Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Unit Assay Type Assay Description Mol
weight
Rot
Bonds
H don H acc LogP Smiles
CHEMBL2370066 ednra_human Human No 7.9 EC50 = 13 nM Bind
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL315841 ednra_human Human No 7.8 EC50 = 17 nM Bind
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL2370067 ednra_human Human No 5.7 EC50 = 2100 nM Bind
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](N)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@H](C=O)Cc1c[nH]c2ccccc12)[C@@H](C)CC
CHEMBL407269 ednra_human Human No 7.6 EC50 = 25 nM Bind
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL313344 ednra_human Human No 5.6 EC50 = 2700 nM Bind
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)CC
CHEMBL387200 ednra_human Human No 6.2 EC50 = 580 nM Bind
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL86703 ednra_human Human No 5.2 EC50 = 6000 nM Bind
Effective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cellsEffective concentration against ET A receptor from rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)C(C)C
CHEMBL112144 ednra_pig Pig No 11.4 IC50 = 0.0 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
629 11 1 10 5.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(Br)cn1
CHEMBL286621 ednra_human Human No 11.0 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
520 9 4 8 3.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1
CHEMBL289634 ednra_human Human No 11.0 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
532 10 2 7 5.4 COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O
CHEMBL411925 ednra_human Human No 11.0 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
532 10 3 7 5.2 CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O
CHEMBL332922 ednra_pig Pig No 10.9 IC50 = 0.0 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
579 11 1 9 5.8 CCc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(SC)cn2)cc1
CHEMBL287683 ednra_human Human No 10.9 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
559 9 2 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1
CHEMBL432856 ednra_human Human No 10.9 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
518 8 3 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)(C)O)c1
CHEMBL112624 ednra_rat Rat Yes 10.8 IC50 = 0.0 nM Bind
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL1627022 ednra_rat Rat Yes 10.8 IC50 = 0.0 nM Bind
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL114380 ednra_pig Pig No 10.8 IC50 = 0.0 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
581 12 1 11 4.6 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2Oc2cccc(OC)c2)nc1
CHEMBL115724 ednra_pig Pig No 10.7 IC50 = 0.0 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
645 11 1 10 5.7 COc1ccccc1Sc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(Br)cn1
CHEMBL294291 ednra_human Human No 10.7 IC50 = 0.0 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
481 6 2 7 4.9 CC(=O)c1c(C)c(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL60058 ednra_human Human No 10.7 IC50 = 0.0 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
482 6 3 8 4.6 C/C(=N\O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL35984 ednra_human Human No 10.7 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
504 9 3 7 4.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCCO)c1
CHEMBL4128926 ednra_human Human No 10.6 IC50 = 0.0 nM Bind
Displacement of [125I]-endothelin-1 from human recombinant ETA receptor after 120 mins by scintillation counting analysisDisplacement of [125I]-endothelin-1 from human recombinant ETA receptor after 120 mins by scintillation counting analysis
583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12
CHEMBL3775234 ednra_human Human Yes 10.6 IC50 = 0.0 nM Bind
Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cellsDisplacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells
None None None None
CHEMBL3775234 ednra_human Human Yes 10.6 IC50 = 0.0 nM Bind
Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method
None None None None
CHEMBL287683 ednra_human Human No 10.6 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
559 9 2 7 4.9 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)C(=O)N(C)C)c1
CHEMBL289634 ednra_human Human No 10.6 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
532 10 2 7 5.4 COCC(C)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O
CHEMBL4538570 ednra_rat Rat No 10.6 IC50 = 0.0 nM Bind
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
607 10 1 10 6.4 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cc3ccccc3s2)nc1
CHEMBL170908 ednra_pig Pig No 10.6 IC50 = 0.0 nM Bind
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
671 13 1 10 6.3 CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(Oc2ccccc2OC)c(OCCOc2ncc(Br)cn2)n1
CHEMBL37427 ednra_human Human No 10.6 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
531 8 2 7 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CN(C)C(C)=O)c1
CHEMBL115333 ednra_pig Pig No 10.6 IC50 = 0.0 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
581 11 1 10 5.2 COc1cccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(SC)cn2)c1
CHEMBL293830 ednra_human Human No 10.5 IC50 = 0.0 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
493 7 2 7 5.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C2CC2)c1
CHEMBL304460 ednra_human Human No 10.5 IC50 = 0.0 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
503 6 2 8 3.8 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(S(C)(=O)=O)c1
CHEMBL60367 ednra_human Human No 10.5 IC50 = 0.0 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
495 7 2 7 5.3 CCC(=O)c1c(C)c(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL287622 ednra_human Human No 10.5 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
490 8 3 7 4.2 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCO)c1
CHEMBL1206706 ednra_rat Rat No 10.5 IC50 = 0.0 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
538 10 1 9 4.8 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F
CHEMBL298725 ednra_rat Rat No 10.5 IC50 = 0.0 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
538 10 1 9 4.8 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1F
CHEMBL9194 ednra_human Human Yes 10.5 IC50 = 0.0 nM Bind
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL115372 ednra_rat Rat No 10.5 IC50 = 0.0 nM Bind
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
549 10 2 9 4.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1
CHEMBL1627023 ednra_rat Rat No 10.5 IC50 = 0.0 nM Bind
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
549 10 2 9 4.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(CO)cn2)cc1
CHEMBL9194 ednra_human Human Yes 10.5 IC50 = 0.0 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL1181545 ednra_pig Pig No 10.4 IC50 = 0.0 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
596 10 1 9 5.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccccn3)cn2)cc1
CHEMBL177173 ednra_pig Pig No 10.4 IC50 = 0.0 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
596 10 1 9 5.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccccn3)cn2)cc1
CHEMBL289216 ednra_human Human No 10.4 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
520 9 3 8 4.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1
CHEMBL112531 ednra_rat Rat No 10.4 IC50 = 0.0 nM Bind
Ability to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptorAbility to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptor
597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL369489 ednra_rat Rat No 10.4 IC50 = 0.0 nM Bind
Ability to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptorAbility to inhibit specific binding of [125I]- -ET-1 to rat A 10 cells which express endothelin A receptor
597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL112531 ednra_rat Rat No 10.4 IC50 = 0.0 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL369489 ednra_rat Rat No 10.4 IC50 = 0.0 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
597 9 1 8 5.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL323464 ednra_rat Rat No 10.4 IC50 = 0.0 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL114298 ednra_pig Pig No 10.4 IC50 = 0.0 nM Bind
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
581 11 2 10 4.7 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(CO)cc2)nc1
CHEMBL324184 ednra_pig Pig No 10.4 IC50 = 0.0 nM Bind
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
613 10 2 9 4.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(CO)cc2)cc1
CHEMBL19950 ednra_human Human No 10.4 IC50 = 0.0 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
467 6 2 7 4.6 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL416324 ednra_human Human No 10.4 IC50 = 0.0 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
496 7 2 8 4.7 CO/N=C(\C)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL60149 ednra_human Human No 10.4 IC50 = 0.0 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
469 6 2 8 3.8 COC(=O)c1cc(C)ccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL19950 ednra_human Human No 10.4 IC50 = 0.0 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
467 6 2 7 4.6 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL288247 ednra_human Human No 10.4 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
518 9 3 7 4.8 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1
CHEMBL170493 ednra_pig Pig No 10.4 IC50 = 0.0 nM Bind
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
674 10 1 9 6.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(-c3ccccn3)nc2OCCOc2ncc(Br)cn2)cc1
CHEMBL323464 ednra_human Human No 10.4 IC50 = 0.0 nM Bind
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL411925 ednra_human Human No 10.4 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
532 10 3 7 5.2 CCC(CO)Cc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O
CHEMBL437472 ednra_human Human No 10.3 IC50 = 0.0 nM Bind
Inhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation counting
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL36627 ednra_human Human No 10.3 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
476 7 2 7 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC)c1
CHEMBL286621 ednra_human Human No 10.3 IC50 = 0.0 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
520 9 4 8 3.5 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(O)CO)c1
CHEMBL177973 ednra_rat Rat No 10.3 IC50 = 0.1 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
606 15 1 10 5.1 COC(=O)CCCCOc1cc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc(OC)c1OC
CHEMBL437472 ednra_human Human No 10.3 IC50 = 0.1 nM Bind
Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL291592 ednra_human Human No 10.3 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
531 7 2 8 4.6 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(S(=O)(=O)C(C)C)c1
CHEMBL62159 ednra_human Human No 10.3 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
464 5 2 7 4.5 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C#N)c1C
CHEMBL291058 ednra_human Human No 10.3 IC50 = 0.1 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
606 13 1 11 4.6 COC(=O)CCCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC
CHEMBL114700 ednra_pig Pig No 10.3 IC50 = 0.1 nM Bind
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membraneIn vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane
629 11 1 10 5.4 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)c1
CHEMBL114700 ednra_pig Pig No 10.3 IC50 = 0.1 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
629 11 1 10 5.4 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)c1
CHEMBL419367 ednra_human Human No 10.3 IC50 = 0.1 nM Bind
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F
CHEMBL9194 ednra_human Human Yes 10.3 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneDisplacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL289216 ednra_human Human No 10.2 IC50 = 0.1 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
520 9 3 8 4.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)CO)c1
CHEMBL114964 ednra_pig Pig No 10.2 IC50 = 0.1 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
585 11 1 10 5.3 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)c1
CHEMBL288247 ednra_human Human No 10.2 IC50 = 0.1 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
518 9 3 7 4.8 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CC(C)CO)c1
CHEMBL62019 ednra_human Human No 10.2 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
531 8 2 8 4.6 CCCS(=O)(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL62112 ednra_human Human No 10.2 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
481 7 2 7 5.0 CCC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL287711 ednra_human Human No 10.2 IC50 = 0.1 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
476 7 3 7 4.1 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CO)c1
CHEMBL37920 ednra_human Human No 10.2 IC50 = 0.1 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
532 9 3 7 5.3 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(CCC(C)(C)O)c1
CHEMBL339904 ednra_rat Rat No 10.2 IC50 = 0.1 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
528 12 1 6 4.8 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL325581 ednra_human Human No 10.2 IC50 = 0.1 nM Bind
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl
CHEMBL300577 ednra_human Human No 10.2 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
496 6 2 7 4.1 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)N(C)C)c1
CHEMBL109644 ednra_human Human No 10.1 IC50 = 0.1 nM Bind
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL111277 ednra_human Human No 10.1 IC50 = 0.1 nM Bind
Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).Binding assay performed using human Endothelin A receptor (hETA) expressed in chinese hamster ovary cells(CHO).
578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL9194 ednra_human Human Yes 10.1 IC50 = 0.1 nM Bind
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL111277 ednra_human Human No 10.1 IC50 = 0.1 nM Bind
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL299921 ednra_human Human No 10.1 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
492 6 2 8 5.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ncco2)c1
CHEMBL432521 ednra_human Human Yes 10.1 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
447 6 2 7 4.2 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1C
CHEMBL58359 ednra_human Human No 10.1 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
444 5 2 7 4.2 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C#N)c1C
CHEMBL176272 ednra_rat Rat No 10.1 IC50 = 0.1 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
553 9 1 8 5.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1
CHEMBL323243 ednra_rat Rat No 10.1 IC50 = 0.1 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
553 9 1 8 5.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(Cl)cn2)cc1
CHEMBL9194 ednra_rat Rat Yes 10.1 IC50 = 0.1 nM Bind
Inhibitory activity against human Endothelin A receptorInhibitory activity against human Endothelin A receptor
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL293398 ednra_human Human No 10.1 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
459 5 2 6 5.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(Cl)c1
CHEMBL69986 ednra_human Human No 10.1 IC50 = 0.1 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
592 12 1 11 4.2 COC(=O)CCCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC
CHEMBL325581 ednra_rat Rat No 10.0 IC50 = 0.1 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl
CHEMBL323464 ednra_rat Rat No 10.0 IC50 = 0.1 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL4467748 ednra_human Human No 10.0 IC50 = 0.1 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
554 12 2 9 3.5 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1
CHEMBL305602 ednra_human Human No 10.0 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
545 8 2 9 3.6 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)CS(C)(=O)=O)c1
CHEMBL448165 ednra_human Human No 10.0 IC50 = 0.1 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
446 6 2 6 4.6 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1
CHEMBL19661 ednra_human Human No 10.0 IC50 = 0.1 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
478 6 2 7 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2noc(C)c2Cl)c(C)c1CC#N
CHEMBL109644 ednra_rat Rat No 10.0 IC50 = 0.1 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL129220 ednra_rat Rat Yes 10.0 IC50 = 0.1 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
540 13 1 7 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(OC)c1
CHEMBL437472 ednra_human Human No 10.0 IC50 = 0.1 nM Bind
Binding affinity to human ETA receptor by radioligand displacement assayBinding affinity to human ETA receptor by radioligand displacement assay
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL59819 ednra_human Human No 10.0 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
497 7 2 8 4.6 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)OC(C)C)c1
CHEMBL1272244 ednra_human Human No 10.0 IC50 = 0.1 nM Bind
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
543 10 2 7 5.1 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2
CHEMBL321242 ednra_pig Pig No 10.0 IC50 = 0.1 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
519 9 1 8 4.8 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncccn2)cc1
CHEMBL290181 ednra_human Human No 10.0 IC50 = 0.1 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
504 8 2 7 5.4 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OC(C)C)c1
CHEMBL8923 ednra_human Human Yes 10.0 IC50 = 0.1 nM Bind
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1
CHEMBL177378 ednra_rat Rat No 9.9 IC50 = 0.1 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
548 13 1 8 5.6 CCOc1cc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc(OCC)c1OCC
CHEMBL336272 ednra_rat Rat No 9.9 IC50 = 0.1 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
494 11 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1
CHEMBL417067 ednra_human Human No 9.9 IC50 = 0.1 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
548 11 1 9 5.0 CCOc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OCC)c1OCC
CHEMBL432012 ednra_human Human No 9.9 IC50 = 0.1 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
446 7 2 6 4.6 CCCNc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2
CHEMBL277706 ednra_human Human No 9.9 IC50 = 0.1 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
495 7 2 7 5.2 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C(C)C)c1
CHEMBL111277 ednra_rat Rat No 9.9 IC50 = 0.1 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL109644 ednra_human Human No 9.9 IC50 = 0.1 nM Funct
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.
