC50: 6.5 µM http://www.sciencedirect.com/science/article/pii/S0223523416305062	CM-272 IC50: 0.008 µM Pubmed IDs: 28548080

EZH1

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GSK126 IC50: 0.089 µM Pubmed IDs: 23051747	EPZ005687 IC50: 1 µM Pubmed IDs: 23023262	EI1 IC50: 1.34 µM Pubmed IDs: 23236167
GSK343 IC50: 0.24 µM Pubmed IDs: 24900432 DOI: 10.1021/ml3003346	UNC1999 IC50: 0.045 µM Pubmed IDs: 23614352	EPZ-6438 IC50: 0.4 µM Pubmed IDs: 23620515
garapatyrao13_cmpd3 IC50: 0.21 µM Pubmed IDs: 24183969	kung15_cpd27 IC50: 2.1 µM Pubmed IDs: 25746813	EPZ011989 IC50: 0.045 µM Pubmed IDs: 26005520
CPI-360 IC50: 0.1 µM Pubmed IDs: 25457180	ZLD1039 IC50: 0.081 µM Pubmed IDs: 26868841	CPI-1205 IC50: 0.052 µM Pubmed IDs: 27739677

EZH2

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1346702-70-2 IC50: 0.004 µM WO2011140325	BRD9539 IC50: 10 µM Pubmed IDs: 22536950	copeland12_75 Patent US 20120071418A1
EPZ005687 IC50: 0.054 µM Pubmed IDs: 23023262	GSK126 IC50: 0.0005 µM Pubmed IDs: 23051747	EI1 IC50: 0.0094 µM Pubmed IDs: 23236167
GSK343 IC50: 0.004 µM Pubmed IDs: 24900432 DOI: 10.1021/ml3003346	UNC1999 IC50: 0.0046 µM Pubmed IDs: 23614352	EPZ-6438 IC50: 0.0025 µM Pubmed IDs: 23620515
garapatyrao13_cmpd3 IC50: 0.032 µM Pubmed IDs: 24183969	kung15_cpd27 IC50: 0.27 µM Pubmed IDs: 25746813	EPZ011989 IC50: 0.003 µM http://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.5b00037
gehling15_cmpd22 IC50: 0.002 µM Pubmed IDs: 26189078 http://www.sciencedirect.com/science/article/pii/S0960894X15006496	CPI-360 IC50: 0.002 µM Pubmed IDs: 25457180	ZLD1039 IC50: 0.0056 µM Pubmed IDs: 26868841
CPI-1205 IC50: 0.0022 µM Pubmed IDs: 27739677

MLL

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wang18_cmpd6e
IC50: 3.2 µM
Pubmed IDs: 29889518

NSD1

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BT5
IC50: 5.8 µM
Pubmed IDs: 32868895

NSD2

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LEM-14
IC50: 11.2 µM

WO 2015/152437

BT5
IC50: 26.7 µM
Pubmed IDs: 32868895

NSD3

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BT5
IC50: 14.3 µM
Pubmed IDs: 32868895

PRDM9

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MRK-740
IC50: 0.08 µM
Pubmed IDs: 31848333

PRMT1

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compound 9 (ref 1); compound 1b (ref 2) IC50: 3 µM Pubmed IDs: 17458842,18348515	compound 10 (ref 1); compound 1c (ref 2) IC50: 9.9 µM Pubmed IDs: 17458842,18348515	compound 4 (ref 1); compound 1a (ref 2) IC50: 11.8 µM Pubmed IDs: 17458842,18348515
compound 8 IC50: 3.4 µM Pubmed IDs: 17458842	AMI-1; (1) compound 1; (3) compound 9 IC50: 8.81 µM Pubmed IDs: 17432842,15056663,17323938	AMI-4 IC50: 0.19 µM Pubmed IDs: 15056663
AMI-5 (eosin); compound 6c (ref 2) IC50: 1.41 µM Pubmed IDs: 17458842,17323938,15056663	AMI-6; compound 6f (ref 2) IC50: 5.11 µM Pubmed IDs: 15056663,17323938	AMI-7 IC50: 1.61 µM Pubmed IDs: 15056663
AMI-8 IC50: 1.8 µM Pubmed IDs: 15056663	AMI-9 IC50: 0.28 µM Pubmed IDs: 15056663	allantodapsone (NSC46613, compound 3) IC50: 1.7 µM Pubmed IDs: 17432842
dowden2010_16 IC50: 2.9 µM Pubmed IDs: 20219369	Bonham10_C4 IC50: 4.2 µM Pubmed IDs: 20345902	sinefungin IC50: 1.63 µM Pubmed IDs: 15056663
NS-1 IC50: 12.7 µM Pubmed IDs: 20666457	NS-2 IC50: 43.1 µM Pubmed IDs: 20666457	Bissinger_2e IC50: 1.5 µM Pubmed IDs: 21440447
BIX-01338 IC50: 6 µM Pubmed IDs: 17289593	A36 IC50: 12 µM Pubmed IDs: 22928876	EPZ020411 IC50: 0.119 µM http://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.5b00071
yu15_cmpd6d IC50: 2 µM http://www.sciencedirect.com/science/article/pii/S0960894X15007003	SKLB-639 IC50: 2.4 µM Pubmed IDs: 26377474	MS023 IC50: 0.03 µM Pubmed IDs: 26598975
GSK3368715 IC50: 0.003 µM Pubmed IDs: 31257072

