McN-A-343 [Ligand Id: 290] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL74300 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| GtoPdb | - | - | 5.2 | pKi | - | - | - | Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells by microplate scintillation counting | B | 5.71 | pKi | 1949.84 | nM | Ki | Bioorg Med Chem (2009) 17: 8174-8185 [PMID:19896386] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M1 receptor transfected in CHO cells after 120 mins by scintillation counting analysis | B | 5.71 | pKi | 1949.84 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3255-3259 [PMID:24980056] |
| ChEMBL | Displacement of [3H]QNB in genetically transformed mouse cell line (m1C2) transfected with Muscarinic acetylcholine receptor M1 | B | 5.14 | pIC50 | 7240 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 803-808 |
| ChEMBL | Inhibitory activity against human Muscarinic acetylcholine receptor M1 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells | F | 5.4 | pIC50 | 4000 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 821-826 |
| ChEMBL | Effective concentration for HMPA (human muscarinic inositol phosphate accumulation) activity measured in CHO cells expressing Muscarinic acetylcholine receptor M1 | F | 5.46 | pEC50 | 3500 | nM | EC50 | Bioorg Med Chem Lett (1992) 2: 821-826 |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| GtoPdb | - | - | 5.1 | pKi | - | - | - | J Pharmacol Exp Ther (1989) 248: 661-70 [PMID:2537406] |
| ChEMBL | In vitro binding affinity for muscarinic M1 receptor by displacing [3H]pirenzepine binding on rat brain homogenate. | B | 6.22 | pKi | 600 | nM | Ki | J Med Chem (1994) 37: 4085-4099 [PMID:7990109] |
| ChEMBL | In vitro binding affinity against muscarinic acetylcholine receptor M1 from rat hippocampus, using [3H]pirenzepine (Pz) as radioligand | B | 6.02 | pIC50 | 955 | nM | IC50 | J Med Chem (1992) 35: 2274-2283 [PMID:1613751] |
| ChEMBL | Displacement of [3H]-Pz (pirenzepine) from the muscarinic receptor M1 of the rat hippocampus | B | 6.02 | pIC50 | 955 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 809-814 |
| ChEMBL | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-Pz as the radioligand. | B | 6.02 | pIC50 | 955 | nM | IC50 | J Med Chem (1995) 38: 3469-3481 [PMID:7658434] |
| ChEMBL | In vitro binding affinity against muscarinic acetylcholine receptor M1 from rat hippocampus, using [3H]oxotremorine-M (Oxo-M) as radioligand | B | 6.45 | pIC50 | 355 | nM | IC50 | J Med Chem (1992) 35: 2274-2283 [PMID:1613751] |
| ChEMBL | Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]OXO-M as the radioligand. | B | 6.45 | pIC50 | 355 | nM | IC50 | J Med Chem (1995) 38: 3469-3481 [PMID:7658434] |
| ChEMBL | M1 agonist activity estimated by rat superior cervical ganglion depolarization | F | 5.41 | pEC50 | >=3900 | nM | EC50 | J Med Chem (1994) 37: 4085-4099 [PMID:7990109] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO cells by microplate scintillation counting | B | 5.49 | pKi | 3235.94 | nM | Ki | Bioorg Med Chem (2009) 17: 8174-8185 [PMID:19896386] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M2 receptor transfected in CHO cells after 120 mins by scintillation counting analysis | B | 5.49 | pKi | 3235.94 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3255-3259 [PMID:24980056] |
| ChEMBL | Inhibitory activity against human Muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate to label antagonist site (RQNB) in CHO cells | F | 4.89 | pIC50 | 12930 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 821-826 |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - | Life Sci (1993) 52: 481-8 [PMID:7680092] |
| ChEMBL | Displacement of [3H]QNB from Muscarinic acetylcholine receptor M2 from rat heart homogenates | B | 4.47 | pIC50 | 34116 | nM | IC50 | Bioorg Med Chem Lett (1992) 2: 803-808 |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| GtoPdb | - | - | 5.3 | pKi | - | - | - | Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO cells by microplate scintillation counting | B | 5.62 | pKi | 2398.83 | nM | Ki | Bioorg Med Chem (2009) 17: 8174-8185 [PMID:19896386] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis | B | 5.62 | pKi | 2398.83 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3255-3259 [PMID:24980056] |
| Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26] | ||||||||
| ChEMBL | In vitro ability to contract isolated guinea pig ileum was used to estimate M2/M3 agonist effect | F | 5.19 | pEC50 | 6500 | nM | EC50 | J Med Chem (1994) 37: 4085-4099 [PMID:7990109] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting | B | 5.04 | pKi | 9120.11 | nM | Ki | Bioorg Med Chem (2009) 17: 8174-8185 [PMID:19896386] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis | B | 5.04 | pKi | 9120.11 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3255-3259 [PMID:24980056] |
| GtoPdb | - | - | 6.7 | pKi | - | - | - | Life Sci (1993) 52: 481-8 [PMID:7680092] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| GtoPdb | - | - | 4.9 | pKi | - | - | - | Br J Pharmacol (1995) 114: 1241-9 [PMID:7620715] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO cells by microplate scintillation counting | B | 5.42 | pKi | 3801.89 | nM | Ki | Bioorg Med Chem (2009) 17: 8174-8185 [PMID:19896386] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic M5 receptor transfected in CHO cells after 120 mins by scintillation counting analysis | B | 5.42 | pKi | 3801.89 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3255-3259 [PMID:24980056] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 4.8 | pIC50 | 15848.93 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
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]
