SB 228357 [Ligand Id: 192] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL14276 (SB-228357) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | 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 | 5.6 | pIC50 | 2511.89 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 assessed as inhibition of [3H]hypoxanthine incorporation incubated for 24 hrs prior to [3H]hypoxanthine addition measured after 24 hrs by beta scintillation counting | F | 5.67 | pIC50 | 2120 | nM | IC50 | ACS Med Chem Lett (2012) 3: 373-377 [PMID:24900481] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5.7 | pIC50 | 1995.26 | 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 | 5.8 | pIC50 | 1584.89 | 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 | 5.8 | pIC50 | 1584.89 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.8 | pIC50 | 1584.89 | 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 | 6 | pIC50 | 1000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7A assessed as inhibition of [3H]hypoxanthine incorporation incubated for 24 hrs prior to [3H]hypoxanthine addition measured after 24 hrs by beta scintillation counting | F | 6.37 | pIC50 | 430 | nM | IC50 | ACS Med Chem Lett (2012) 3: 373-377 [PMID:24900481] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine receptor 2A in HEK293 cells, using [3H]ketanserin as radioligand. | B | 6.9 | pKi | 125.89 | nM | Ki | J Med Chem (2000) 43: 1123-1134 [PMID:10737744] |
| GtoPdb | - | - | 7 | pKi | - | - | - |
Br J Pharmacol (1999) 126: 572-4 [PMID:10188965]; J Med Chem (2000) 43: 1123-34 [PMID:10737744] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand. | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2000) 43: 1123-1134 [PMID:10737744] |
| GtoPdb | - | - | 8.1 | pKi | - | - | - |
Br J Pharmacol (1999) 126: 572-4 [PMID:10188965]; J Med Chem (2000) 43: 1123-34 [PMID:10737744] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand. | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2000) 43: 1123-1134 [PMID:10737744] |
| GtoPdb | - | - | 9.1 | pKi | - | - | - |
Br J Pharmacol (1999) 126: 572-4 [PMID:10188965]; J Med Chem (2000) 43: 1123-34 [PMID:10737744] |
| ChEMBL | Inhibition of human 5HT2c receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium influx measured up to 30 secs by aequorin luminescence assay | F | 8 | pIC50 | 10 | nM | IC50 | ACS Med Chem Lett (2012) 3: 373-377 [PMID:24900481] |
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]
