ChEMBL ligand: CHEMBL5075067
methyltransferase 3, N6-adenosine-methyltransferase complex catalytic subunit/METTL3/METTL14 in Human [ChEMBL: CHEMBL4106140] [GtoPdb: 3181] [UniProtKB: Q86U44, Q9HCE5] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
methyltransferase 3, N6-adenosine-methyltransferase complex catalytic subunit/METTL3/METTL14 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106140] [GtoPdb: 3181] [UniProtKB: Q86U44, Q9HCE5]
ChEMBL	Inhibition of METTL3/METTL14-mediated m6A mRNA expression in human FaDu cells incubated for 24 hrs by LC-MS/MS analysis	B	6.48	pIC50	331	nM	IC50	J Med Chem (2025) 68: 2981-3003 [PMID:39883878]
ChEMBL	Inhibition of METTL3/METTL14-mediated m6A mRNA expression in human A549 cells incubated for 24 hrs by LC-MS/MS analysis	B	6.58	pIC50	264	nM	IC50	J Med Chem (2025) 68: 2981-3003 [PMID:39883878]
ChEMBL	Inhibition of METTL3/METTL14-mediated m6A mRNA expression in human MV4-11 cells incubated for 24 hrs by LC-MS/MS analysis	B	6.74	pIC50	182	nM	IC50	J Med Chem (2025) 68: 2981-3003 [PMID:39883878]
ChEMBL	Inhibition of METTL3/METTL14-mediated m6A mRNA expression in human Calu-6 cells incubated for 24 hrs by LC-MS/MS analysis	B	6.77	pIC50	169	nM	IC50	J Med Chem (2025) 68: 2981-3003 [PMID:39883878]
ChEMBL	Inhibition of METTL3/METTL14-mediated m6A mRNA expression in human Kasumi 1 cells incubated for 24 hrs by LC-MS/MS analysis	B	6.86	pIC50	138	nM	IC50	J Med Chem (2025) 68: 2981-3003 [PMID:39883878]
ChEMBL	Inhibition of METTL3/METTL14-mediated m6A mRNA expression in human SK-OV-3 cells incubated for 24 hrs by LC-MS/MS analysis	B	6.87	pIC50	134	nM	IC50	J Med Chem (2025) 68: 2981-3003 [PMID:39883878]
GtoPdb	-	-	8.21	pIC50	6.1	nM	IC50	WO2021111124A1. Polyheterocyclic compounds as mettl3 inhibitors (2021)
ChEMBL	Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5'P-uacacucgaucuggacuaaagcugcuc-3' and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis	B	8.21	pIC50	6.1	nM	IC50	J Med Chem (2023) 66: 1654-1677 [PMID:36692498]
ChEMBL	Inhibition of full-length His-tagged METTL3 (unknown origin) coexpressed with full-length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using 5'P-uacacucgaucuggacuaaagcugcuc-3' RNA as substrate pre-incubated for 10 mins and followed by substrate addition and measured after 60 mins by methyltransferase assay	B	8.21	pIC50	6.1	nM	IC50	WO-2021111124-A1. Polyheterocyclic compounds as mettl3 inhibitors (2021)
ChEMBL	Displacement of [3H]-SAM from METTL3/METTL14 (unknown origin) using 5'biotinylated-UACACUCGAUCUGGACUAAAGGUGCUC-3' RNA as substrate preincubated for 10 mins followed by substrate/[3H]-SAM addition measured after 90 mins by SPA	B	8.4	pIC50	4	nM	IC50	J Med Chem (2025) 68: 2981-3003 [PMID:39883878]

ChEMBL data shown on this page come from version 37:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]