PF-03882845 [Ligand Id: 9061] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1215331 (Pf-03882845, PF-3882845) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
| GtoPdb | - | - | 5.05 | pIC50 | 8910 | nM | IC50 | J Med Chem (2014) 57: 4273-88 [PMID:24738581] |
| ChEMBL | Antagonist activity at androgen receptor | F | 5.05 | pIC50 | >8910 | nM | IC50 | J Med Chem (2010) 53: 5979-6002 [PMID:20672822] |
| ChEMBL | Antagonist activity at androgen receptor (unknown origin) by Gal4-based cellular assay | B | 5.05 | pIC50 | >8910 | nM | IC50 | J Med Chem (2014) 57: 4273-4288 [PMID:24738581] |
| Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| ChEMBL | Antagonist activity at estrogen receptor | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 5979-6002 [PMID:20672822] |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | Antagonist activity at glucocorticoid receptor | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2010) 53: 5979-6002 [PMID:20672822] |
| ChEMBL | Antagonist activity at glucocorticoid receptor (unknown origin) by Gal4-based cellular assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2014) 57: 4273-4288 [PMID:24738581] |
| nuclear receptor binding SET domain protein 1/Histone-lysine N-methyltransferase, H3 lysine-36 and H4 lysine-20 specific in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3588738] [GtoPdb: 2696] [UniProtKB: Q96L73] | ||||||||
| ChEMBL | Inhibition of N-terminal polyhistidine-tagged recombinant human NSD1 (1538 to 2696 residues) expressed in baculovirus infected insect cell using SAM as substrate preincubated for 20 mins followed by substrate addition measured after 1 hrs by hotspot assay | B | 4.92 | pIC50 | 12000 | nM | IC50 | Eur J Med Chem (2023) 256: 115440-115440 [PMID:37182335] |
| nuclear receptor binding SET domain protein 2/Histone-lysine N-methyltransferase NSD2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108645] [GtoPdb: 3220] [UniProtKB: O96028] | ||||||||
| ChEMBL | Inhibition of N-terminal polyhistidine-tagged human NSD2 expressed in baculovirus infected insect cell using SAM as substrate preincubated for 20 mins followed by substrate addition measured after 1 hrs by hotspot assay | B | 5.12 | pIC50 | 7600 | nM | IC50 | Eur J Med Chem (2023) 256: 115440-115440 [PMID:37182335] |
| Histone-lysine N-methyltransferase NSD3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108646] [UniProtKB: Q9BZ95] | ||||||||
| ChEMBL | Inhibition of N-terminal GST-fused recombinant human NSD3 (1021 to 1322 residues) expressed in Escherichia coli using SAM as substrate preincubated for 20 mins followed by substrate addition measured after 1 hrs by hotspot assay | B | 5.49 | pIC50 | 3200 | nM | IC50 | Eur J Med Chem (2023) 256: 115440-115440 [PMID:37182335] |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| ChEMBL | Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay | F | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2010) 53: 5979-6002 [PMID:20672822] |
| ChEMBL | Antagonist activity at mineralocorticoid receptor (unknown origin) by Gal4-based cellular assay | B | 8.04 | pIC50 | 9.2 | nM | IC50 | J Med Chem (2014) 57: 4273-4288 [PMID:24738581] |
| GtoPdb | - | - | 8.04 | pIC50 | 9.2 | nM | IC50 | J Med Chem (2014) 57: 4273-88 [PMID:24738581] |
| ChEMBL | Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay | F | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2010) 53: 5979-6002 [PMID:20672822] |
| ChEMBL | Binding affinity to mineralocorticoid receptor (unknown origin) | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2014) 57: 4273-4288 [PMID:24738581] |
| Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
| GtoPdb | - | - | 6.38 | pIC50 | 416 | nM | IC50 | J Med Chem (2014) 57: 4273-88 [PMID:24738581] |
| ChEMBL | Antagonist activity at progesterone receptor | F | 6.38 | pIC50 | 416 | nM | IC50 | J Med Chem (2010) 53: 5979-6002 [PMID:20672822] |
| ChEMBL | Antagonist activity at progesterone receptor (unknown origin) by Gal4-based cellular assay | B | 6.38 | pIC50 | 416 | nM | IC50 | J Med Chem (2014) 57: 4273-4288 [PMID:24738581] |
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]