PRMT3

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siarheyeva12_cmp1 IC50: 2.5 µM Pubmed IDs: 22795084	liu13_cmp24 IC50: 0.23 µM Pubmed IDs: 23445220	SGC707 IC50: 0.031 µM Pubmed IDs: 25728001
MS023 IC50: 0.119 µM Pubmed IDs: 26598975	GSK3368715 IC50: 0.048 µM Pubmed IDs: 31257072

PRMT5

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1313207-04-3 WO 2011079236	A9145C IC50: 0.035 µM Pubmed IDs: 23071334	EPZ_WO2014100764 IC50: 0.1 µM WO2014100764
DS-437 IC50: 6 µM http://pubs.acs.org/doi/abs/10.1021/ml500467h	EPZ015666 IC50: 0.022 µM Pubmed IDs: 25915199	GSK591 IC50: 0.011 µM Pubmed IDs: 26985292
LLY-283 IC50: 0.02 µM http://www.thesgc.org/chemical-probes/LLY-283 10.1021/acsmedchemlett.8b00014	mao17_cmpd17 IC50: 0.33 µM Pubmed IDs: 28650658	JNJ-64619178 IC50: 0.00014 µM http://cancerres.aacrjournals.org/content/78/13_Supplement/4859
lin19_cmpd9 IC50: 0.055 µM Pubmed IDs: https://doi.org/10.1021/acsmedchemlett.9b00074

PRMT6

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EPZ020411 IC50: 0.01 µM http://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.5b00071	MS023 IC50: 0.004 µM Pubmed IDs: 26598975	ferreira16_cmpd7 IC50: 0.3 µM Pubmed IDs: 26824386
MS049 IC50: 0.043 µM Pubmed IDs: 27584694	GSK3368715 IC50: 0.006 µM Pubmed IDs: 31257072

PRMT7

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DS-437
IC50: 6 µM

http://pubs.acs.org/doi/abs/10.1021/ml500467h

PRMT8

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EPZ020411 IC50: 0.223 µM http://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.5b00071	MS023 IC50: 0.005 µM Pubmed IDs: 26598975	ferreira16_cmpd7 IC50: 2.1 µM Pubmed IDs: 26824386
GSK3368715 IC50: 0.002 µM Pubmed IDs: 31257072

SETD2

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zheng12_cmp3d
IC50: 0.48 µM
Pubmed IDs: 23043551

EPZ-719
IC50: 0.005 µM
Pubmed IDs: 34671445
https://pubs.acs.org/doi/10.1021/acsmedchemlett.1c00272

SETD7

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compound 10 (ref 1); compound 1c (ref 2) IC50: 19.1 µM Pubmed IDs: 17458842,18348515	compound 9 (ref 1); compound 1b (ref 2) IC50: 34.6 µM Pubmed IDs: 17458842,18348515	compound 4 (ref 1); compound 1a (ref 2) IC50: 63.6 µM Pubmed IDs: 17458842,18348515
compound 8 IC50: 37.1 µM Pubmed IDs: 17458842	cyproheptadine IC50: 20 µM Norikazu et al. (2012) Kyushu Institute of Technology. Patent JP 2011-224604 20111012. Priority: JP 2010-230916 20101013. AN 2012:768019	CCT021895 IC50: 20 µM Pubmed IDs: 22772057
Setin-1 IC50: 22 µM Pubmed IDs: 24650704	PFI-2 IC50: 0.018 µM Pubmed IDs: 25136132 http://www.thesgc.org/chemical-probes/PFI-2	DC-S239 IC50: 4.59 µM Pubmed IDs: 26390175
hirano18_cmpd2n IC50: 0.41 µM Pubmed IDs: 29882380

SETD8

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EBI-099 IC50: 4.7 µM Kodoma et al. WO 2011010715	EBI-435 Kodoma et al. WO 2011010715	EBI-455 Kodoma et al. WO 2011010715
UNC0379 IC50: 7.3 µM Pubmed IDs: 25032507	SPS8I1 IC50: 0.2 µM Pubmed IDs: 25137013	SPS8I2-Ryuvidine IC50: 0.7 µM Pubmed IDs: 25137013

SMYD2

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AZ505 IC50: 0.12 µM Pubmed IDs: 21782458	LLY-507 IC50: 0.015 µM Pubmed IDs: 25825497 http://www.thesgc.org/chemical-probes/LLY-507	SPS8I1 IC50: 0.5 µM Pubmed IDs: 25137013
A-893 IC50: 0.0028 µM Pubmed IDs: 26101576 http://pubs.acs.org/doi/abs/10.1021/acsmedchemlett.5b00124	BAY-598 IC50: 0.005 µM Pubmed IDs: 27075367	cowen16_cmpd40 IC50: 0.138 µM Pubmed IDs: 28002961
cowen16_cmpd47 IC50: 0.017 µM Pubmed IDs: 28002961

SMYD3

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EPZ030456 IC50: 0.048 µM DOI: 10.1021/acsmedchemlett.5b00272	EPZ031686 IC50: 0.036 µM DOI: 10.1021/acsmedchemlett.5b00272	GSK2807 IC50: 0.13 µM Pubmed IDs: 27066749
huang19_cmpd29 IC50: 0.012 µM Pubmed IDs: 31223458

SUV39H1

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BIX-01338
IC50: 1.1 µM
Pubmed IDs: 17289593

SUV420H1

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A-196
IC50: 0.025 µM
Pubmed IDs: 28114273

dai17_cmpd204
IC50: 0.053 µM

Patent US20170174688

SUV420H2

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A-196
IC50: 0.144 µM
Pubmed IDs: 28114273