592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL60276 ednra_human Human No 9.9 IC50 = 0.1 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
468 6 3 7 3.5 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1
CHEMBL18626 ednra_human Human No 9.9 IC50 = 0.1 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
478 6 2 7 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1CC#N
CHEMBL19921 ednra_human Human No 9.9 IC50 = 0.1 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
454 6 2 7 4.6 Cc1cc(C)c(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O
CHEMBL277595 ednra_human Human No 9.8 IC50 = 0.2 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1
CHEMBL167314 ednra_pig Pig No 9.8 IC50 = 0.2 nM Bind
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
705 14 2 12 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(SCCO)nc1OCCOc1ncc(Br)cn1
CHEMBL437472 ednra_pig Pig No 9.8 IC50 = 0.2 nM Bind
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL128818 ednra_human Human No 9.8 IC50 = 0.2 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1
CHEMBL437472 ednra_human Human No 9.8 IC50 = 0.2 nM Bind
Displacement of radiolabeled endothelin-1 from human endothelin ETA receptorDisplacement of radiolabeled endothelin-1 from human endothelin ETA receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL112141 ednra_pig Pig No 9.8 IC50 = 0.2 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
571 10 1 10 5.6 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)s2)nc1
CHEMBL1181553 ednra_pig Pig No 9.8 IC50 = 0.2 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
583 10 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL177924 ednra_pig Pig No 9.8 IC50 = 0.2 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
583 10 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)C)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL340575 ednra_rat Rat No 9.8 IC50 = 0.2 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
508 12 1 5 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1
CHEMBL277595 ednra_human Human No 9.8 IC50 = 0.2 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1
CHEMBL279471 ednra_human Human No 9.8 IC50 = 0.2 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
458 6 2 7 4.4 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2C)c(C)c1CC#N
CHEMBL110053 ednra_human Human No 9.8 IC50 = 0.2 nM Bind
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
515 13 1 6 3.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O
CHEMBL128818 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
510 11 1 4 5.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)c(F)c1
CHEMBL1790959 ednra_pig Pig No 9.7 IC50 = 0.2 nM Bind
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL61211 ednra_rat Rat No 9.7 IC50 = 0.2 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1
CHEMBL61211 ednra_rat Rat No 9.7 IC50 = 0.2 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1
CHEMBL61211 ednra_rat Rat No 9.7 IC50 = 0.2 nM Bind
Displacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 minsDisplacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 mins
460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1
CHEMBL280659 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
455 5 3 7 4.4 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1O
CHEMBL1790963 ednra_pig Pig No 9.7 IC50 = 0.2 nM Bind
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL4553625 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
570 13 2 10 2.8 COCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1
CHEMBL168604 ednra_pig Pig No 9.7 IC50 = 0.2 nM Bind
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
689 14 2 12 4.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(OCCO)nc1OCCOc1ncc(Br)cn1
CHEMBL437472 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL302974 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
605 11 1 11 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCN3CCOCC3)c2)cc1
CHEMBL308646 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
564 10 1 11 3.4 COC(=O)COc1cc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc(OC)c1OC
CHEMBL101424 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
443 7 1 5 4.9 C=CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2
CHEMBL70385 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
637 12 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1
CHEMBL437472 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL1790960 ednra_pig Pig No 9.7 IC50 = 0.2 nM Bind
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
None None None CCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL323055 ednra_rat Rat No 9.7 IC50 = 0.2 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
564 12 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CC(C)C
CHEMBL64632 ednra_rat Rat No 9.7 IC50 = 0.2 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
476 7 1 7 5.2 COc1ccc(OC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1
CHEMBL294563 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
481 6 2 7 4.9 CC(=O)c1cc(C)cc(C)c1NC(=O)c1sc(C)cc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL102969 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
445 7 1 5 5.1 CCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2
CHEMBL419367 ednra_rat Rat No 9.7 IC50 = 0.2 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F
CHEMBL36671 ednra_human Human No 9.7 IC50 = 0.2 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
462 6 3 7 4.3 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(O)c1
CHEMBL9334 ednra_rat Rat No 9.7 IC50 = 0.2 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
496 11 1 6 4.3 CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1
CHEMBL437472 ednra_human Human No 9.6 IC50 = 0.2 nM Bind
Displacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Endothelin-1 from human recombinant ETA receptor expressed in CHOK1 cells after 2 hrs
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL1205177 ednra_human Human Yes 9.6 IC50 = 0.2 nM Bind
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O
CHEMBL61425 ednra_human Human Yes 9.6 IC50 = 0.2 nM Bind
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O
CHEMBL1205177 ednra_human Human Yes 9.6 IC50 = 0.2 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O
CHEMBL61425 ednra_human Human Yes 9.6 IC50 = 0.2 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
927 12 9 11 0.8 CC(C)C[C@@H]1NC(=O)[C@@H](c2cccs2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N2CCN(c3ccccc3)CC2)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O
CHEMBL1184515 ednra_rat Rat No 9.6 IC50 = 0.3 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
601 10 1 9 6.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1
CHEMBL367445 ednra_rat Rat No 9.6 IC50 = 0.3 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
601 10 1 9 6.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3cccs3)cn2)cc1
CHEMBL313871 ednra_human Human Yes 9.6 IC50 = 0.3 nM Bind
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2
CHEMBL8978 ednra_human Human Yes 9.6 IC50 = 0.3 nM Bind
Ability to displace endothelin ([125I]ET1) from human Endothelin A receptorAbility to displace endothelin ([125I]ET1) from human Endothelin A receptor
539 10 2 7 4.8 CCCc1cc(C(=O)O)ccc1OC(C(=O)NS(=O)(=O)c1ccc(C(C)C)cc1)c1ccc2c(c1)OCO2
CHEMBL293192 ednra_rat Rat No 9.6 IC50 = 0.3 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
442 8 1 6 5.7 CCCCSC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL2304284 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Inhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation countingInhibition of ETA receptor in human SK-N-MC cells after 60 mins by scintillation counting
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL353560 ednra_rat Rat No 9.5 IC50 = 0.3 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
502 15 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCCCC(C)C
CHEMBL116281 ednra_pig Pig No 9.5 IC50 = 0.3 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
601 10 1 9 6.4 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc3ccccc3c2)nc1
CHEMBL304762 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
578 12 2 10 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCC(=O)O)c2)cc1
CHEMBL109778 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1
CHEMBL109926 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
530 14 1 6 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC
CHEMBL432974 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC
CHEMBL8981 ednra_human Human Yes 9.5 IC50 = 0.3 nM Funct
Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK
506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1
CHEMBL8981 ednra_human Human Yes 9.5 IC50 = 0.3 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1
CHEMBL70385 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
637 12 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1
CHEMBL4455360 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
568 13 2 9 3.9 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1
CHEMBL4458005 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
524 13 2 9 3.8 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1
CHEMBL8981 ednra_mouse Mouse Yes 9.5 IC50 = 0.3 nM Bind
Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomesDisplacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes
506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1
CHEMBL2165339 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
600 12 2 8 4.0 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1
CHEMBL1205068 ednra_rat Rat No 9.5 IC50 = 0.3 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
520 10 1 9 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1
CHEMBL48907 ednra_rat Rat No 9.5 IC50 = 0.3 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
520 10 1 9 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1
CHEMBL69832 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
592 13 2 10 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCCC(=O)O)c2)cc1
CHEMBL8981 ednra_human Human Yes 9.5 IC50 = 0.3 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1
CHEMBL69741 ednra_rat Rat No 9.5 IC50 = 0.3 nM Bind
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
520 8 1 10 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4nsnc4c3)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1
CHEMBL72037 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1
CHEMBL437472 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL9194 ednra_rat Rat Yes 9.5 IC50 = 0.3 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL1204799 ednra_human Human Yes 9.5 IC50 = 0.3 nM Funct
Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK
528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]
CHEMBL25438 ednra_human Human Yes 9.5 IC50 = 0.3 nM Funct
Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK
528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]
CHEMBL9194 ednra_human Human Yes 9.5 IC50 = 0.3 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL9194 ednra_rat Rat Yes 9.5 IC50 = 0.3 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL63267 ednra_rat Rat No 9.5 IC50 = 0.3 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
424 8 1 5 5.8 CCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL102314 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
445 6 1 5 5.0 COc1ccc([C@@H]2c3nc(CC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1
CHEMBL112624 ednra_rat Rat Yes 9.5 IC50 = 0.3 nM Bind
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL1627022 ednra_rat Rat Yes 9.5 IC50 = 0.3 nM Bind
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL64447 ednra_rat Rat No 9.5 IC50 = 0.3 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
438 9 1 6 5.1 C=CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL10862 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1
CHEMBL1204672 ednra_human Human No 9.5 IC50 = 0.3 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1
CHEMBL319452 ednra_human Human No 9.5 IC50 = 0.4 nM Bind
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
635 12 1 12 4.1 CCOC(=O)CNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1
CHEMBL9194 ednra_rat Rat Yes 9.4 IC50 = 0.4 nM Bind
Binding affinity against Endothelin A receptor in MMQ cells in ratBinding affinity against Endothelin A receptor in MMQ cells in rat
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL8923 ednra_rat Rat Yes 9.4 IC50 = 0.4 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
510 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1
CHEMBL8981 ednra_human Human Yes 9.4 IC50 = 0.4 nM Bind
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1
CHEMBL114660 ednra_pig Pig No 9.4 IC50 = 0.4 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
597 12 1 11 5.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)ncnc1OCCOc1ncc(SC)cn1
CHEMBL105591 ednra_human Human No 9.4 IC50 = 0.4 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
431 6 1 5 4.8 CCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2
CHEMBL323464 ednra_human Human No 9.4 IC50 = 0.4 nM Funct
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.
564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL109778 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1
CHEMBL1207463 ednra_human Human No 9.4 IC50 = 0.4 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
614 12 2 11 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1
CHEMBL408055 ednra_human Human No 9.4 IC50 = 0.4 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
614 12 2 11 3.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCS(=O)(=O)O)c2)cc1
CHEMBL437472 ednra_human Human No 9.4 IC50 = 0.4 nM Bind
Inhibition of human ETA receptorInhibition of human ETA receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](CO)C(=O)N[C@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL300547 ednra_human Human No 9.4 IC50 = 0.4 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
529 7 2 7 5.6 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)c2ccccc2)c1
CHEMBL325581 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl
CHEMBL112624 ednra_human Human Yes 9.4 IC50 = 0.4 nM Bind
Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)
613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL1627022 ednra_human Human Yes 9.4 IC50 = 0.4 nM Bind
Antagonist activity at ET-A receptor (unknown origin)Antagonist activity at ET-A receptor (unknown origin)
613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL450337 ednra_human Human No 9.4 IC50 = 0.4 nM Bind
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
649 13 1 12 4.5 CCOC(=O)CCNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1
CHEMBL9194 ednra_rat Rat Yes 9.4 IC50 = 0.4 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL112624 ednra_human Human Yes 9.4 IC50 = 0.4 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL1627022 ednra_human Human Yes 9.4 IC50 = 0.4 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
613 11 2 9 4.5 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)CO)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL2163692 ednra_human Human No 9.4 IC50 = 0.4 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
588 13 2 10 3.6 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cc(OC)ccc1Cl
CHEMBL368996 ednra_human Human No 9.4 IC50 = 0.4 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
690 12 2 14 3.9 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1cnccn1
CHEMBL417413 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
426 8 1 6 4.9 CCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL109926 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
530 14 1 6 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2cc(OC)c3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC
CHEMBL291247 ednra_human Human No 9.4 IC50 = 0.4 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
504 9 2 7 5.4 CCCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O
CHEMBL62264 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
410 7 1 5 5.4 CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL62264 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
410 7 1 5 5.4 CCCCC1=C(C(=O)O)[C@@H](c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL110053 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
515 13 1 6 3.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCN1CCCC1=O
CHEMBL116046 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
565 10 1 9 5.5 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1
CHEMBL177979 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
565 10 1 9 5.5 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1
CHEMBL1790962 ednra_pig Pig No 9.4 IC50 = 0.4 nM Bind
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL419383 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
574 15 1 7 4.9 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL269141 ednra_rat Rat No 9.4 IC50 = 0.4 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
538 12 1 6 5.2 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(CCC(C)C)CCC(C)C)cc1
CHEMBL283582 ednra_human Human No 9.4 IC50 = 0.4 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
453 6 2 6 4.9 CCc1cc(C)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL8981 ednra_rat Rat Yes 9.4 IC50 = 0.4 nM Bind
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1
CHEMBL61211 ednra_human Human No 9.4 IC50 = 0.5 nM Bind
Binding affinity at human Endothelin A receptorBinding affinity at human Endothelin A receptor
460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)[C@@H](c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1
CHEMBL354528 ednra_pig Pig No 9.4 IC50 = 0.5 nM Bind
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
727 12 1 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(N2CCN(C)CC2)nc1OCCOc1ncc(Br)cn1
CHEMBL109644 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
592 15 1 7 5.0 CCCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL322297 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
578 13 1 7 4.5 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCC(C)C
CHEMBL9488 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
524 12 1 6 5.1 CCCCN(CCCC)C(=O)C(C)N1CC(c2ccc3c(c2)OCO3)C(C(=O)O)C1c1ccc(OC)cc1
CHEMBL111277 ednra_human Human No 9.3 IC50 = 0.5 nM Funct
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.
578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL112832 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL62762 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
440 9 1 6 5.3 CCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL116108 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
585 10 1 9 6.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1
CHEMBL175501 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
585 10 1 9 6.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(-c3ccco3)cn2)cc1
CHEMBL111612 ednra_human Human Yes 9.3 IC50 = 0.5 nM Bind
Inhibitory activity against human endothelin A receptorInhibitory activity against human endothelin A receptor
532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC
CHEMBL112832 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL174573 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
536 11 1 9 4.4 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1
CHEMBL368558 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
524 13 1 6 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](CC(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL10781 ednra_human Human No 9.3 IC50 = 0.5 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
536 9 1 10 3.9 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1
CHEMBL11369 ednra_human Human No 9.3 IC50 = 0.5 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
520 8 1 9 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C
CHEMBL316523 ednra_human Human No 9.3 IC50 = 0.5 nM Bind
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
691 14 1 12 5.6 CCOC(=O)C(CC(C)C)NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1
CHEMBL112832 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3occc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL2103873 ednra_human Human Yes 9.3 IC50 = 0.5 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br
CHEMBL2110610 ednra_human Human Yes 9.3 IC50 = 0.5 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
517 4 1 5 5.0 CCc1cc(C2=C(C(=O)O)N(c3ccccc3C(F)(F)F)S(=O)(=O)c3ccccc32)cc2c1OCO2
CHEMBL4521348 ednra_human Human No 9.3 IC50 = 0.5 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
552 13 2 9 3.2 CCCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(OC)cn2)c1-c1ccc(Br)cc1
CHEMBL4528516 ednra_human Human No 9.3 IC50 = 0.5 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
540 13 2 10 3.4 CCCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1
CHEMBL2103873 ednra_human Human Yes 9.3 IC50 = 0.5 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
586 11 2 8 3.6 CCCNS(=O)(=O)Nc1ncnc(c1c1ccc(cc1)Br)OCCOc1ncc(cn1)Br
CHEMBL282187 ednra_human Human No 9.3 IC50 = 0.5 nM Bind
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
512 11 2 7 3.8 COCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(C)nc2OC)c1-c1ccc(CC(C)C)cc1
CHEMBL32066 ednra_human Human No 9.3 IC50 = 0.5 nM Bind
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
468 8 2 6 3.8 CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(C)nc2OC)c1-c1ccc(CC(C)C)cc1
CHEMBL62395 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
460 6 1 6 5.2 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1
CHEMBL322537 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
498 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1
CHEMBL430506 ednra_human Human No 9.3 IC50 = 0.5 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
447 7 1 6 4.3 CCOCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2
CHEMBL111277 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
578 14 1 7 4.6 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL65619 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
474 7 1 6 5.4 COc1ccc(CC2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1
CHEMBL321035 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
596 12 1 8 4.4 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccc(OC)cc1
CHEMBL65353 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
422 5 1 5 5.4 CC(C)Oc1ccc2c(c1)C(C1CCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2
CHEMBL323464 ednra_rat Rat No 9.3 IC50 = 0.5 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
564 13 1 7 4.2 CCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1
CHEMBL325581 ednra_human Human No 9.3 IC50 = 0.6 nM Funct
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.
