L-765314 [Ligand Id: 506] 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: CHEMBL19476 (L-765314, NCGC00094440-01) |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
