AM404 [Ligand Id: 12556] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL39878 (AM-404) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| proteasome 20S subunit beta 1/proteasome 20S subunit beta 8/proteasome 20S subunit beta 9/proteasome 20S subunit beta 6/proteasome 20S subunit beta 5/proteasome 20S subunit beta 2/20S proteasome in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL3831201] [GtoPdb: 2404, 2408, 2409, 2407, 2406, 2405] [UniProtKB: A5LHX3, O14818, P20618, P25786, P25787, P25788, P25789, P28062, P28065, P28066, P28070, P28072, P28074, P40306, P49720, P49721, P60900, Q8TAA3, Q99436] | ||||||||
| ChEMBL | Stimulation of human 20S proteasome using 11 amino acid FRET peptide as substrate measured every 2 mins over 1 hr by FRET assay | B | 4.55 | pEC50 | 28000 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 420-423 [PMID:30587447] |
| Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612] | ||||||||
| ChEMBL | Inhibition of fatty acid amide hydrolase (FAAH) was determined using rat brain homogenates as the enzyme source and [3H]anandamide as substrate | B | 5.43 | pIC50 | 3700 | nM | IC50 | J Med Chem (2003) 46: 1512-1522 [PMID:12672252] |
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor | B | 5.75 | pKi | 1760 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 138-141 [PMID:16213718] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells | B | 5.82 | pKi | 1500 | nM | Ki | J Med Chem (2008) 51: 7800-7805 [PMID:19053765] |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Tested for binding affinity to Cannabinoid receptor 1 | B | 5.75 | pKi | 1760 | nM | Ki | J Med Chem (1999) 42: 896-902 [PMID:10072686] |
| ChEMBL | Displacement of [3H]CP-55940 from Cannabinoid receptor 1 of rat forebrain membranes | B | 5.75 | pKi | 1760 | nM | Ki | J Med Chem (1996) 39: 4515-4519 [PMID:8893848] |
| ChEMBL | Binding affinity against G protein coupled Cannabinoid receptor 1 using [3H]WIN-55212-2 in rat cerebellum membranes | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 1512-1522 [PMID:12672252] |
| ChEMBL | Binding affinity to CB1 cannabinoid receptor using [3H]WIN-55212-2 in rat cerebellum membranes | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2001) 44: 4505-4508 [PMID:11741470] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | B | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2008) 51: 7800-7805 [PMID:19053765] |
| ChEMBL | Binding affinity against G protein coupled human Cannabinoid receptor 2 using [3H]CP-55940 in HEK293 EBNA transfected cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 1512-1522 [PMID:12672252] |
| ChEMBL | Binding affinity to human CB2 cannabinoid receptor using [3H]CP-55940 in HEK293 EBNA transfected cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2001) 44: 4505-4508 [PMID:11741470] |
| CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936] | ||||||||
| ChEMBL | Compound was evaluated for its binding affinity for mouse spleen Cannabinoid receptor 2 | B | 4.89 | pKi | 13000 | nM | Ki | J Med Chem (1996) 39: 4515-4519 [PMID:8893848] |
| Cruzipain in Trypanosoma cruzi (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3563] [UniProtKB: P25779] | ||||||||
| ChEMBL | Inhibition of Trypanosoma cruzi cruzain by quantitative high throughput screening | B | 4.22 | pIC50 | >60000 | nM | IC50 | J Med Chem (2010) 53: 37-51 [PMID:19908840] |
| ChEMBL | Inhibition of Trypanosoma cruzi cruzain by Flexstation microplate spectrofluorimetry | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Med Chem (2010) 53: 37-51 [PMID:19908840] |
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| ChEMBL | Agonist activity at TRPV1 | F | 7.59 | pEC50 | 26 | nM | EC50 | Bioorg Med Chem (2012) 20: 101-107 [PMID:22172309] |
| TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] | ||||||||
| ChEMBL | Binding affinity against vanilloid receptor 1 (VR1) using [3H]RTX in rat spinal cord membranes | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2003) 46: 1512-1522 [PMID:12672252] |
| ChEMBL | Binding affinity to vanilloid VR1 receptor using [3H]resiniferatoxin ([3H]-RTX) in rat spinal cord membranes | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (2001) 44: 4505-4508 [PMID:11741470] |
| ChEMBL | Agonist activity at TRPV1 in rat isolated mesenteric arteries assessed as vasorelaxation of phenylephrine-induced contraction | B | 7.3 | pEC50 | 50.12 | nM | EC50 | Eur J Med Chem (2021) 213: 113042-113042 [PMID:33257173] |
| TRPV4 in Human [GtoPdb: 510] [UniProtKB: Q9HBA0] | ||||||||
| GtoPdb | - | - | 5 | pIC50 | 10000 | nM | IC50 | Heliyon (2020) 6: e03301 [PMID:32051870] |
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]
