leuprolide [Ligand Id: 1175] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1201199 (ABBOTT-43818 FREE BASE, CKD-841, Leuporelin, (-)-leuprolide, Leuprolide, Leuprorelin, Leuprorelin slow release, NSC-377526, TAP-144 FREE BASE) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968] | ||||||||
| GtoPdb | - | - | 9.1 | pKi | 0.79 | nM | Ki | Endocrinology (2007) 148: 857-67 [PMID:17095587] |
| ChEMBL | Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2006) 49: 3809-3825 [PMID:16789738] |
| ChEMBL | The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (1998) 41: 4190-4195 [PMID:9784092] |
| ChEMBL | Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2006) 49: 3809-3825 [PMID:16789738] |
| ChEMBL | Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis | B | 9.54 | pIC50 | 0.29 | nM | IC50 | Medchemcomm (2015) 6: 1656-1665 |
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969] | ||||||||
| ChEMBL | The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (1998) 41: 4190-4195 [PMID:9784092] |
| GtoPdb | - | - | 9.1 | pIC50 | - | - | - | Endocrinology (1994) 135: 315-20 [PMID:8013367] |
| ChEMBL | The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (1998) 41: 4190-4195 [PMID:9784092] |
| ChEMBL | Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2006) 49: 3809-3825 [PMID:16789738] |
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]