584 13 1 7 4.1 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCCl
CHEMBL419367 ednra_rat Rat No 9.3 IC50 = 0.6 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F
CHEMBL22513 ednra_human Human No 9.3 IC50 = 0.6 nM Bind
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
549 8 2 8 3.4 CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12
CHEMBL22513 ednra_human Human No 9.3 IC50 = 0.6 nM Bind
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
549 8 2 8 3.4 CCOc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12
CHEMBL323561 ednra_human Human No 9.3 IC50 = 0.6 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
447 7 2 6 3.7 COc1ccc([C@@H]2c3nc(CCCO)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1
CHEMBL9139 ednra_human Human No 9.3 IC50 = 0.6 nM Bind
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
482 10 1 6 3.9 CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1
CHEMBL111612 ednra_rat Rat Yes 9.3 IC50 = 0.6 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
532 15 1 6 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC
CHEMBL113757 ednra_rat Rat No 9.3 IC50 = 0.6 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
549 10 1 9 4.8 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1
CHEMBL368796 ednra_rat Rat No 9.3 IC50 = 0.6 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
549 10 1 9 4.8 COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C)cc2)nc1
CHEMBL9313 ednra_rat Rat No 9.3 IC50 = 0.6 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
538 14 1 6 5.5 CCCCCN(CCCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1
CHEMBL419749 ednra_rat Rat No 9.2 IC50 = 0.6 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
560 14 1 7 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL66426 ednra_rat Rat No 9.2 IC50 = 0.6 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
450 6 1 5 6.1 CC(C)Oc1ccc2c(c1)C(CC1CCCCC1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2
CHEMBL110366 ednra_rat Rat No 9.2 IC50 = 0.6 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL103846 ednra_human Human No 9.2 IC50 = 0.6 nM Bind
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
677 13 1 12 5.2 CCOC(=O)C(NC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1)C(C)C
CHEMBL110366 ednra_rat Rat No 9.2 IC50 = 0.6 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL2373291 ednra_pig Pig No 9.2 IC50 = 0.6 nM Bind
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL111712 ednra_rat Rat No 9.2 IC50 = 0.6 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
590 16 1 8 4.5 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCOC)cc1
CHEMBL314691 ednra_human Human Yes 9.2 IC50 = 0.6 nM Funct
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 methodAntagonist 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
None None None None
CHEMBL64282 ednra_rat Rat No 9.2 IC50 = 0.6 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
438 9 1 5 6.1 CCCCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL417555 ednra_rat Rat No 9.2 IC50 = 0.6 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
396 5 1 5 4.8 CC(C)Oc1ccc2c(c1)C(C(C)C)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2
CHEMBL297783 ednra_human Human No 9.2 IC50 = 0.6 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
454 6 1 8 4.0 Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1noc(C)c1Cl)OCO2
CHEMBL277595 ednra_human Human No 9.2 IC50 = 0.6 nM Bind
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
439 5 2 6 4.7 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1
CHEMBL31544 ednra_human Human No 9.2 IC50 = 0.6 nM Bind
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
498 10 3 7 3.2 COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(=O)NCCO)c1-c1ccc(CC(C)C)cc1
CHEMBL323485 ednra_rat Rat No 9.2 IC50 = 0.6 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
484 13 1 5 4.8 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C1CC1
CHEMBL112162 ednra_pig Pig No 9.2 IC50 = 0.6 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
601 11 1 10 4.3 COc1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(C)cc2)cc1OC
CHEMBL111010 ednra_rat Rat No 9.2 IC50 = 0.7 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
588 13 1 8 4.3 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc2c(c1)OCCO2
CHEMBL3980643 ednra_human Human No 9.2 IC50 = 0.7 nM Funct
Agonist activity at ETA receptor in human SKNMC cells assessed as induction of Ca2+ mobilization by fluorimetric methodAgonist activity at ETA receptor in human SKNMC cells assessed as induction of Ca2+ mobilization by fluorimetric method
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O)[C@@H](C)CC
CHEMBL65599 ednra_rat Rat No 9.2 IC50 = 0.7 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
454 10 1 6 5.7 CCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL61711 ednra_human Human No 9.2 IC50 = 0.7 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
552 7 2 7 5.5 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)N(C)CC(C)(C)C)c1
CHEMBL1204990 ednra_human Human No 9.2 IC50 = 0.7 nM Bind
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
485 7 2 6 4.3 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3ccccc31)OCO2
CHEMBL121647 ednra_rat Rat No 9.2 IC50 = 0.7 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1
CHEMBL366441 ednra_rat Rat No 9.2 IC50 = 0.7 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1
CHEMBL2165332 ednra_human Human No 9.2 IC50 = 0.7 nM Bind
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
570 11 2 8 3.9 Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL121647 ednra_human Human No 9.2 IC50 = 0.7 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1
CHEMBL366441 ednra_human Human No 9.2 IC50 = 0.7 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
530 9 2 6 4.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)C(C)C)cc1
CHEMBL112685 ednra_rat Rat No 9.2 IC50 = 0.7 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
506 12 1 5 5.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3ccoc3c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL4463633 ednra_human Human No 9.2 IC50 = 0.7 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
616 12 3 9 2.6 O=C(O)CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1
CHEMBL4565926 ednra_human Human No 9.2 IC50 = 0.7 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
540 11 2 9 3.1 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Br)cc1
CHEMBL2165332 ednra_human Human No 9.2 IC50 = 0.7 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
570 11 2 8 3.9 Cc1ccc(-c2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL303484 ednra_human Human No 9.2 IC50 = 0.7 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
619 12 1 11 3.9 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN3CCOCC3)c2)cc1
CHEMBL72037 ednra_human Human No 9.2 IC50 = 0.7 nM Bind
Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cellsReceptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells
665 13 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1
CHEMBL2373292 ednra_pig Pig No 9.2 IC50 = 0.7 nM Bind
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)[C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL109778 ednra_rat Rat No 9.1 IC50 = 0.7 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
509 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1ccccn1
CHEMBL64832 ednra_rat Rat No 9.1 IC50 = 0.7 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
410 7 1 5 5.4 CCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL38000 ednra_human Human No 9.1 IC50 = 0.7 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
490 8 2 7 5.0 CCOc1cc(OC)ccc1[C@@H]1c2nc(NC(C)C)ccc2[C@H](c2ccc3c(c2)OCO3)[C@H]1C(=O)O
CHEMBL427748 ednra_pig Pig No 9.1 IC50 = 0.8 nM Bind
Tested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptorTested for the competitive binding versus [125I]- ET-1 determined in porcine cardiac ventricular membrane for Endothelin A receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H]2CSSC[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL338754 ednra_human Human No 9.1 IC50 = 0.8 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
524 12 1 4 5.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1
CHEMBL111934 ednra_pig Pig No 9.1 IC50 = 0.8 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
571 10 1 9 4.3 COc1ccc(S(=O)(=O)Nc2ncnc(OCCOc3ncc(Br)cn3)c2-c2ccc(C)cc2)cc1
CHEMBL413093 ednra_human Human No 9.1 IC50 = 0.8 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
468 6 1 6 4.7 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1
CHEMBL111218 ednra_rat Rat No 9.1 IC50 = 0.8 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
472 13 1 5 4.7 C/C=C/CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC
CHEMBL110899 ednra_rat Rat No 9.1 IC50 = 0.8 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
546 12 1 7 4.0 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC(C)C
CHEMBL128240 ednra_rat Rat No 9.1 IC50 = 0.8 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
492 11 1 4 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(C)cc1
CHEMBL323951 ednra_rat Rat No 9.1 IC50 = 0.8 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
500 13 1 5 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC
CHEMBL325935 ednra_rat Rat No 9.1 IC50 = 0.8 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
472 13 1 5 4.7 C/C=C\CC[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC
CHEMBL10847 ednra_human Human No 9.1 IC50 = 0.8 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
550 11 1 9 4.7 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C
CHEMBL1204671 ednra_human Human No 9.1 IC50 = 0.8 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
550 11 1 9 4.7 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1C
CHEMBL31763 ednra_human Human No 9.1 IC50 = 0.8 nM Bind
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
518 8 2 6 4.0 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccc(CC(C)C)cc1
CHEMBL4078537 ednra_human Human No 9.1 IC50 = 0.8 nM Bind
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
567 10 2 9 4.6 CCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2
CHEMBL320839 ednra_human Human No 9.1 IC50 = 0.8 nM Bind
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
589 11 1 10 4.8 C=CCNC(=O)OC1(c2ccc(OC)cc2)OC(=O)C(c2ccc3c(c2)OCO3)=C1Cc1cc(OC)c(OC)c(OC)c1
CHEMBL113611 ednra_rat Rat No 9.1 IC50 = 0.8 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
524 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL23261 ednra_human Human Yes 9.1 IC50 = 0.8 nM Bind
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
410 9 1 7 2.9 COC([C@@H](C(=O)O)Oc1nc(OC)cc(n1)OC)(c1ccccc1)c1ccccc1
CHEMBL2165338 ednra_human Human Yes 9.1 IC50 = 0.8 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
572 10 2 8 3.2 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1
CHEMBL287517 ednra_human Human No 9.1 IC50 = 0.8 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
552 9 2 7 6.2 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCc2ccccc2)c1
CHEMBL63067 ednra_rat Rat No 9.1 IC50 = 0.8 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
412 6 1 6 4.6 CC(C)OC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL86965 ednra_rat Rat No 9.1 IC50 = 0.8 nM Bind
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
502 7 2 7 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCC(C(=O)O)CC1
CHEMBL9283 ednra_rat Rat No 9.1 IC50 = 0.8 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
530 10 1 6 5.1 CCCCN(C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1)c1ccccc1
CHEMBL9334 ednra_human Human No 9.1 IC50 = 0.8 nM Bind
Radioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cellsRadioligand binding selectivity to human Endothelin A receptor in chinese hamster ovary cells
496 11 1 6 4.3 CCCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1
CHEMBL113611 ednra_rat Rat No 9.1 IC50 = 0.9 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
524 12 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL9502 ednra_rat Rat No 9.1 IC50 = 0.9 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
482 10 1 6 3.9 CCCCN(CC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1
CHEMBL326685 ednra_rat Rat No 9.1 IC50 = 0.9 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
500 14 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC/C=C(/C)CC
CHEMBL114933 ednra_pig Pig No 9.1 IC50 = 0.9 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
565 11 1 10 4.9 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncc(C)cn2)c1
CHEMBL37973 ednra_human Human No 9.1 IC50 = 0.9 nM Bind
Inhibitory activity against [125I]ET1 binding to human endothelin A receptorInhibitory activity against [125I]ET1 binding to human endothelin A receptor
518 9 2 7 5.7 COc1ccc([C@@H]2c3nc(NC(C)C)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)c(OCC(C)C)c1
CHEMBL128479 ednra_human Human No 9.1 IC50 = 0.9 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
540 12 1 5 5.4 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)c(F)c1
CHEMBL441277 ednra_pig Pig No 9.1 IC50 = 0.9 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
557 10 1 10 5.3 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2cccs2)nc1
CHEMBL10854 ednra_human Human No 9.1 IC50 = 0.9 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
550 9 1 10 4.2 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1C
CHEMBL129740 ednra_rat Rat No 9.0 IC50 = 0.9 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CC)cc1
CHEMBL321520 ednra_human Human No 9.0 IC50 = 0.9 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
447 7 1 6 4.6 CCCOc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2
CHEMBL62376 ednra_rat Rat No 9.0 IC50 = 1.0 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
456 10 2 7 4.3 CC(C)Oc1ccc2c(c1)C(OCCCCCO)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2
CHEMBL445101 ednra_human Human No 9.0 IC50 = 1.0 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
424 6 1 6 4.5 Cc1ccc(CC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C)c1
CHEMBL10922 ednra_human Human No 9.0 IC50 = 1.0 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
520 10 1 8 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C
CHEMBL1204674 ednra_human Human No 9.0 IC50 = 1.0 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
520 10 1 8 4.7 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1C
CHEMBL1180344 ednra_human Human No 9.0 IC50 = 1 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
516 9 2 6 4.5 CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1
CHEMBL123107 ednra_human Human No 9.0 IC50 = 1 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
516 9 2 6 4.5 CCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1
CHEMBL293012 ednra_rat Rat No 9.0 IC50 = 1 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
450 5 1 6 5.6 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1
CHEMBL322920 ednra_human Human No 9.0 IC50 = 1 nM Bind
Binding affinity for human Endothelin A receptor expressed in LtK- cellsBinding affinity for human Endothelin A receptor expressed in LtK- cells
703 11 1 10 7.5 COc1ccc(C2(OC(=O)N[C@@H](C)c3cccc4ccccc34)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1
CHEMBL307936 ednra_pig Pig No 9.0 IC50 = 1 nM Bind
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
585 12 5 5 3.6 CSCCC(NC(=O)[C@@H](Cc1c(C)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O
CHEMBL326191 ednra_rat Rat No 9.0 IC50 = 1 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL1111 ednra_human Human Yes 9.0 IC50 = 1 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
378 7 1 5 3.5 COC([C@@H](C(=O)O)Oc1nc(C)cc(n1)C)(c1ccccc1)c1ccccc1
CHEMBL293012 ednra_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
450 5 1 6 5.6 Cc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)s1
CHEMBL4448273 ednra_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
674 12 1 13 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)c1ccccn1
CHEMBL4542394 ednra_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
526 12 2 10 3.0 CCNS(=O)(=O)Nc1ncnc(OCCOc2cc(OC)ccc2Cl)c1-c1ncc(SC)cn1
CHEMBL4549357 ednra_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
656 14 2 13 4.2 COc1ccccc1Oc1c(NS(=O)(=O)CCc2cccs2)nc(N2CCOCC2)nc1OCCOC(=O)Nc1ccccn1
CHEMBL238539 ednra_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
508 8 1 7 5.2 CN(Cc1cc(-c2ncco2)ccc1-c1ccccc1S(=O)(=O)Nc1ccno1)C(=O)CC(C)(C)C
CHEMBL2165329 ednra_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
602 13 2 10 3.7 COc1cccc(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1
CHEMBL1205090 ednra_rat Rat No 9.0 IC50 = 1 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
554 10 1 9 5.3 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl
CHEMBL51234 ednra_rat Rat No 9.0 IC50 = 1 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
554 10 1 9 5.3 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1Cl
CHEMBL285976 ednra_human Human No 9.0 IC50 = 1 nM Bind
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
454 8 2 6 3.6 COc1nc(C)cnc1NS(=O)(=O)c1cccc(C(N)=O)c1-c1ccc(CC(C)C)cc1
CHEMBL286014 ednra_human Human No 9.0 IC50 = 1 nM Bind
