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ChEMBL ligand: CHEMBL45281 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] | ||||||||
ChEMBL | Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay | B | 5.56 | pIC50 | 2770 | nM | IC50 | Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559] |
CRF1 receptor/Corticotropin releasing factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1800] [GtoPdb: 212] [UniProtKB: P34998] | ||||||||
ChEMBL | Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3870-3873 [PMID:15990298] |
ChEMBL | Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell. | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 3997-4000 [PMID:14592493] |
ChEMBL | Binding affinity for recombinant human CRF1 receptor | B | 8.57 | pKi | 2.7 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3869-3873 [PMID:15225687] |
ChEMBL | Antagonist activity at human CRF-1 receptor | F | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2011) 54: 4187-4206 [PMID:21618986] |
ChEMBL | Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2005) 48: 1540-1549 [PMID:15743196] |
ChEMBL | Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells | B | 8.7 | pKi | 2 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3870-3873 [PMID:15990298] |
ChEMBL | Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1. | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (1999) 42: 2351-2357 [PMID:10395475] |
ChEMBL | Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (1996) 39: 4358-4360 [PMID:8893829] |
GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | J Med Chem (1996) 39: 4358-60 [PMID:8893829] |
CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353] | ||||||||
ChEMBL | Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand. | B | 7.51 | pKi | 31 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 331-333 [PMID:11212103] |
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 HB3 after 72 hrs by SYBR green assay | F | 5.3 | pIC50 | 5011.87 | 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 | 5.4 | pIC50 | 3981.07 | 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 | 5.4 | pIC50 | 3981.07 | 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 W2 after 72 hrs by SYBR green assay | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
ChEMBL | Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay | B | 5.31 | pEC50 | 4950 | nM | EC50 | Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559] |
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]