BAY-277 [Ligand Id: 13974] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL5465171 (BAY_277, BAY-277)
  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
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  • Methionyl aminopeptidase 2/Methionine aminopeptidase 2 in Human [ChEMBL: CHEMBL3922] [GtoPdb: 1573] [UniProtKB: P50579]
  • Methionyl aminopeptidase 2/Methionine aminopeptidase 2 in Mouse [ChEMBL: CHEMBL1075272] [GtoPdb: 1573] [UniProtKB: O08663]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • DAT/Sodium-dependent dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL GPCRScan assay: inhibition of H3 B 7.14 pKi 72.84 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of H3 B 7.14 pKi 72.84 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of H3 B 7.15 pKi 70.79 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of H3 B 7.15 pKi 70.79 nM Ki Data for DCP probe BAY-277
Methionyl aminopeptidase 2/Methionine aminopeptidase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3922] [GtoPdb: 1573] [UniProtKB: P50579]
ChEMBL 2D HUVEC cells proliferation assay F 7.92 pIC50 12 nM IC50 Data for DCP probe BAY-277
ChEMBL METAP2 biochemical assay (human) B 8.24 pIC50 5.8 nM IC50 Data for DCP probe BAY-277
GtoPdb - - 8.24 pIC50 5.8 nM IC50 Overview for BAY-277 a degrader of METAP2. thesgc.org
Methionyl aminopeptidase 2/Methionine aminopeptidase 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075272] [GtoPdb: 1573] [UniProtKB: O08663]
ChEMBL METAP2 biochemical assay (mouse) B 8.23 pIC50 5.9 nM IC50 Data for DCP probe BAY-277
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL GPCRScan assay: inhibition of M1 B 5.78 pKi 1670.44 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M1 B 5.78 pKi 1670.44 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M1 B 5.78 pKi 1659.59 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M1 B 5.78 pKi 1659.59 nM Ki Data for DCP probe BAY-277
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL GPCRScan assay: inhibition of M2 B 6.17 pKi 676.76 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M2 B 6.17 pKi 676.76 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M2 B 6.17 pKi 676.08 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M2 B 6.17 pKi 676.08 nM Ki Data for DCP probe BAY-277
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL GPCRScan assay: inhibition of M3 B 5.65 pKi 2262.9 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M3 B 5.65 pKi 2262.9 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M3 B 5.68 pKi 2089.3 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M3 B 5.68 pKi 2089.3 nM Ki Data for DCP probe BAY-277
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL GPCRScan assay: inhibition of M4 B 6.2 pKi 631.53 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M4 B 6.2 pKi 631.53 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M4 B 6.21 pKi 616.6 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M4 B 6.21 pKi 616.6 nM Ki Data for DCP probe BAY-277
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL GPCRScan assay: inhibition of M5 B 6.25 pKi 567.76 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M5 B 6.25 pKi 567.76 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M5 B 6.25 pKi 562.34 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of M5 B 6.25 pKi 562.34 nM Ki Data for DCP probe BAY-277
σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2]
ChEMBL GPCRScan assay: inhibition of Sigma 2 B 6.06 pKi 866.55 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of Sigma 2 B 6.06 pKi 866.55 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of Sigma 2 B 6.08 pKi 831.76 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of Sigma 2 B 6.08 pKi 831.76 nM Ki Data for DCP probe BAY-277
DAT/Sodium-dependent dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL GPCRScan assay: inhibition of DAT B 5.43 pKi 3731.65 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of DAT B 5.43 pKi 3731.65 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of DAT B 5.47 pKi 3388.44 nM Ki Data for DCP probe BAY-277
ChEMBL GPCRScan assay: inhibition of DAT B 5.47 pKi 3388.44 nM Ki Data for DCP probe BAY-277

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]