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
546 8 1 6 4.6 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(C(=O)N(C)C)c1-c1ccc(CC(C)C)cc1
CHEMBL112134 ednra_pig Pig No 9.0 IC50 = 1 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
591 9 1 8 5.4 Cc1ccc(-c2c(NS(=O)(=O)c3ccc4ccccc4c3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL116220 ednra_pig Pig No 9.0 IC50 = 1 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
667 9 1 8 4.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(I)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL367453 ednra_human Human No 9.0 IC50 = 1 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1
CHEMBL94786 ednra_human Human No 9.0 IC50 = 1 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
689 12 2 13 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccn1
CHEMBL68269 ednra_human Human No 9.0 IC50 = 1 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
577 12 1 10 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OCCCN(C)C)c2)cc1
CHEMBL1790519 ednra_human Human No 9.0 IC50 = 1 nM Bind
Inhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cellsInhibition of binding to Endothelin A receptor of rabbit renal vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N(C)[C@@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC
CHEMBL308088 ednra_human Human No 9.0 IC50 = 1 nM Bind
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
681 13 2 13 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCSCC2)nc1OCCOC(=O)Nc1ccccn1
CHEMBL323951 ednra_human Human No 9.0 IC50 = 1 nM Bind
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
500 13 1 5 5.3 C/C=C\C(C)(C)C[C@H]1[C@H](C(=O)O)[C@@H](c2ccc3c(c2)OCO3)CN1CC(=O)N(CCCC)CCCC
CHEMBL114074 ednra_rat Rat No 9.0 IC50 = 1.1 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
527 13 1 7 4.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCc1nc(C)c(C)o1
CHEMBL128061 ednra_rat Rat No 9.0 IC50 = 1.1 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
522 13 1 5 5.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCC)cc1
CHEMBL322537 ednra_human Human No 9.0 IC50 = 1.1 nM Bind
Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)Tested for binding affinity for human Endothelin A receptor by measuring its ability to displace [125I]ET1 from chinese hamster ovary cells(CHO)
498 13 1 7 3.6 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCn1cccn1
CHEMBL329251 ednra_human Human No 9.0 IC50 = 1.1 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
544 7 2 6 4.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3F)c3ccccc32)n1
CHEMBL80782 ednra_human Human No 9.0 IC50 = 1.1 nM Bind
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
409 4 1 5 3.8 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1Br
CHEMBL4528664 ednra_human Human No 9.0 IC50 = 1.1 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
494 9 2 7 5.1 CCCc1nc(SC2CCC(CC(=O)O)CC2)c(C(=O)O)n1Cc1cc2c(cc1Cl)OCO2
CHEMBL22562 ednra_human Human No 9.0 IC50 = 1.1 nM Bind
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
535 7 2 8 3.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12
CHEMBL22562 ednra_human Human No 9.0 IC50 = 1.1 nM Bind
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
535 7 2 8 3.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(N)=O)ccc12
CHEMBL2163694 ednra_human Human Yes 9.0 IC50 = 1.1 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
585 11 1 8 4.5 CCCCS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1
CHEMBL2163704 ednra_human Human No 9.0 IC50 = 1.1 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
647 15 1 13 4.7 COc1ccccc1Oc1c(NS(=O)(=O)CCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(SC)cn1
CHEMBL313044 ednra_rat Rat No 9.0 IC50 = 1.1 nM Bind
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccsc2)nn1CC1CCCCC1
CHEMBL313153 ednra_rat Rat No 9.0 IC50 = 1.1 nM Bind
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
458 6 1 6 5.9 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCCC1
CHEMBL424358 ednra_pig Pig No 9.0 IC50 = 1.1 nM Bind
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
639 10 1 8 6.7 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)nc(C(C)C)nc2OCCOc2ncc(Br)cn2)cc1
CHEMBL10832 ednra_human Human No 9.0 IC50 = 1.1 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
506 10 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1
CHEMBL1204670 ednra_human Human No 9.0 IC50 = 1.1 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
506 10 1 8 4.4 COc1ccc(C(=O)/C(Cc2ccc(OC)c(OC)c2OC)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1
CHEMBL8981 ednra_human Human Yes 9.0 IC50 = 1.1 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)c(OC)c2)cc1
CHEMBL111769 ednra_rat Rat No 8.9 IC50 = 1.2 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
518 11 1 7 3.3 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CC
CHEMBL4061110 ednra_human Human No 8.9 IC50 = 1.2 nM Bind
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
581 11 2 9 5.0 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(-c3nnn[nH]3)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2
CHEMBL326191 ednra_rat Rat No 8.9 IC50 = 1.2 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
508 12 1 5 4.9 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL10697 ednra_human Human No 8.9 IC50 = 1.2 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
473 6 2 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(NC(C)=O)cc2)cc1
CHEMBL2163690 ednra_human Human No 8.9 IC50 = 1.2 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
542 11 2 8 3.5 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1
CHEMBL115230 ednra_pig Pig No 8.9 IC50 = 1.2 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
593 11 1 9 6.3 CSc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2-c2ccc(C(C)C)cc2)nc1
CHEMBL324246 ednra_pig Pig No 8.9 IC50 = 1.2 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
551 11 1 10 4.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ccncn2)c1
CHEMBL414165 ednra_human Human No 8.9 IC50 = 1.2 nM Bind
Inhibitory effect against Human ET-A receptorInhibitory effect against Human ET-A receptor
None None None CC(C)C[C@H]1NC(=O)[C@H](c2cccs2)NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O
CHEMBL9139 ednra_rat Rat No 8.9 IC50 = 1.2 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
482 10 1 6 3.9 CCCN(CCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1
CHEMBL32572 ednra_human Human No 8.9 IC50 = 1.3 nM Bind
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
532 8 2 6 4.3 CNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1
CHEMBL59288 ednra_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
492 6 2 8 5.0 Cc1cc(-c2ncco2)cc(C)c1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL435773 ednra_rat Rat No 8.9 IC50 = 1.3 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
462 6 1 6 5.2 COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1
CHEMBL324639 ednra_rat Rat No 8.9 IC50 = 1.3 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
592 15 1 7 5.0 CCCCCS(=O)(=O)N(CCC)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OCC)c(F)c1
CHEMBL435773 ednra_rat Rat No 8.9 IC50 = 1.3 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
462 6 1 6 5.2 COc1ccc([C@@H]2c3cc(OC(C)C)ccc3O[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1
CHEMBL320124 ednra_rat Rat No 8.9 IC50 = 1.3 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
486 13 1 5 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC=C(C)C
CHEMBL432974 ednra_rat Rat No 8.9 IC50 = 1.3 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC
CHEMBL113529 ednra_rat Rat No 8.9 IC50 = 1.3 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
496 13 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(OC)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL4573273 ednra_human Human No 8.9 IC50 = 1.3 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
496 11 2 9 3.0 CCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1
CHEMBL1204799 ednra_rat Rat Yes 8.9 IC50 = 1.3 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]
CHEMBL25438 ednra_rat Rat Yes 8.9 IC50 = 1.3 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
528 10 0 9 0.1 COc1ccc(cc1)C(=O)/C(=C(/c1ccc2c(c1)OCO2)\C(=O)[O-])/Cc1cc(OC)c(c(c1)OC)OC.[Na+]
CHEMBL312979 ednra_rat Rat No 8.9 IC50 = 1.3 nM Bind
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
442 6 1 6 5.4 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2ccco2)nn1CC1CCCCC1
CHEMBL88011 ednra_rat Rat No 8.9 IC50 = 1.3 nM Bind
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
502 7 2 7 5.2 O=C(O)c1c(Cc2cc3c(cc2Cl)OCO3)c(-c2cccs2)nn1CC1CCCC(C(=O)O)C1
CHEMBL295557 ednra_human Human No 8.9 IC50 = 1.3 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
506 6 1 10 4.1 CC#N.Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2cc3c(cc2C#N)OCO3)c1Cl
CHEMBL293421 ednra_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
535 7 2 7 6.1 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(=O)C2CCCCC2)c1
CHEMBL340190 ednra_rat Rat No 8.9 IC50 = 1.4 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
516 11 1 5 5.0 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(F)c(F)c1
CHEMBL108142 ednra_rat Rat No 8.9 IC50 = 1.4 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
566 11 1 7 4.4 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)c1ccccc1
CHEMBL115147 ednra_pig Pig No 8.9 IC50 = 1.4 nM Bind
Ability to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membraneAbility to inhibit [125I]ET1 binding to endothelin A receptor in porcine aortic membrane
627 11 2 9 4.6 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C(=O)O)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL431286 ednra_human Human No 8.9 IC50 = 1.4 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
560 7 2 6 4.8 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(F)cccc3Cl)c3ccccc32)n1
CHEMBL80857 ednra_human Human No 8.9 IC50 = 1.4 nM Bind
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2ccccc2-c2ccccc2)c1Br
CHEMBL268480 ednra_human Human No 8.9 IC50 = 1.4 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2)cc1
CHEMBL111611 ednra_rat Rat No 8.9 IC50 = 1.4 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
532 13 1 7 4.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)C1OCCO1
CHEMBL3989834 ednra_human Human Yes 8.9 IC50 = 1.4 nM Bind
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
479 8 1 9 3.9 COc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cn1)C)c1ccncc1
CHEMBL4456288 ednra_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
507 9 1 9 4.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OC
CHEMBL4519822 ednra_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
522 14 2 11 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1Oc1cccc(OC)c1
CHEMBL282724 ednra_human Human Yes 8.9 IC50 = 1.4 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C
CHEMBL2261599 ednra_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
534 7 1 8 4.1 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C(C)=O)ccc12
CHEMBL2163725 ednra_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
687 14 2 12 3.6 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(N2CCOCC2)nc1OCCOc1ncc(Br)cn1
CHEMBL2165330 ednra_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
636 13 2 10 4.4 COc1ccc(Cl)c(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1
CHEMBL2165333 ednra_human Human No 8.9 IC50 = 1.4 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
590 11 2 8 4.3 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Cl)cc1
CHEMBL1206680 ednra_rat Rat No 8.9 IC50 = 1.4 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
534 10 1 9 5.0 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C
CHEMBL295483 ednra_rat Rat No 8.9 IC50 = 1.4 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
534 10 1 9 5.0 COc1ccc(C(=O)/C(Cc2cc(OC)c(OC)c(OC)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1C
CHEMBL957 ednra_rat Rat Yes 8.9 IC50 = 1.4 nM Bind
In vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptorIn vitro for specific binding of [125I]ET1 to A10 cell expressed in endothelin A receptor
551 10 2 10 4.2 OCCOc1nc(nc(c1Oc1ccccc1OC)NS(=O)(=O)c1ccc(cc1)C(C)(C)C)c1ncccn1
CHEMBL115017 ednra_pig Pig No 8.9 IC50 = 1.4 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
609 9 1 8 5.3 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(F)(F)F)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1
CHEMBL282724 ednra_human Human Yes 8.9 IC50 = 1.4 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C
CHEMBL282724 ednra_human Human Yes 8.9 IC50 = 1.4 nM Bind
Inhibitory concentration towards Endothelin A receptor in humanInhibitory concentration towards Endothelin A receptor in human
454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C
CHEMBL282724 ednra_human Human Yes 8.9 IC50 = 1.4 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
454 6 1 8 4.0 O=C(c1sccc1S(=O)(=O)Nc1onc(c1Cl)C)Cc1cc2OCOc2cc1C
CHEMBL1271586 ednra_human Human No 8.8 IC50 = 1.4 nM Bind
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
557 11 2 7 5.5 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2
CHEMBL58058 ednra_human Human No 8.8 IC50 = 1.5 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
501 6 2 6 6.0 Cc1cc(C)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(-c2ccccc2)c1
CHEMBL419211 ednra_rat Rat No 8.8 IC50 = 1.5 nM Bind
Binding affinity against endothelin A receptor in MMQ cells in ratBinding affinity against endothelin A receptor in MMQ cells in rat
506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL62669 ednra_rat Rat No 8.8 IC50 = 1.5 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
412 7 1 6 4.6 CCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL113400 ednra_rat Rat No 8.8 IC50 = 1.5 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
502 12 1 4 5.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)c(F)c2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL419211 ednra_rat Rat No 8.8 IC50 = 1.5 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
506 12 1 4 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)CCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL4436531 ednra_human Human No 8.8 IC50 = 1.5 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
510 12 2 9 3.4 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(SC)cn2)c1-c1ccc(Cl)cc1
CHEMBL2163708 ednra_human Human No 8.8 IC50 = 1.5 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
707 12 1 12 5.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1
CHEMBL9194 ednra_rat Rat Yes 8.8 IC50 = 1.5 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
510 12 1 6 4.7 CCCCN(C(=O)CN1C[C@@H]([C@H]([C@@H]1c1ccc(cc1)OC)C(=O)O)c1ccc2c(c1)OCO2)CCCC
CHEMBL31592 ednra_human Human No 8.8 IC50 = 1.6 nM Bind
In vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptorsIn vitro binding was measured by the displacement of [125I]ET1 from membranes prepared from MEL cells transfected with cloned human ETA receptors
576 11 2 7 4.3 COCCNC(=O)c1cccc(S(=O)(=O)Nc2ncc(Br)nc2OC)c1-c1ccc(CC(C)C)cc1
CHEMBL326861 ednra_rat Rat No 8.8 IC50 = 1.6 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
532 12 1 7 3.7 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)CCC
CHEMBL1184133 ednra_human Human No 8.8 IC50 = 1.6 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
544 11 2 6 5.3 CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1
CHEMBL334076 ednra_human Human No 8.8 IC50 = 1.6 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
544 11 2 6 5.3 CCCCC(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1
CHEMBL62465 ednra_rat Rat No 8.8 IC50 = 1.6 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
460 6 1 6 5.2 COc1cccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)c1
CHEMBL4590018 ednra_rat Rat No 8.8 IC50 = 1.6 nM Bind
Displacement of 125I-ET1 from ETA receptor in rat A7R5 cellsDisplacement of 125I-ET1 from ETA receptor in rat A7R5 cells
521 11 2 10 3.5 COc1ccccc1Oc1c(NS(=O)(=O)/C=C/c2ccccc2)nc(-c2ncccn2)nc1OCCO
CHEMBL241460 ednra_human Human No 8.8 IC50 = 1.6 nM Bind
Displacement of [125I]ET1 from human ETA receptor expressed in CHO cellsDisplacement of [125I]ET1 from human ETA receptor expressed in CHO cells
859 27 2 14 5.3 CC(=O)CC(=O)CCc1ccc(NC(=O)CCOCCOCCOCCOCC(=O)N(C)Cc2cc(-c3ncco3)ccc2-c2ccccc2S(=O)(=O)Nc2ccno2)cc1
CHEMBL2165334 ednra_human Human Yes 8.8 IC50 = 1.6 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
634 11 2 8 4.4 O=S(=O)(NCc1ccccc1)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1
CHEMBL168904 ednra_pig Pig No 8.8 IC50 = 1.6 nM Bind
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
639 11 1 8 6.5 CCCc1nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c(-c2ccc(C)cc2)c(OCCOc2ncc(Br)cn2)n1
CHEMBL430695 ednra_human Human No 8.8 IC50 = 1.6 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
429 5 1 5 4.7 COc1ccc([C@@H]2c3nc(C4CC4)ccc3[C@H](c3ccc4c(c3)OCO4)[C@H]2C(=O)O)cc1
CHEMBL419367 ednra_human Human No 8.8 IC50 = 1.7 nM Funct
Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.Ability to block the ET-1-induced hydrolysis of inositol phosphate in Endothelin A receptor of MMQ cells.
