BAY1214784 [Ligand Id: 12784] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4537788 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Inhibition of Cannabinoid CB1 at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_217030) | B | 5.59 | pKi | 2570 | nM | Ki | Data for DCP probe BAY-784 |
| ChEMBL | Inhibition of Cannabinoid CB1 at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_217030) | B | 5.46 | pIC50 | 3440 | nM | IC50 | Data for DCP probe BAY-784 |
| ChEMBL | Selectivity interaction (Leadprofiling screen (Ricerca, enzymes, receptors, transporters, and ion channels )) EUB0000347a CNR1 | B | 5.46 | pIC50 | 3440 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of CB1 receptor (unknown origin) | B | 5.47 | pIC50 | 3400 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968] | ||||||||
| ChEMBL | Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay | B | 8.01 | pKd | 9.83 | nM | Kd | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| ChEMBL | Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay | B | 8.26 | pKd | 5.52 | nM | Kd | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| ChEMBL | Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| ChEMBL | Binding assay (Tag Lite) | B | 7.57 | pIC50 | 27 | nM | IC50 | Data for DCP probe BAY-784 |
| ChEMBL | Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR | B | 7.57 | pIC50 | 27 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| ChEMBL | Mechanistic assay measuring cellular IP1 | F | 7.68 | pIC50 | 21 | nM | IC50 | Data for DCP probe BAY-784 |
| ChEMBL | Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR | B | 7.68 | pIC50 | 21 | nM | IC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| GtoPdb | Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay | - | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969] | ||||||||
| ChEMBL | Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG expressed in HEK293 cells assessed as reduction in channel inward tail current by whole cell voltage clamp assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Inhibition of MAPK3 (unknown origin) | B | 5.31 | pIC50 | 4900 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| ChEMBL | Inhibition of Protein Serine/Threonine Kinase, MAPK3 (ERK1) at 10 µM in the Eurofins-Panlabs enzyme assay (Eurofins_assay_171000) | B | 5.31 | pIC50 | 4870 | nM | IC50 | Data for DCP probe BAY-784 |
| ChEMBL | Selectivity interaction (Leadprofiling screen (Ricerca, enzymes, receptors, transporters, and ion channels )) EUB0000347a MAPK3 | B | 5.31 | pIC50 | 4870 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibition of MAPK14 (unknown origin) | B | 4.97 | pIC50 | 10700 | nM | IC50 | J Med Chem (2020) 63: 11854-11881 [PMID:32960053] |
| ChEMBL | Inhibition of Protein Serine/Threonine Kinase, MAPK14 (p38α) at 10 µM in the Eurofins-Panlabs enzyme assay (Eurofins_assay_176610) | B | 4.97 | pIC50 | 10700 | nM | IC50 | Data for DCP probe BAY-784 |
| ChEMBL | Selectivity interaction (Leadprofiling screen (Ricerca, enzymes, receptors, transporters, and ion channels )) EUB0000347a MAPK14 | B | 4.97 | pIC50 | 10700 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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 | 5.96 | pKi | 1107.9 | nM | Ki | Data for DCP probe BAY-784 |
| ChEMBL | Selectivity interaction (GPCR panel (PDSP screen)) EUB0000347a TMEM97 | B | 5.96 | pKi | 1107.9 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | GPCRScan assay: inhibition of Sigma 2 | B | 5.96 | pKi | 1096.48 | nM | Ki | Data for DCP probe BAY-784 |
ChEMBL data shown on this page come from version 34:
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]
