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) [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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
