McN-A-343 [Ligand Id: 290] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL74300
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
  • 5.66
1 CHEMBL74300_lig_chart_1 Muscarinic acetylcholine receptor M1 HumanRat
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
  • 6
2 CHEMBL74300_lig_chart_2 Muscarinic acetylcholine receptor M2 HumanRat
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • Muscarinic acetylcholine receptor M3 in Guinea pig [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26]
  • 0
3 CHEMBL74300_lig_chart_3 Muscarinic acetylcholine receptor M3 HumanGuinea pig
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • 5.04
4 CHEMBL74300_lig_chart_4 Muscarinic acetylcholine receptor M4 Human
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • 5.42
5 CHEMBL74300_lig_chart_5 Muscarinic acetylcholine receptor M5 Human
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
6 CHEMBL74300_lig_chart_6 Plasmodium falciparum Plasmodium falciparum
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]