618 13 1 7 4.8 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)c(F)c1)S(=O)(=O)CCCC(F)(F)F
CHEMBL412706 ednra_pig Pig No 8.8 IC50 = 1.7 nM Funct
Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes
None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL274359 ednra_human Human No 8.8 IC50 = 1.7 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)cc(OC)c2)cc1
CHEMBL109648 ednra_human Human Yes 8.8 IC50 = 1.7 nM Bind
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cellsDisplacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
577 11 3 13 2.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(-c2ccnc(-c3nn[nH]n3)c2)nc1OCCO
CHEMBL2261357 ednra_human Human No 8.8 IC50 = 1.7 nM Bind
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
549 8 3 8 2.3 Cn1cc(C(C(=O)NS(=O)(=O)c2ccc(CC(=O)O)cc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21
CHEMBL2163720 ednra_human Human No 8.8 IC50 = 1.7 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
646 15 2 12 3.8 CCCCNS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC
CHEMBL2165337 ednra_human Human Yes 8.8 IC50 = 1.7 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
558 9 2 8 2.8 CNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1
CHEMBL175129 ednra_rat Rat No 8.7 IC50 = 1.8 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
446 8 1 6 4.4 COc1ccc(C/C(C(=O)c2ccc(OC)cc2)=C(/C(=O)O)c2ccc3c(c2)OCO3)cc1
CHEMBL330104 ednra_human Human No 8.7 IC50 = 1.8 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
576 7 2 6 5.3 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)n1
CHEMBL11115 ednra_human Human No 8.7 IC50 = 1.8 nM Funct
Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK
446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1
CHEMBL11115 ednra_human Human No 8.7 IC50 = 1.8 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
446 6 1 7 3.8 COc1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1
CHEMBL275701 ednra_human Human No 8.7 IC50 = 1.8 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c(OC)cc2OC)cc1
CHEMBL62578 ednra_rat Rat No 8.7 IC50 = 1.8 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
537 7 1 8 4.2 COc1ccc(C2=C(C(=O)NS(C)(=O)=O)C(c3ccc4c(c3)OCO4)Oc3ccc(OC(C)C)cc32)cc1
CHEMBL63057 ednra_rat Rat No 8.7 IC50 = 1.8 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
426 8 1 6 4.6 COCCCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL320569 ednra_rat Rat No 8.7 IC50 = 1.8 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
516 13 1 6 4.7 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCCO1
CHEMBL2304015 ednra_pig Pig No 8.7 IC50 = 1.8 nM Bind
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
None None None Cc1[nH]c2ccccc2c1C[C@@H]1NC(=O)[C@@H](C2CC2)NC(=O)[C@H](C2CCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC1=O
CHEMBL278109 ednra_human Human No 8.7 IC50 = 1.8 nM Bind
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
505 6 2 7 3.0 Cc1ccc(S(=O)(=O)NC(=O)C(c2ccc3c(c2)OCO3)c2cn(C)c3cc(C(N)=O)ccc23)cc1
CHEMBL414605 ednra_human Human No 8.7 IC50 = 1.8 nM Bind
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
550 10 4 5 4.7 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N(C)C2CCCCC2)nc1C(=O)O
CHEMBL1271586 ednra_human Human No 8.7 IC50 = 1.9 nM Bind
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
557 11 2 7 5.5 CCCCOc1ccc2c(c1)c(=O)c(Cc1cccc(C(=O)O)c1)c(C(=O)O)n2Cc1cc2c(cc1CC)OCO2
CHEMBL9119 ednra_rat Rat No 8.7 IC50 = 1.9 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
468 8 1 6 3.4 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)C)cc1
CHEMBL2163716 ednra_human Human No 8.7 IC50 = 1.9 nM Bind
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1
CHEMBL63058 ednra_rat Rat No 8.7 IC50 = 1.9 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
424 7 1 5 5.6 CC(C)CCC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL305524 ednra_pig Pig No 8.7 IC50 = 1.9 nM Bind
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
665 13 5 5 4.7 CCSCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O
CHEMBL2163691 ednra_human Human No 8.7 IC50 = 1.9 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
554 13 2 10 2.9 CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1Oc1cccc(OC)c1
CHEMBL2163716 ednra_human Human No 8.7 IC50 = 1.9 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
680 14 2 12 4.2 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1
CHEMBL114201 ednra_pig Pig No 8.7 IC50 = 1.9 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
551 11 1 10 4.6 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2ncccn2)c1
CHEMBL175931 ednra_pig Pig No 8.7 IC50 = 1.9 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
759 9 1 9 8.1 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(Cl)cc3)ncnc2OCCOc2ncc(Br)cn2)cc1.O=C1C2=C(CCCC2)c2ccccc21
CHEMBL320208 ednra_human Human No 8.7 IC50 = 1.9 nM Bind
Inhibitory activity against I-labeled ET-1 binding to Endothelin A receptorInhibitory activity against I-labeled ET-1 binding to Endothelin A receptor
459 8 1 5 5.5 CCCCCc1ccc2c(n1)[C@@H](c1ccc(OC)cc1)[C@H](C(=O)O)[C@H]2c1ccc2c(c1)OCO2
CHEMBL109408 ednra_rat Rat No 8.0 IC50 = 10 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
580 12 1 7 4.5 CCCN(CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)S(=O)(=O)Cc1ccccc1
CHEMBL111728 ednra_rat Rat No 8.0 IC50 = 10 nM Bind
Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
504 10 1 7 2.9 CCCS(=O)(=O)N(C)CCN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL2058375 ednra_human Human No 8.0 IC50 = 10 nM Funct
Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells
532 9 1 6 6.6 CCCCc1nc2ccc(F)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1
CHEMBL2058376 ednra_human Human No 8.0 IC50 = 10 nM Funct
Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells
582 9 1 6 7.5 CCCCc1nc2ccc(C(F)(F)F)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1
CHEMBL10843 ednra_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
408 5 1 6 4.2 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCC2)cc1
CHEMBL10860 ednra_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
467 5 1 7 4.4 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2nccc3ccccc23)cc1
CHEMBL109474 ednra_rat Rat No 8.0 IC50 = 10 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
516 13 1 6 4.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCOCC1
CHEMBL420729 ednra_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
558 10 2 6 5.6 CCc1cc(CC)c(NC(=O)CN2C[C@H](c3ccc4c(c3)OCO4)[C@@H](C(=O)O)[C@@H]2c2ccc(OC)cc2)c(CC)c1
CHEMBL4579445 ednra_human Human No 8.0 IC50 = 10 nM Bind
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
704 13 2 11 5.2 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)cc(C(=O)N2CCN(C)CC2)cc1OCCOC(=O)Nc1ccccn1
CHEMBL3735931 ednra_human Human No 8.0 IC50 = 10 nM Bind
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
647 11 2 7 7.3 CCCc1nc2c(C)cc(C(=O)NCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1
CHEMBL3753406 ednra_human Human No 8.0 IC50 = 10 nM Bind
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
584 10 3 7 5.7 CCCc1nc2c(C)cc(C(=O)NCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1
CHEMBL352775 ednra_pig Pig No 8.0 IC50 = 10 nM Bind
In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
733 15 2 12 6.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(SCCC(=O)O)nc1OCCOc1ncc(Br)cn1
CHEMBL283535 ednra_human Human No 8.0 IC50 = 10 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
483 6 2 9 3.7 CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2
CHEMBL45160 ednra_human Human No 8.0 IC50 = 10 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
483 6 2 9 3.7 CC(=O)c1c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)ccc2c1OCO2
CHEMBL273660 ednra_human Human No 8.0 IC50 = 10 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1
CHEMBL369085 ednra_human Human No 8.0 IC50 = 10 nM Bind
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cellsInhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2cc(OC)c3c(c2)OCO3)cc1
CHEMBL65939 ednra_human Human No 8.0 IC50 = 10 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
529 9 1 8 4.3 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCN3CCCC3)c2)cc1
CHEMBL6412 ednra_human Human No 8.0 IC50 = 10 nM Bind
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
392 5 1 6 3.2 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc2c(N(C)C)cccc12
CHEMBL283535 ednra_human Human No 8.0 IC50 = 10 nM Bind
Inhibitory concentration was determined against selective Endothelin A receptorInhibitory concentration was determined against selective Endothelin A receptor
483 6 2 9 3.7 CC(=O)c1cc2c(cc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2
CHEMBL316629 ednra_human Human No 8.0 IC50 = 10.2 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
568 9 2 8 4.0 COc1ccc(CN2C(=O)CN[C@](c3cccc(OC)c3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1
CHEMBL96472 ednra_human Human No 8.0 IC50 = 10.2 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
542 7 2 6 4.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3Cl)c3ccccc32)n1
CHEMBL2163709 ednra_human Human No 8.0 IC50 = 10.4 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
651 12 1 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccccc2)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1
CHEMBL297215 ednra_human Human No 8.0 IC50 = 10.8 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
500 8 3 9 2.9 COc1cc(OC)c(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)c(C(N)=O)c1
CHEMBL283598 ednra_human Human No 7.0 IC50 = 100 nM Bind
Affinity for human endothelin A receptor expressed in Ltk cells.Affinity for human endothelin A receptor expressed in Ltk cells.
491 5 1 9 4.7 O=C(O)c1c(Sc2ccc3c(c2)OCO3)c2cc3c(cc2n1Cc1ccc2c(c1)OCO2)OCO3
CHEMBL1180336 ednra_human Human No 7.0 IC50 = 100 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
620 11 2 6 6.3 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC
CHEMBL122673 ednra_human Human No 7.0 IC50 = 100 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
620 11 2 6 6.3 CCc1ccccc1C(NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1)c1ccccc1CC
CHEMBL94907 ednra_human Human No 7.0 IC50 = 100 nM Bind
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
None None None CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL2304010 ednra_pig Pig No 7.0 IC50 = 100 nM Bind
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
None None None CSC(C)(C)[C@@H]1NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc2c(Cl)[nH]c3ccccc23)NC(=O)[C@@H](C(C)C)NC1=O
CHEMBL435185 ednra_human Human No 7.0 IC50 = 100 nM Bind
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
530 8 2 6 5.3 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)Nc2c(C)cccc2C(C)C)cc1
CHEMBL281121 ednra_human Human No 7.0 IC50 = 100 nM Bind
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
548 7 1 8 4.5 COC(=O)c1ccc2c(C(C(=O)NS(=O)(=O)c3ccc(C(C)C)cc3)c3ccc4c(c3)OCO4)cn(C)c2c1
CHEMBL27732 ednra_human Human No 7.0 IC50 = 100 nM Funct
Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.Inhibition of ET- 1 stimulated arachidonic acid release (AAR) in cultured rabbit renal vascular smooth muscle cells expressing the endothelin A receptor.
507 7 1 9 5.0 COc1cc2c(Sc3ccc4c(c3)OCO4)c(C(=O)O)n(Cc3ccc4c(c3)OCO4)c2cc1OC
CHEMBL89688 ednra_human Human No 7.0 IC50 = 100.2 nM Bind
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
426 4 1 5 4.9 Cc1ccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1
CHEMBL26522 ednra_rat Rat Yes 6.0 IC50 = 1000 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
270 3 1 4 2.2 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1C
CHEMBL315047 ednra_human Human No 6.0 IC50 = 1000 nM Bind
Binding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cellsBinding affinity against ET A receptor from rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL323331 ednra_human Human No 6.0 IC50 = 1000 nM Bind
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
937 26 9 8 4.6 CCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(c1ccccc1)c1ccccc1
CHEMBL318020 ednra_human Human No 6.0 IC50 = 1000 nM Bind
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL77090 ednra_human Human Yes 6.0 IC50 = 1000 nM Bind
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
266 3 1 4 2.4 Cc1ccccc1S(=O)(=O)Nc1onc(C)c1C
CHEMBL328964 ednra_rat Rat No 6.0 IC50 = 1000 nM Bind
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
374 9 1 3 5.1 O=C(O)CCC(C(=O)c1cccc(OCc2ccccc2)c1)c1ccccc1
CHEMBL324304 ednra_human Human No 6.0 IC50 = 1000 nM Bind
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
441 7 2 6 3.9 Cc1ccc(-c2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCO)cc1
CHEMBL327247 ednra_rat Rat Yes 6.0 IC50 = 1000 nM Bind
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
400 8 2 4 4.9 O=C(O)c1cc(-c2ccc(OCc3ccccc3)cc2OCc2ccccc2)[nH]n1
CHEMBL315047 ednra_human Human No 6.0 IC50 = 1000 nM Bind
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL6399 ednra_human Human No 6.0 IC50 = 1000 nM Bind
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
328 4 1 5 2.5 CN(C)c1cccc2c(S(=O)(=O)Nc3cnccn3)cccc12
CHEMBL176430 ednra_rat Rat No 6.0 IC50 = 1000 nM Bind
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
496 11 5 4 3.8 CCN(CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C)[nH]1
CHEMBL356916 ednra_pig Pig No 5.0 IC50 = 10000 nM Bind
Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.Ability to bind with Endothelin A receptor competitively in the presence of (125 I) endothelin using receptor binding assay.
498 9 2 5 4.6 COc1ccc(CN(C(=O)/C=C/c2ccc3c(c2)OCO3)C(Cc2c[nH]c3ccccc23)C(=O)O)cc1
CHEMBL281427 ednra_rat Rat No 5.0 IC50 = 10000 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3ccc(N)cc3c2)c1C
CHEMBL262229 ednra_human Human No 5.0 IC50 = 10000 nM Bind
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
966 25 9 8 5.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)C(C)(C)C)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL78601 ednra_human Human No 5.0 IC50 = 10000 nM Bind
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
286 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccc(Cl)cc2)c1C
CHEMBL100795 ednra_human Human No 5.0 IC50 = 10000 nM Funct
Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.
