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 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]
