L-765314 [Ligand Id: 506] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL19476 (L-765314, NCGC00094440-01) |
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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 | Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1A adrenergic receptor | B | 6.38 | pKi | 420 | nM | Ki | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| ChEMBL | Binding constant measured against Alpha-1A adrenergic receptor in human prostate; +:inactive | B | 6.38 | pKi | 420 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 657-664 [PMID:15664832] |
| ChEMBL | Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the human prostate Alpha-1A adrenergic receptor subtype | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1A adrenergic receptor | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| ChEMBL | Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat prostate Alpha-1A adrenergic receptor subtype. | B | 6.47 | pIC50 | 340 | nM | IC50 | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - | J Med Chem (1998) 41: 1205-8 [PMID:9548811] |
| ChEMBL | Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1B adrenergic receptor | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| ChEMBL | Compound was tested for the tissue binding affinity using [125I]- HEAT as radioligand to the human aorta Alpha-1B adrenergic receptor | B | 5.24 | pIC50 | 5800 | nM | IC50 | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| ChEMBL | Compound was tested for the tissue binding affinity using [125I]- HEAT as radioligand to the human aorta Alpha-1B adrenergic receptor subtype. | B | 8.06 | pIC50 | 8.8 | nM | IC50 | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
| ChEMBL | Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1B adrenergic receptor | B | 8.27 | pKi | 5.4 | nM | Ki | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| GtoPdb | - | - | 8.3 | pKi | - | - | - | J Med Chem (1998) 41: 1205-8 [PMID:9548811] |
| ChEMBL | Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat liver Alpha-1B adrenergic receptor | B | 8.03 | pIC50 | 9.3 | nM | IC50 | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| ChEMBL | Compound was tested for the tissue binding affinity using [3H]- Prazosin as radioligand to the rat spleen Alpha-1B adrenergic receptor subtype. | B | 8.03 | pIC50 | 9.3 | nM | IC50 | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | Compound was tested for its binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1D adrenergic receptor | B | 7.47 | pKi | 34 | nM | Ki | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| ChEMBL | Compound was evaluated for its ability to displace [125I]HEAT binding from rat Alpha-1D adrenergic receptor | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (1998) 41: 1205-1208 [PMID:9548811] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 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 | 5.1 | pIC50 | 7943.28 | 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 | 5.1 | pIC50 | 7943.28 | 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 | 5.5 | pIC50 | 3162.28 | 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 | 5.5 | pIC50 | 3162.28 | 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 | 5.5 | pIC50 | 3162.28 | 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 | 5.7 | pIC50 | 1995.26 | 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]
