mitragynine [Ligand Id: 13149] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL299031 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1A receptor expressed in CHO cell membranes incubated for 60 mins | B | 5.87 | pKi | 1340 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1B receptor expressed in CHO cell membranes incubated for 60 mins | B | 5.32 | pKi | 4770 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | Displacement of [3H]prazosin from human recombinant adrenergic alpha-1D receptor expressed in CHO cell membranes incubated for 60 mins | B | 5.26 | pKi | 5480 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2A receptor expressed in CHO cell membranes incubated for 60 mins | B | 5.33 | pKi | 4720 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2B receptor expressed in CHO cell membranes incubated for 60 mins | B | 5.03 | pKi | 9290 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Displacement of [3H]RX 821002 from human recombinant adrenergic alpha-2C receptor expressed in CHO cell membranes incubated for 60 mins | B | 5.63 | pKi | 2320 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Binding affinity to DOP (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| ChEMBL | Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor delta 1 using [3H]DPDPE as radioligand | B | 7.22 | pKi | 60.26 | nM | Ki | J Med Chem (2002) 45: 1949-1956 [PMID:11960505] |
| ChEMBL | Inhibition of DOP (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Displacement of [125I]-IBNtxA from mouse delta opioid receptor-1 expressed in CHO cell membranes incubated for 90 mins | B | 6 | pKi | 1011 | nM | Ki | J Med Chem (2016) 59: 8381-8397 [PMID:27556704] |
| ChEMBL | Antagonist activity at mouse delta opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of DPDPE-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | F | 5.4 | pIC50 | >4000 | nM | IC50 | J Med Chem (2016) 59: 8381-8397 [PMID:27556704] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Binding affinity to KOP (unknown origin) | B | 6.11 | pKi | 772 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| ChEMBL | Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in rat RBL cell membranes incubated for 60 mins | B | 6.7 | pKi | 198 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| ChEMBL | Agonist activity at KOP (unknown origin) | F | 5.07 | pEC50 | 8500 | nM | EC50 | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Displacement of [125I]-IBNtxA from mouse kappa opioid receptor-1 expressed in CHO cell membranes incubated for 90 mins | B | 6.64 | pKi | 231 | nM | Ki | J Med Chem (2016) 59: 8381-8397 [PMID:27556704] |
| ChEMBL | Antagonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of U50,488H-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | F | 5.4 | pIC50 | >4000 | nM | IC50 | J Med Chem (2016) 59: 8381-8397 [PMID:27556704] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor kappa 1 using [3H]- U-69,593 as radioligand | B | 5.96 | pKi | 1096.48 | nM | Ki | J Med Chem (2002) 45: 1949-1956 [PMID:11960505] |
| ChEMBL | Displacement of [3H]U-69593 from kappa opoid receptor in Dunkin-Hartley guinea pig brain after 1 hr by liquid scintillation spectrometry | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2013) 56: 4840-4848 [PMID:23517479] |
| ChEMBL | Inhibition of kappa opioid receptor in guinea pig brain membranes | B | 6.91 | pKi | 123 | nM | Ki | Eur J Med Chem (2019) 183: 111701-111701 [PMID:31550662] |
| ChEMBL | Agonist activity at kappa opioid receptor in guinea pig brain membranes by [35S]-GTPgammaS binding assay | F | 6.64 | pEC50 | 230 | nM | EC50 | Eur J Med Chem (2019) 183: 111701-111701 [PMID:31550662] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Binding affinity to MOP (unknown origin) | B | 6.63 | pKi | 233 | nM | Ki | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cell membranes incubated for 60 mins | B | 6.79 | pKi | 161 | nM | Ki | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| ChEMBL | Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cells incubated for 120 mins by radiometric scintillation analysis | B | 6.79 | pKi | 161 | nM | Ki | J Nat Prod (2021) 84: 1034-1043 [PMID:33635670] |