343 3 1 4 4.2 OCC(c1ccc2c(c1)OCO2)c1c2ccccc2nc2ccccc12
CHEMBL3751994 ednra_human Human No 5.0 IC50 = 10000 nM Bind
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
644 12 3 9 5.7 CCCc1nc2c(C)cc(C(=O)NCc3ccc(OC)c(OC)c3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1
CHEMBL469424 ednra_rat Rat Yes 5.0 IC50 = 10000 nM Bind
Displacement of endothelin-1 from ETA receptor in rat A10 cellsDisplacement of endothelin-1 from ETA receptor in rat A10 cells
348 5 3 7 2.7 COC(=O)c1cc(O)cc(OC)c1Oc1cc(C)cc(O)c1C(=O)O
CHEMBL4455096 ednra_human Human No 5.0 IC50 = 10000 nM Bind
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
439 7 2 6 3.6 O=S(=O)(Nc1ncnc(OCCO)c1-c1ccc(Cl)cc1)c1ccc(Cl)cc1
CHEMBL3144803 ednra_rat Rat No 5.0 IC50 = 10000 nM Bind
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
430 5 1 3 5.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3ccc(Cl)c(Cl)c3)c2=O)c1
CHEMBL3144845 ednra_rat Rat No 5.0 IC50 = 10000 nM Bind
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
376 4 1 4 3.6 O=c1c(Cc2ccc3c(c2)OCO3)c(C(F)(F)F)[nH]n1Cc1ccccc1
CHEMBL281427 ednra_rat Rat No 5.0 IC50 = 10000 nM Bind
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
317 3 2 5 2.8 Cc1noc(NS(=O)(=O)c2ccc3ccc(N)cc3c2)c1C
CHEMBL6566 ednra_human Human Yes 5.0 IC50 = 10000 nM Bind
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
419 4 1 4 4.2 Cc1nc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)ccc1Br
CHEMBL273488 ednra_human Human No 5.0 IC50 = 10000 nM Bind
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
391 3 1 4 5.4 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(Cl)ccc2n1-c1ccccc1
CHEMBL96325 ednra_human Human No 7.0 IC50 = 101 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
580 7 2 4 6.6 O=C(O)[C@@H](Oc1cccc(Cl)c1)[C@@]1(c2ccccc2)NCC(=O)N(Cc2c(Cl)cccc2Cl)c2ccccc21
CHEMBL94446 ednra_human Human No 7.0 IC50 = 102 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
584 8 2 6 5.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)n1
CHEMBL173189 ednra_human Human No 7.0 IC50 = 102 nM Bind
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
454 6 1 5 5.0 Cc1ccc(CCc2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c(C)c1
CHEMBL434983 ednra_human Human No 5.0 IC50 = 10210 nM Bind
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
366 4 2 6 2.3 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1Br
CHEMBL4078297 ednra_human Human No 6.0 IC50 = 1024 nM Bind
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
583 10 2 7 5.9 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CCCC4)ccc31)OCO2
CHEMBL96506 ednra_human Human No 7.0 IC50 = 104 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
576 7 2 6 5.0 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccccc3C(F)(F)F)c3ccccc32)n1
CHEMBL48031 ednra_human Human No 7.0 IC50 = 104 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
455 5 2 6 4.2 Cc1cccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1
CHEMBL172666 ednra_human Human No 7.0 IC50 = 104 nM Bind
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
514 8 1 8 4.9 CCCc1cc2c(cc1OCc1sccc1S(=O)(=O)Nc1onc(C)c1Br)OCO2
CHEMBL175268 ednra_human Human No 6.0 IC50 = 1050 nM Bind
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
653 14 2 10 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(C2CC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1
CHEMBL9040 ednra_rat Rat No 7.0 IC50 = 106 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
450 7 1 6 2.4 C#CCN(C)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1
CHEMBL174086 ednra_human Human No 7.0 IC50 = 106 nM Bind
Inhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assayInhibitory of human Endothelin A receptor by using I-ET-1 as radioligand in a competitive radioligand assay
440 6 1 5 4.7 Cc1ccc(CCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1
CHEMBL67664 ednra_human Human Yes 6.0 IC50 = 1060 nM Bind
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
322 4 2 6 2.2 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)O)c1Cl
CHEMBL275306 ednra_rat Rat No 7.0 IC50 = 108 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
427 9 1 6 3.7 CCCOCCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1
CHEMBL8776 ednra_rat Rat No 6.0 IC50 = 1080 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
454 4 1 6 2.7 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2C(=O)N2CCOCC2)cc1
CHEMBL63169 ednra_human Human Yes 6.0 IC50 = 1090 nM Bind
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
336 4 1 7 2.3 COC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL176696 ednra_rat Rat No 8.0 IC50 = 11 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
446 8 1 6 4.4 COc1ccc(C(=O)/C(Cc2ccccc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1OC
CHEMBL386778 ednra_pig Pig No 8.0 IC50 = 11 nM Funct
Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL405337 ednra_pig Pig No 8.0 IC50 = 11 nM Funct
Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL405916 ednra_pig Pig No 8.0 IC50 = 11 nM Funct
Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL409180 ednra_pig Pig No 8.0 IC50 = 11 nM Funct
Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL3601500 ednra_rat Rat Yes 8.0 IC50 = 11 nM Funct
Antagonist activity at endothelin A receptor in rat A7r5 cells assessed as inhibition of ET-1-induced increase in cytosolic free Ca2+ level treated 1 min prior to ET-1 addition by fura-2 dye-based spectrofluorometric analysisAntagonist activity at endothelin A receptor in rat A7r5 cells assessed as inhibition of ET-1-induced increase in cytosolic free Ca2+ level treated 1 min prior to ET-1 addition by fura-2 dye-based spectrofluorometric analysis
632 5 3 6 8.1 CC1(C)CC[C@]2(C(=O)O)CC[C@]3(COC(=O)/C=C/c4ccc(O)c(O)c4)C(=CC[C@@H]4[C@@]5(C)CCC(=O)C(C)(C)[C@@H]5CC[C@]43C)[C@@H]2C1
CHEMBL2058377 ednra_human Human No 8.0 IC50 = 11 nM Funct
Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cellsAntagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells
559 10 1 8 6.4 CCCCc1nc2ccc([N+](=O)[O-])cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1
CHEMBL96422 ednra_human Human No 8.0 IC50 = 11 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
592 8 2 7 4.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cccc(OC(F)(F)F)c3)c3ccccc32)n1
CHEMBL10846 ednra_human Human No 8.0 IC50 = 11 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1OC
CHEMBL276252 ednra_human Human No 8.0 IC50 = 11 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
476 7 1 8 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OC)c2OC)cc1
CHEMBL417428 ednra_human Human No 8.0 IC50 = 11 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
474 6 1 8 3.6 COC(=O)c1ccc(CC2=C(c3ccc4c(c3)OCO4)C(=O)OC2(O)c2ccc(OC)cc2)cc1
CHEMBL3736242 ednra_human Human No 8.0 IC50 = 11 nM Bind
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
591 10 1 8 6.2 CCCCc1nn(-c2ccccc2Cl)c(=O)n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1
CHEMBL2261600 ednra_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
517 6 1 8 3.7 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(C#N)ccc12
CHEMBL315087 ednra_rat Rat No 8.0 IC50 = 11 nM Bind
In vitro binding affinity to endothelin A receptor in rat heart ventriclesIn vitro binding affinity to endothelin A receptor in rat heart ventricles
490 7 2 6 5.0 O=C(O)c1ccc(Cn2nc(-c3ccccc3)c(Cc3cc4c(cc3Cl)OCO4)c2C(=O)O)cc1
CHEMBL176963 ednra_human Human No 8.0 IC50 = 11 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
533 10 2 10 3.3 C#CCOc1nc(-c2ccnc(CO)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC
CHEMBL174448 ednra_rat Rat No 8.0 IC50 = 11 nM Bind
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
536 10 5 5 4.4 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O
CHEMBL174448 ednra_human Human No 8.0 IC50 = 11 nM Bind
Inhibitory activity was evaluated against human Endothelin A receptorInhibitory activity was evaluated against human Endothelin A receptor
536 10 5 5 4.4 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)nc1C(=O)O
CHEMBL94766 ednra_human Human No 7.9 IC50 = 11.8 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
562 7 2 6 4.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3cc(F)c(F)c(F)c3)c3ccccc32)n1
CHEMBL366442 ednra_rat Rat No 7.0 IC50 = 110 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
450 7 1 5 5.0 COc1ccc(C(=O)/C(Cc2ccc(Cl)cc2)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1
CHEMBL64244 ednra_rat Rat No 7.0 IC50 = 110 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
444 5 1 5 5.6 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1
CHEMBL10733 ednra_human Human No 7.0 IC50 = 110 nM Funct
Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK
450 5 1 6 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1
CHEMBL302776 ednra_pig Pig No 7.0 IC50 = 110 nM Bind
Binding activity against Endothelin A receptor of Porcine aortic smooth muscle membranesBinding activity against Endothelin A receptor of Porcine aortic smooth muscle membranes
None None None CC(C)C[C@@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O
CHEMBL80980 ednra_human Human No 7.0 IC50 = 110 nM Bind
Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
366 3 1 4 3.7 Cc1noc(NS(=O)(=O)c2cccc3ccccc23)c1Br
CHEMBL309397 ednra_human Human No 7.0 IC50 = 110 nM Bind
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
384 3 1 4 3.9 Cc1noc(NS(=O)(=O)c2cc(Cl)ccc2Cl)c1Br
CHEMBL80342 ednra_human Human No 7.0 IC50 = 110 nM Bind
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
436 5 1 4 4.3 CCCc1ccc(Br)cc1S(=O)(=O)Nc1onc(C)c1Br
CHEMBL10733 ednra_human Human No 7.0 IC50 = 110 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
450 5 1 6 4.5 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(Cl)cc2)cc1
CHEMBL64244 ednra_rat Rat No 7.0 IC50 = 110 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
444 5 1 5 5.6 COc1ccc(C2=C(C(=O)O)C(c3ccc4c(c3)OCO4)Oc3ccc(C(C)C)cc32)cc1
CHEMBL1744023 ednra_pig Pig No 7.0 IC50 = 110 nM Bind
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
675 15 5 4 5.9 CCCCCC[C@@H](NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(CC(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O
CHEMBL417903 ednra_human Human No 7.0 IC50 = 110 nM Bind
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
521 10 2 8 3.9 CCOc1ccc2c(c1)[C@H](c1cccc(OC)c1OCC(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2
CHEMBL421365 ednra_rat Rat No 7.0 IC50 = 110 nM Bind
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
394 9 1 4 5.5 Cc1ccccc1C(CCC(=O)O)C(=O)c1cccc(OCc2ccsc2)c1
CHEMBL3144737 ednra_rat Rat No 7.0 IC50 = 110 nM Bind
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
456 6 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)C(F)(F)F)c(Cc3ccc4c(c3)OCO4)c2=O)c1
CHEMBL173826 ednra_rat Rat No 7.0 IC50 = 110 nM Bind
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
552 10 6 6 3.3 Cc1[nH]c([C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)NC2CCC(O)CC2)nc1C(=O)O
CHEMBL335143 ednra_pig Pig No 7.0 IC50 = 110 nM Bind
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O
CHEMBL352929 ednra_human Human No 6.0 IC50 = 1100 nM Bind
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
596 11 4 7 3.7 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1cn(C)c2ccccc12)C(=O)NCc1nc(C(=O)O)cs1
CHEMBL94689 ednra_human Human No 6.0 IC50 = 1100 nM Bind
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
918 24 9 8 4.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c(C)c(C)c(C)c(C)c1C)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL327861 ednra_rat Rat No 6.0 IC50 = 1100 nM Bind
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
391 7 1 5 4.8 COc1cccc(/C(=C\c2cc(OCc3ccsc3)ccc2C#N)C(=O)O)c1
CHEMBL52110 ednra_human Human No 6.0 IC50 = 1100 nM Bind
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
507 9 1 8 4.4 CCOc1ccc2c(c1)[C@H](c1cc(OC)c(OC)c(OC)c1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2
CHEMBL1178832 ednra_human Human No 6.0 IC50 = 1100 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
455 6 2 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl
CHEMBL45351 ednra_human Human No 6.0 IC50 = 1100 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
455 6 2 9 3.6 Cc1noc(NS(=O)(=O)c2ccsc2/C(Cc2ccc3c(c2)OCO3)=N\O)c1Cl
CHEMBL274370 ednra_human Human No 6.0 IC50 = 1100 nM Bind
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
417 5 1 6 4.7 COc1ccc(-c2c(C(=O)O)n(-c3ccc4c(c3)OCO4)c3ccc(OC)cc23)cc1
CHEMBL74118 ednra_human Human No 6.0 IC50 = 1100 nM Bind
Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cellsReceptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
581 11 1 10 5.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C)nc1OCCOC(=O)c1ccoc1
CHEMBL2296888 ednra_human Human Yes 5.0 IC50 = 11000 nM Bind
Antagonist activity at ETA receptor (unknown origin)Antagonist activity at ETA receptor (unknown origin)
206 2 1 3 2.4 COc1cccc2oc(C(=O)O)c(C)c12
CHEMBL269428 ednra_human Human No 5.0 IC50 = 11000 nM Bind
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)C(c1ccccc1)(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL331066 ednra_human Human No 5.0 IC50 = 11000 nM Bind
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
558 11 2 6 5.2 CCc1cccc(CC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(CCOC)cc1
CHEMBL3753277 ednra_human Human No 5.0 IC50 = 11000 nM Bind
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
616 11 3 7 5.9 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3F)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1
CHEMBL298976 ednra_rat Rat Yes 5.0 IC50 = 11000 nM Bind
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
379 3 2 5 2.0 Cc1onc(NS(=O)(=O)c2ccc(N)cc2)c1I
CHEMBL435894 ednra_rat Rat No 5.0 IC50 = 11000 nM Bind
Inhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranesInhibition of Endothelin-1 binding to Endothelin A receptor binding sites in MMQ cell membranes
567 10 4 5 5.8 CC(C)C[C@H](NC(=O)N1CCCCCC1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)c1nc(C(=O)O)c(C(C)C)s1
CHEMBL102494 ednra_human Human No 5.0 IC50 = 11000 nM Bind
Inhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cellsInhibition of binding of [125I]ET1 to cloned human Endothelin A receptor expressed in LtK- cells
375 3 0 5 4.1 COC(=O)C(c1ccc2c(c1)OCO2)c1c2c(nc3ccccc13)CCCC2
CHEMBL15689 ednra_human Human No 5.0 IC50 = 11000 nM Bind
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
457 9 1 5 5.8 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)ccc1OC(C(=O)O)c1ccccc1
CHEMBL276819 ednra_human Human No 5.0 IC50 = 11000 nM Bind
Inhibition of human endothelin A (ETA) receptor expressed in CHO cellsInhibition of human endothelin A (ETA) receptor expressed in CHO cells
715 13 1 7 8.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br
CHEMBL276819 ednra_human Human No 5.0 IC50 = 11000 nM Bind
Inhibitory concentration against endothelin receptor type AInhibitory concentration against endothelin receptor type A
715 13 1 7 8.3 CCCc1cc(Cn2c(CC)nc3c(C)cc(C)nc32)cc(CCC)c1OC(C(=O)O)c1cc(Br)c(OC)c(OC)c1Br
CHEMBL10750 ednra_human Human No 5.0 IC50 = 11000 nM Bind
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
371 4 1 4 4.8 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccccc1
CHEMBL3633040 ednra_human Human No 7.0 IC50 = 112 nM Funct
Antagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assayAntagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assay
619 11 2 8 6.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(S(F)(F)(F)(F)F)cc2)cc(-c2ncccn2)cc1OCCO
CHEMBL328073 ednra_human Human No 7.0 IC50 = 112 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
544 8 2 7 4.5 COc1ccc(CN2C(=O)CN[C@](C3CCCCC3)([C@H](Oc3nc(C)cc(C)n3)C(=O)O)c3ccccc32)cc1
