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 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] |
| 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 | 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] |
| 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 | 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 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 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]