| ChEMBL | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of cAMP accumulation by HTRF assay | F | 6.47 | pEC50 | 339 | nM | EC50 | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| ChEMBL | Agonist activity at MOP (unknown origin) | F | 6.47 | pEC50 | 339 | nM | EC50 | J Med Chem (2022) 65: 1612-1661 [PMID:34995453] |
| ChEMBL | Agonist activity at human recombinant mu opioid receptor expressed in CHO cells assessed as stimulation of cAMP accumulation incubated for 10 mins by HTRF assay | F | 6.51 | pEC50 | 307.5 | nM | EC50 | J Med Chem (2020) 63: 433-439 [PMID:31834797] |
| ChEMBL | Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay | F | 6.62 | pEC50 | 241.2 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
| GtoPdb | Determined as inhibition of forskolin-stimulated cAMP accumulation in HEK293T cells expressing human mu opioid receptor | - | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
| ChEMBL | Agonist activity at human MOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Glo-sensor cAMP assay | F | 9.31 | pEC50 | 0.49 | nM | EC50 | J Med Chem (2021) 64: 13873-13892 [PMID:34505767] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Displacement of [125I]-IBNtxA from mouse mu opioid receptor-1 expressed in CHO cell membranes incubated for 90 mins | B | 6.64 | pKi | 230 | nM | Ki | J Med Chem (2016) 59: 8381-8397 [PMID:27556704] |
| GtoPdb | Determined as agonist-induced [35S]GTPγS binding in CHO cells expressing mouse mu opioid receptor | - | 6.69 | pEC50 | 203 | nM | EC50 | J Med Chem (2016) 59: 8381-97 [PMID:27556704] |
| ChEMBL | Agonist activity at mouse mu opioid receptor-1 expressed in CHO cell membranes assessed as [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis | F | 6.69 | pEC50 | 203 | nM | EC50 | J Med Chem (2016) 59: 8381-8397 [PMID:27556704] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Inhibition of mu opioid receptor in guinea pig brain membranes | B | 7.89 | pKi | 13 | nM | Ki | Eur J Med Chem (2019) 183: 111701-111701 [PMID:31550662] |
| ChEMBL | Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor mu 1 using [3H]- DAMGO as radioligand | B | 8.14 | pKi | 7.24 | nM | Ki | J Med Chem (2002) 45: 1949-1956 [PMID:11960505] |
| ChEMBL | Displacement of [3H]DAMGO from mu opoid receptor in Dunkin-Hartley guinea pig brain after 1.5 hrs by liquid scintillation spectrometry | B | 8.14 | pKi | 7.2 | nM | Ki | J Med Chem (2013) 56: 4840-4848 [PMID:23517479] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig brain membranes by [35S]-GTPgammaS binding assay | F | 6.64 | pEC50 | 230 | nM | EC50 | Eur J Med Chem (2019) 183: 111701-111701 [PMID:31550662] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]8-OH-DAPT from human recombinant 5-HT1A receptor expressed in CHO cells measured after 60 to 90 mins by radioligand completion assay relative to control | B | 5.23 | pKi | 5880 | nM | Ki | J Med Chem (2021) 64: 13510-13523 [PMID:34467758] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]LSD from human recombinant 5-HT2A receptor expressed in HEK cells by radioligand completion assay relative to control | B | 5.3 | pKi | 5010 | nM | Ki | J Med Chem (2021) 64: 13510-13523 [PMID:34467758] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Displacement of [3H]LSD from human recombinant 5-HT2B receptor expressed in HEK cells by radioligand completion assay relative to control | B | 5.9 | pKi | 1260 | nM | Ki | J Med Chem (2021) 64: 13510-13523 [PMID:34467758] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Displacement of [3H]LSD from human recombinant 5-HT2C receptor expressed in HEK cells by radioligand completion assay relative to control | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13510-13523 [PMID:34467758] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]5-CT from human recombinant 5-HT7A receptor expressed in HEK cells by radioligand completion assay | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2021) 64: 13510-13523 [PMID:34467758] |
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]