CHEMBL9495 ednra_rat Rat No 7.0 IC50 = 112 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
482 7 1 6 3.8 COc1ccc([C@@H]2[C@@H](C(=O)O)[C@H](c3ccc4c(c3)OCO4)CN2CC(=O)N(C)CC(C)(C)C)cc1
CHEMBL2163712 ednra_human Human No 7.0 IC50 = 113 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
589 11 1 12 3.1 COc1ccccc1Oc1c(NS(C)(=O)=O)nc(-c2ncccn2)nc1OCCOc1ncc(Br)cn1
CHEMBL94141 ednra_rat Rat No 7.0 IC50 = 113 nM Bind
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
407 9 1 5 5.5 Cc1ccccc1[C@H](CCC(=O)O)Oc1cc(OCc2ccsc2)ccc1C#N
CHEMBL444274 ednra_mouse Mouse No 6.9 IC50 = 114 nM Bind
Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells
None None None CC[C@@H](C)[C@H](NC(=O)[C@H](CCc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL313801 ednra_human Human No 6.9 IC50 = 115 nM Bind
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
482 7 1 5 6.2 Cc1cc(CCC(C)C)ccc1-c1ccsc1S(=O)(=O)Nc1onc(C)c1Br
CHEMBL1271746 ednra_human Human No 6.9 IC50 = 115.9 nM Bind
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
555 10 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2
CHEMBL11064 ednra_human Human No 5.9 IC50 = 1150 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
444 6 1 6 4.6 CC(C)Oc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1
CHEMBL368107 ednra_human Human No 6.9 IC50 = 116 nM Bind
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
712 15 2 12 4.5 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCCNS(=O)(=O)c1ccc(C)cc1
CHEMBL27344 ednra_rat Rat No 5.9 IC50 = 1170 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
359 5 1 5 3.6 CCc1noc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)c1C
CHEMBL327350 ednra_human Human No 5.9 IC50 = 1180 nM Bind
Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cellsDisplacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL176749 ednra_human Human No 6.9 IC50 = 119 nM Bind
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
604 13 2 9 4.6 CCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC
CHEMBL62302 ednra_pig Pig No 7.9 IC50 = 12 nM Funct
Antagonist activity against ET-A from porcine heart membranesAntagonist activity against ET-A from porcine heart membranes
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL10588 ednra_human Human No 7.9 IC50 = 12 nM Funct
Antagonistic activity against human Endothelin A receptor expressed in LtKAntagonistic activity against human Endothelin A receptor expressed in LtK
430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C
CHEMBL10588 ednra_human Human No 7.9 IC50 = 12 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C
CHEMBL274175 ednra_human Human No 7.9 IC50 = 12 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
506 8 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc(OC)c(OC)c2OC)cc1
CHEMBL62374 ednra_rat Rat No 7.9 IC50 = 12 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
388 4 1 5 4.4 CC(C)Oc1ccc2c(c1)C(Cl)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2
CHEMBL321831 ednra_rat Rat No 7.9 IC50 = 12 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
502 13 1 6 4.3 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1CCCO1
CHEMBL123305 ednra_human Human No 7.9 IC50 = 12 nM Bind
Binding affinity towards human Endothelin A receptor (hET -A)Binding affinity towards human Endothelin A receptor (hET -A)
558 11 2 6 5.8 CCCc1cccc(CCC)c1NC(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL330425 ednra_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation countingDisplacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
432 5 2 6 2.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1
CHEMBL24015 ednra_human Human No 7.9 IC50 = 12 nM Bind
Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptorDisplacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
491 6 2 7 2.6 Cn1cc(C(C(=O)NS(=O)(=O)c2ccccc2)c2ccc3c(c2)OCO3)c2ccc(C(N)=O)cc21
CHEMBL3400984 ednra_rat Rat No 7.9 IC50 = 12 nM Bind
Displacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry methodDisplacement of [125I]ET-1 from rat ETA receptor after 1 hr by Lowry method
404 10 1 4 5.5 CC(=O)c1ccc(OCc2ccccc2)cc1OC(CCC(=O)O)c1ccccc1
CHEMBL172144 ednra_rat Rat No 7.9 IC50 = 12 nM Bind
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
417 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O
CHEMBL173792 ednra_rat Rat No 7.9 IC50 = 12 nM Bind
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
417 7 1 6 4.4 Cc1ccccc1C(Oc1cc(OCc2ccc3c(c2)OCO3)ccc1C#N)C(=O)O
CHEMBL1205063 ednra_rat Rat No 7.9 IC50 = 12 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
538 10 1 9 4.8 COc1cc(F)ccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1
CHEMBL48458 ednra_rat Rat No 7.9 IC50 = 12 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
538 10 1 9 4.8 COc1cc(F)ccc1C(=O)/C(Cc1cc(OC)c(OC)c(OC)c1)=C(\C(=O)O)c1ccc2nsnc2c1
CHEMBL298212 ednra_human Human No 7.9 IC50 = 12 nM Bind
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
535 8 2 8 3.4 CCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1OCC(=O)O)N(C(=O)C(=O)O)[C@@H]2c1ccc2c(c1)OCO2
CHEMBL331580 ednra_pig Pig No 7.9 IC50 = 12 nM Bind
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cellsIn vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
556 11 1 10 5.3 COc1cccc(Oc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)ncnc2OCCOc2nccs2)c1
CHEMBL296326 ednra_human Human No 7.9 IC50 = 12 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
455 5 2 6 4.2 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1
CHEMBL366885 ednra_human Human No 7.9 IC50 = 12 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
661 11 2 13 3.6 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccncc1
CHEMBL367686 ednra_human Human No 7.9 IC50 = 12 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
603 10 2 13 4.2 C#CCOc1nc(-c2ccnc(-c3noc(S)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC
CHEMBL71787 ednra_human Human No 7.9 IC50 = 12 nM Bind
Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor.
572 10 1 9 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cccc(OCCCN3CCN(C)CC3)c2)cc1
CHEMBL148751 ednra_mouse Mouse No 7.9 IC50 = 12 nM Bind
Inhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cellsInhibition of [125I]ET1 binding to Endothelin A receptor of murine 3T3 cells
None None None CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)CN(Cc1ccccc1)C(=O)[C@@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC
CHEMBL10588 ednra_human Human No 7.9 IC50 = 12 nM Funct
Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.
430 5 1 6 4.1 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1C
CHEMBL137659 ednra_pig Pig No 7.9 IC50 = 12 nM Bind
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
None None None CC[C@H](C)[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O
CHEMBL330425 ednra_human Human No 7.9 IC50 = 12.3 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
432 5 2 6 2.4 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(C)c3ccccc32)n1
CHEMBL304860 ednra_human Human No 7.9 IC50 = 12.4 nM Bind
Displacement of [125I]ET-1 from Endothelin A receptorDisplacement of [125I]ET-1 from Endothelin A receptor
553 9 3 9 5.1 CCCc1c(O)c(C(C)=O)cc(C(C)=O)c1NC(=O)c1sc(C)cc1S(=O)(=O)Nc1onc(C)c1Cl
CHEMBL6785 ednra_human Human No 7.9 IC50 = 12.6 nM Bind
Inhibition of specific binding of [125-I] ET-1 to human Endothelin A receptorInhibition of specific binding of [125-I] ET-1 to human Endothelin A receptor
450 6 1 6 3.7 CCN(C)c1cccc2c(S(=O)(=O)Nc3ncc(Br)nc3OC)cccc12
CHEMBL312685 ednra_human Human No 6.9 IC50 = 120 nM Bind
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
330 3 1 4 2.9 Cc1cccc(S(=O)(=O)Nc2onc(C)c2Br)c1
CHEMBL80538 ednra_human Human No 6.9 IC50 = 120 nM Bind
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
392 4 1 4 4.2 Cc1noc(NS(=O)(=O)c2cccc(-c3ccccc3)c2)c1Br
CHEMBL298922 ednra_human Human No 6.9 IC50 = 120 nM Bind
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
461 8 1 6 4.8 CCCOc1ccc2c(c1)[C@@H](c1ccc(OC)cc1)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2
CHEMBL292901 ednra_pig Pig No 6.9 IC50 = 120 nM Bind
Inhibition of endothelin (ET-A) binding to porcine heart membranes Inhibition of endothelin (ET-A) binding to porcine heart membranes
None None None CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC(C)=O)C1c2ccccc2CCc2ccccc21)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O
CHEMBL174818 ednra_rat Rat No 6.9 IC50 = 120 nM Bind
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
595 11 4 8 4.2 COC(=O)C1(NC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](Cc2cn(C)c3ccccc23)c2nc(C(=O)O)c(C)o2)CCCCC1
CHEMBL335416 ednra_pig Pig No 6.9 IC50 = 120 nM Bind
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
None None None CCCC[C@@H]1NC(=O)[C@H]2CCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC1=O
CHEMBL62425 ednra_rat Rat No 5.9 IC50 = 1200 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
458 7 1 4 6.6 COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1
CHEMBL156404 ednra_rat Rat No 5.9 IC50 = 1200 nM Bind
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
485 7 1 7 5.2 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3OC)c3c2oc2ccccc23)c(OC)c1
CHEMBL156539 ednra_rat Rat No 5.9 IC50 = 1200 nM Bind
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
469 5 1 7 4.9 COc1ccccc1Cn1c(=O)c(C(=O)O)c(-c2ccc3c(c2)OCO3)c2oc3ccccc3c21
CHEMBL62425 ednra_rat Rat No 5.9 IC50 = 1200 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
458 7 1 4 6.6 COc1ccc(C2=C(C(=O)O)C(c3ccc(C(C)C)cc3)Oc3ccc(OC(C)C)cc32)cc1
CHEMBL62586 ednra_rat Rat No 5.9 IC50 = 1200 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
460 7 1 6 5.2 CCCOc1cccc2c1C(c1ccc(OC)cc1)=C(C(=O)O)C(c1ccc3c(c1)OCO3)O2
CHEMBL412460 ednra_rat Rat No 5.9 IC50 = 1200 nM Bind
In vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricleIn vitro binding affinity against Endothelin A receptor by using endothelin (ET-1) as radioligand in rat heart ventricle
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C(C)C)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL291404 ednra_human Human No 5.9 IC50 = 1200 nM Bind
In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptorIn vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
456 5 1 7 4.1 Cc1cccc(OC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Br)c1
CHEMBL172538 ednra_human Human No 5.9 IC50 = 1200 nM Bind
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
442 6 1 6 4.5 Cc1ccc(OCc2sccc2S(=O)(=O)Nc2onc(C)c2Br)cc1
CHEMBL55666 ednra_rat Rat No 5.9 IC50 = 1200 nM Bind
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
489 9 1 7 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1OC)c(C(=O)O)c(=O)n2Cc1ccccc1OC
CHEMBL273613 ednra_human Human No 5.9 IC50 = 1200 nM Funct
Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.
400 4 1 5 4.1 Cc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)cc1
CHEMBL282557 ednra_rat Rat No 4.9 IC50 = 12000 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
325 6 3 6 1.6 Cc1noc(NS(=O)(=O)c2ccc(NCC(=O)O)cc2)c1C
CHEMBL102494 ednra_human Human No 4.9 IC50 = 12000 nM Funct
Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.Compound was tested for its ability to inhibit Endothelin A receptor induced arachidonic acid release(AARA) in rabbit renal artery vascular smooth muscles.
375 3 0 5 4.1 COC(=O)C(c1ccc2c(c1)OCO2)c1c2c(nc3ccccc13)CCCC2
CHEMBL273258 ednra_human Human No 4.9 IC50 = 12000 nM Bind
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
387 4 1 5 4.7 COc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2-c1ccccc1
CHEMBL368929 ednra_human Human No 6.9 IC50 = 121 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
539 10 1 10 3.4 C#CCOc1nc(N2CCOCC2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC
CHEMBL9132 ednra_rat Rat No 6.9 IC50 = 121 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
496 11 1 6 4.3 CCCN(CCC)C(=O)CCN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1
CHEMBL1271746 ednra_human Human No 6.9 IC50 = 121.3 nM Bind
Antagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assayAntagonist activity at ETA receptor (unknown origin) expressed in HEK293T cells measured after 30 mins by CCF4-AM dye based GeneBlazer FRET assay
555 10 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OCC4CC4)ccc31)OCO2
CHEMBL1184076 ednra_human Human No 6.9 IC50 = 122 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1
CHEMBL331548 ednra_human Human No 6.9 IC50 = 122 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
592 9 2 6 5.8 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(c2ccccc2)c2cc(C)ccc2C)cc1
CHEMBL1184091 ednra_human Human No 5.9 IC50 = 1228 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
562 7 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1
CHEMBL332144 ednra_human Human No 5.9 IC50 = 1228 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
562 7 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC2c3ccccc3-c3ccccc32)cc1
CHEMBL96463 ednra_human Human No 6.9 IC50 = 123 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
552 8 3 7 3.7 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3ccc(C(=O)O)cc3)c3ccccc32)n1
CHEMBL47383 ednra_human Human No 6.9 IC50 = 123 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
484 6 1 9 3.7 Cc1noc(NS(=O)(=O)c2ccsc2C2(Cc3ccc4c(c3)OCO4)OCCO2)c1Cl
CHEMBL417971 ednra_rat Rat No 5.9 IC50 = 1240 nM Bind
Inhibitory activity against the Endothelin A receptor of rat MMQ cellsInhibitory activity against the Endothelin A receptor of rat MMQ cells
461 8 1 6 3.4 CCCCS(=O)(=O)N1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1
CHEMBL173358 ednra_human Human No 6.9 IC50 = 125 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
574 9 2 9 4.8 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ccncc2)nc1OCC#CCO
CHEMBL177143 ednra_human Human No 6.9 IC50 = 125 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
531 10 1 9 4.7 C#CCOc1nc(-c2ccncc2)nc(NS(=O)(=O)c2ccc(C(C)C)cn2)c1Oc1ccccc1OC
CHEMBL268339 ednra_human Human No 6.9 IC50 = 125.9 nM Bind
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
406 4 1 5 3.3 CN(C)c1cccc2c(S(=O)(=O)Nc3cnc(Br)cn3)cccc12
CHEMBL415292 ednra_human Human No 5.9 IC50 = 1258.9 nM Bind
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
361 4 1 4 3.8 CN(C)c1cccc2c(S(=O)(=O)Nc3ccc(Cl)nc3)cccc12
CHEMBL6583 ednra_human Human No 5.9 IC50 = 1258.9 nM Bind
Inhibition of specific binding of [125-I]ET-1 to human endothelin A receptorInhibition of specific binding of [125-I]ET-1 to human endothelin A receptor
342 4 1 5 2.8 Cc1cnc(NS(=O)(=O)c2cccc3c(N(C)C)cccc23)cn1
CHEMBL96193 ednra_human Human No 6.9 IC50 = 126 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
531 8 2 8 2.1 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CCN3CCOCC3)c3ccccc32)n1
CHEMBL3752680 ednra_human Human No 6.9 IC50 = 126 nM Bind
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
598 11 3 7 5.8 CCCc1nc2c(C)cc(C(=O)NCCc3ccccc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1
CHEMBL139734 ednra_human Human No 5.9 IC50 = 1280 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
665 12 1 10 6.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOCc1ccccc1
CHEMBL94602 ednra_human Human No 6.9 IC50 = 129 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
576 8 2 5 5.9 COc1cccc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(Cc3c(Cl)cccc3Cl)c3ccccc32)c1
CHEMBL352657 ednra_human Human No 6.9 IC50 = 129 nM Bind
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
506 6 1 8 4.6 Cc1noc(NS(=O)(=O)c2ccsc2COc2cc3c(cc2Cl)OCO3)c1Br
CHEMBL297048 ednra_human Human No 5.9 IC50 = 1290 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
419 5 2 9 2.9 Cc1nnc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)s1
