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: CHEMBL314691 |
---|
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 |
---|---|---|---|---|---|---|---|---|
ABCC2/Canalicular multispecific organic anion transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of BQ-485 uptake in bile canalicular membrane vesicles from SD rat | F | 4.08 | pKi | 84100 | nM | Ki | J Pharmacol Exp Ther (1999) 288: 575-581 [PMID:9918561] |
ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] | ||||||||
ChEMBL | Affinity against ET A receptor | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 253-258 |
ChEMBL | Antagonist activity at Homo sapiens (human) ETA receptor | B | 7.43 | pIC50 | 37 | nM | IC50 | Med Chem Res (2013) 22: 5472-5480 |
ChEMBL | Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer | B | 7.61 | pIC50 | 24.8 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6840-6844 [PMID:20932745] |
ChEMBL | Displacement of [125I]ET-1 from Endothelin A receptor | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2004) 47: 1969-1986 [PMID:15055997] |
ChEMBL | Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis | B | 7.69 | pIC50 | 20.5 | nM | IC50 | J Med Chem (2012) 55: 7849-7861 [PMID:22862294] |
ChEMBL | Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method | F | 9.21 | pIC50 | 0.62 | nM | IC50 | Eur J Med Chem (2016) 121: 658-670 [PMID:27318985] |
GtoPdb | - | - | 7.4 | pA2 | - | - | Ki | Br J Pharmacol (1995) 115: 191-7 [PMID:7647976] |
Endothelin receptor ET-A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4130] [UniProtKB: Q29010] | ||||||||
ChEMBL | Compound was evaluated for the binding affinity to Endothelin A receptor in the porcine aortic smooth muscle | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (1992) 35: 1493-1508 [PMID:1315867] |
ChEMBL | Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes. | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1483-1488 |
ETA receptor/Endothelin receptor ET-A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684] | ||||||||
ChEMBL | Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (1998) 41: 5198-5218 [PMID:9857090] |
ChEMBL | Displacement of [125I]ET-1 from ETA receptor in Sprague-Dawley Rattus norvegicus (rat) myocardium after 1 hr | B | 7.55 | pIC50 | 28 | nM | IC50 | Med Chem Res (2013) 22: 5472-5480 |
ChEMBL | In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor. | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (1998) 41: 2732-2744 [PMID:9667964] |
ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
ChEMBL | Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2012) 55: 7849-7861 [PMID:22862294] |
Endothelin receptor ET-B in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3949] [UniProtKB: P35463] | ||||||||
ChEMBL | Compound was evaluated for the binding affinity to Endothelin B receptor in the porcine cerebellum. | B | 4.64 | pIC50 | 23000 | nM | IC50 | J Med Chem (1992) 35: 1493-1508 [PMID:1315867] |
ChEMBL | Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin B receptor in porcine cerebellum membranes | B | 4.74 | pIC50 | 18000 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1483-1488 |
ETB receptor/Endothelin receptor ET-B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4631] [GtoPdb: 220] [UniProtKB: P21451] | ||||||||
ChEMBL | Ability to inhibit binding of [125I]-ET-1 to membranes prepared from A10 rat cerebellum (Endothelin B receptor) | B | 4.49 | pKi | 32000 | nM | Ki | J Med Chem (1998) 41: 5198-5218 [PMID:9857090] |
ChEMBL | Affinity against ET B receptor | B | 5.15 | pKi | 7000 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 253-258 |
ChEMBL | In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor. | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (1998) 41: 2732-2744 [PMID:9667964] |
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]