CHEMBL173833 ednra_rat Rat No 4.9 IC50 = 12900 nM Bind
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
551 11 4 6 5.1 CCn1cc(C[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)NC2CCCCC2)c2nc(C(=O)O)c(C)o2)c2ccccc21
CHEMBL313867 ednra_human Human No 7.9 IC50 = 13 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
476 7 3 7 1.9 Cc1cc(C)nc(O[C@H](C(=O)O)[C@@]2(c3ccccc3)NCC(=O)N(CC(=O)O)c3ccccc32)n1
CHEMBL94983 ednra_human Human No 7.9 IC50 = 13 nM Bind
Binding affinity against endothelin A receptor from rabbit renal vascular smooth musclesBinding affinity against endothelin A receptor from rabbit renal vascular smooth muscles
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL10834 ednra_human Human No 7.9 IC50 = 13 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
446 6 1 7 3.8 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccccc2)c(OC)c1
CHEMBL273948 ednra_human Human No 7.9 IC50 = 13 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
422 5 1 6 4.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2CC2CCCCC2)cc1
CHEMBL320254 ednra_rat Rat No 7.9 IC50 = 13 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
532 13 1 7 4.2 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CCC1OC(C)C(C)O1
CHEMBL73925 ednra_human Human No 7.9 IC50 = 13 nM Bind
Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranesBinding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
631 12 5 4 4.5 CCCCC(NC(=O)[C@@H](Cc1c(Br)[nH]c2ccccc12)NC(=O)C(NC(=O)N1[C@@H](C)CCC[C@H]1C)C1CC1)C(=O)O
CHEMBL12013 ednra_human Human No 7.9 IC50 = 13 nM Bind
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
546 8 1 7 6.2 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(C)c1)C(=O)CCCC2
CHEMBL45087 ednra_human Human No 7.9 IC50 = 13 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
412 5 2 7 3.5 Cc1ccc(NC(=O)c2sccc2S(=O)(=O)Nc2onc(C)c2Cl)nc1
CHEMBL170401 ednra_human Human No 7.9 IC50 = 13 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
587 10 2 13 3.6 C#CCOc1nc(-c2ccnc(-c3noc(O)n3)c2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC
CHEMBL173743 ednra_human Human No 7.9 IC50 = 13 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
589 10 1 10 4.9 COCC#CCOc1nc(-c2ncccn2)nc(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)c1Oc1ccccc1OC
CHEMBL264035 ednra_human Human No 7.9 IC50 = 13 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
688 12 2 12 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCC#CCOC(=O)Nc1ccccc1
CHEMBL2370830 ednra_pig Pig No 7.9 IC50 = 13 nM Bind
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
None None None CC(C)C[C@H]1NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CCCCN2C(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O
CHEMBL1272299 ednra_human Human No 7.9 IC50 = 13.5 nM Bind
Displacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayerDisplacement of [125I]ET1 from ETA receptor expressed in african green monkey CCL-81 cells monolayer
543 9 2 7 5.1 CCc1cc2c(cc1Cn1c(C(=O)O)c(Cc3cccc(C(=O)O)c3)c(=O)c3cc(OC(C)C)ccc31)OCO2
CHEMBL1184117 ednra_human Human No 7.9 IC50 = 13.6 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
544 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1
CHEMBL333034 ednra_human Human No 7.9 IC50 = 13.6 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
544 10 2 6 5.2 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)C)c2ccccc2)cc1
CHEMBL330354 ednra_human Human No 7.9 IC50 = 13.9 nM Funct
Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligandAntagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand
618 10 2 6 5.8 CCCCc1cccc([C@]2([C@H](Oc3nc(C)cc(C)n3)C(=O)O)NCC(=O)N(Cc3c(F)cc(F)cc3F)c3ccccc32)c1
CHEMBL26079 ednra_rat Rat No 6.9 IC50 = 130 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
385 4 1 5 3.4 Cc1noc(NS(=O)(=O)c2cccc3c(N4CCCC4=O)cccc23)c1C
CHEMBL27370 ednra_rat Rat No 6.9 IC50 = 130 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
331 4 2 5 3.3 CNc1cccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc12
CHEMBL283652 ednra_rat Rat No 6.9 IC50 = 130 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
373 5 1 5 4.1 Cc1noc(NS(=O)(=O)c2cccc3c(N(C)C(C)C)cccc23)c1C
CHEMBL3633039 ednra_human Human No 6.9 IC50 = 130 nM Funct
Antagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assayAntagonist activity at human ETA receptor expressed in CHO cells assessed as inhibition of ET-1-induced Ca2+ efflux from endoplasmic reticulum into cytosol by fluo-4 dye-based FLIPR assay
561 10 2 8 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(F)(F)F)cc2)cc(-c2ncccn2)cc1OCCO
CHEMBL61406 ednra_rat Rat No 6.9 IC50 = 130 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
510 14 1 6 7.3 CCCCCCCCCCOC1=C(C(=O)O)C(c2ccc3c(c2)OCO3)Oc2ccc(OC(C)C)cc21
CHEMBL62814 ednra_rat Rat Yes 6.9 IC50 = 130 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
474 8 1 6 5.6 CCCCOc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccccc1OC)O2
CHEMBL109736 ednra_rat Rat No 6.9 IC50 = 130 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
452 8 1 5 3.3 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)CCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL114084 ednra_rat Rat No 6.9 IC50 = 130 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
468 8 1 6 3.2 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCCO3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL317064 ednra_human Human Yes 6.9 IC50 = 130 nM Bind
Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cellsInhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL97470 ednra_human Human No 6.9 IC50 = 130 nM Funct
Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cellsInhibition of ET-1 stimulated arachidonic acid release in rabbit renal vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL10218 ednra_human Human No 6.9 IC50 = 130 nM Bind
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
473 7 1 7 5.3 CCCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)n2Cc1ccc2c(c1)OCO2
CHEMBL337567 ednra_pig Pig No 6.9 IC50 = 130 nM Bind
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
None None None CSCC[C@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](C(C)C)NC1=O
CHEMBL150719 ednra_human Human No 6.9 IC50 = 130 nM Bind
The inhibitory constant was evaluated against Endothelin A receptor in rabbit renal artery tissueThe inhibitory constant was evaluated against Endothelin A receptor in rabbit renal artery tissue
None None None CC[C@@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@H](C)CC
CHEMBL158204 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Ability to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranesAbility to displace [125I]endothelin-1 from endothelin A receptor in rat aorta membranes
459 5 1 5 5.8 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccccc3Cl)c3c2oc2ccccc23)cc1
CHEMBL27187 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
359 4 2 5 3.2 CC(=O)Nc1ccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc2c1
CHEMBL286521 ednra_rat Rat Yes 5.9 IC50 = 1300 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2cccc(N)c2)c1C
CHEMBL3143473 ednra_human Human No 5.9 IC50 = 1300 nM Funct
Antagonistic activity against endothelin A (ETA) receptor using human neuroblastoma cell line.Antagonistic activity against endothelin A (ETA) receptor using human neuroblastoma cell line.
None None None CCCC[C@@H](NC(=O)[C@@H](Cc1cn(COC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O
CHEMBL3305972 ednra_human Human No 5.9 IC50 = 1300 nM Funct
Antagonistic activity against endothelin A (ETA) receptor using human neuroblastoma cell line.Antagonistic activity against endothelin A (ETA) receptor using human neuroblastoma cell line.
None None None CCCC[C@@H](NC(=O)[C@@H](Cc1cn(COC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O
CHEMBL10819 ednra_human Human No 5.9 IC50 = 1300 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
462 8 1 7 4.1 COc1ccc(C2(O)OC(=O)C(c3cc(OC)c(OC)c(OC)c3)=C2Cc2ccccc2)cc1
CHEMBL66094 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Binding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cellsBinding affinity for endothelin A receptor by inhibition of [125I]ET1 binding in rat aorta smooth muscle cells
472 6 1 5 6.3 CC(C)Oc1ccc2c(c1)C(c1ccc3c(c1)OCO3)=C(C(=O)O)C(c1ccc(C(C)C)cc1)O2
CHEMBL112777 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
502 14 1 5 5.5 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1C(C)(C)CCCC
CHEMBL328444 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
415 7 1 5 5.5 O=C(O)/C(=C/c1cc(OCc2ccsc2)ccc1[N+](=O)[O-])c1ccccc1Cl
CHEMBL91741 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
399 6 1 5 4.5 N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1/C=C(/C(=O)O)c1ccccc1
CHEMBL300066 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
485 9 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC#N)c1
CHEMBL54274 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptorDisplacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
502 10 1 7 5.8 COc1cccc(Sc2c(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)noc2CCCC(C)=O)c1
CHEMBL4568795 ednra_human Human No 5.9 IC50 = 1300 nM Bind
Displacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting method
641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O
CHEMBL4596821 ednra_human Human No 5.9 IC50 = 1300 nM Bind
Displacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting methodDisplacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting method
641 12 4 7 4.8 CCCC[C@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O
CHEMBL4471434 ednra_human Human No 5.9 IC50 = 1300 nM Bind
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranesDisplacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
549 10 2 8 5.4 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)cc(-c2ncccn2)cc1OCCO
CHEMBL3144735 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
In vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assayIn vitro inhibition of endothelin binding to endothelin A receptor in rat heart ventricles was measured using a 125-I labelled ET-1 competition assay
440 5 1 5 4.2 COc1cccc(Cn2[nH]c(C(F)(F)F)c(Cc3cc(Cl)c4c(c3)OCO4)c2=O)c1
CHEMBL73506 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptorInhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor
469 5 1 7 4.9 COc1ccc(-c2c(C(=O)O)c(=O)n(Cc3ccc4c(c3)OCO4)c3c2oc2ccccc23)cc1
CHEMBL292580 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)Inhibition of [125I]ET1 binding to rat aorta membranes(ETA)
459 8 1 6 4.8 CCOc1ccc2c(c1)c(-c1ccc(OC)cc1)c(C(=O)O)c(=O)n2Cc1ccccc1OC
CHEMBL27187 ednra_rat Rat No 5.9 IC50 = 1300 nM Bind
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
359 4 2 5 3.2 CC(=O)Nc1ccc2c(S(=O)(=O)Nc3onc(C)c3C)cccc2c1
CHEMBL286521 ednra_rat Rat Yes 5.9 IC50 = 1300 nM Bind
Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cellsInhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2cccc(N)c2)c1C
CHEMBL10136 ednra_human Human No 5.9 IC50 = 1300 nM Bind
Inhibitory concentration to the endothelin A receptor expressed in LtK cellsInhibitory concentration to the endothelin A receptor expressed in LtK cells
507 6 1 7 6.0 O=C(O)c1c(-c2ccc3c(c2)OCO3)c2cc(OCc3ccccc3)ccc2n1-c1ccc2c(c1)OCO2
CHEMBL11131 ednra_human Human Yes 5.9 IC50 = 1300 nM Funct
Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.Tested for antagonistic activity against Endothelin A receptor in the rabbit renal artery vascular smooth muscle cells.
386 4 1 5 3.8 O=C1OC(O)(c2ccccc2)C(Cc2ccccc2)=C1c1ccc2c(c1)OCO2
CHEMBL30246 ednra_human Human No 4.9 IC50 = 13000 nM Bind
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cellsAbility to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
346 4 2 5 2.9 Cc1noc(NS(=O)(=O)c2cccc3c(C(=O)O)cccc23)c1C
CHEMBL30246 ednra_rat Rat No 4.9 IC50 = 13000 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
346 4 2 5 2.9 Cc1noc(NS(=O)(=O)c2cccc3c(C(=O)O)cccc23)c1C
CHEMBL725 ednra_rat Rat Yes 4.9 IC50 = 13000 nM Bind
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
309 4 2 5 2.1 CC(=O)Nc1ccc(S(=O)(=O)Nc2onc(C)c2C)cc1
CHEMBL103886 ednra_human Human Yes 4.9 IC50 = 13000 nM Funct
Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.Antagonistic activity against endothelin A receptor in rabbit renal artery vascular smooth muscle cells.
320 3 1 4 2.9 Cc1cc(C(C(N)=O)c2ccc3c(c2)OCO3)c2ccccc2n1
CHEMBL78734 ednra_human Human No 4.9 IC50 = 13000 nM Bind
Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparationBinding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation
334 3 1 4 2.7 Cc1noc(NS(=O)(=O)c2ccc(F)cc2)c1Br
CHEMBL38071 ednra_rat Rat No 4.9 IC50 = 13000 nM Bind
Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.Compound was evaluated for the binding affinity to endothelin receptor in the rat heart ventricle.
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL4447655 ednra_human Human No 4.9 IC50 = 13000 nM Bind
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cellsDisplacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
592 11 3 9 5.0 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(C(=O)Nc2ccccc2)nc1OCCO
CHEMBL3752145 ednra_human Human No 4.9 IC50 = 13000 nM Bind
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranesDisplacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
628 12 3 8 5.8 CCCc1nc2c(C)cc(C(=O)NCCc3ccc(OC)cc3)cc2n1Cc1ccc(-c2ccccc2C(=O)Nc2nnn[nH]2)cc1
CHEMBL1791280 ednra_human Human No 4.9 IC50 = 13000 nM Bind
Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cellsInhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL1180341 ednra_human Human No 6.9 IC50 = 131 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
558 9 2 6 5.6 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1
CHEMBL122933 ednra_human Human No 6.9 IC50 = 131 nM Bind
Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptorBinding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
558 9 2 6 5.6 COc1ccc([C@H]2[C@H](C(=O)O)[C@@H](c3ccc4c(c3)OCO4)CN2CC(=O)NC(CC(C)(C)C)c2ccccc2)cc1
CHEMBL277275 ednra_human Human No 5.9 IC50 = 1317 nM Bind
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
771 17 2 14 5.7 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2cc(OC)c(OC)c(OC)c2)nc1OCCNS(=O)(=O)c1cccs1
CHEMBL295207 ednra_human Human No 6.9 IC50 = 132 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
471 6 2 7 3.9 COc1ccccc1NC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Br
CHEMBL170229 ednra_human Human No 5.9 IC50 = 1320 nM Bind
Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.Binding affinity against ETA receptor from dog spleen membranes using [125I]ET1 as radioligand.
None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1cn(C)c2ccccc12)NC(=O)[C@H](CC(C)C)NC(=O)N1CCCCCC1)C(=O)O
CHEMBL329861 ednra_human Human No 5.9 IC50 = 1320 nM Bind
Compound was tested for binding affinity against Endothelin A receptorCompound was tested for binding affinity against Endothelin A receptor
428 5 1 6 4.3 COc1cccc(-c2ccsc2S(=O)(=O)Nc2onc(C)c2Br)c1
CHEMBL174781 ednra_human Human No 5.9 IC50 = 1320 nM Bind
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
577 14 2 10 3.4 CCCS(=O)(=O)NCCOc1nc(C2CC2)nc(NS(=O)(=O)c2ccc(C)cn2)c1Oc1ccccc1OC
CHEMBL176538 ednra_human Human No 6.9 IC50 = 134 nM Bind
Inhibition of I-ET-1 binding to human Endothelin A receptorInhibition of I-ET-1 binding to human Endothelin A receptor
514 8 1 8 4.9 CCCc1cc2c(cc1OCc1ccsc1S(=O)(=O)Nc1onc(C)c1Br)OCO2
CHEMBL113379 ednra_rat Rat No 6.9 IC50 = 137 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
452 8 1 5 3.3 CCCN(C)C(=O)CN1C[C@H](c2ccc3c(c2)OCC3)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL3735300 ednra_human Human No 6.9 IC50 = 137 nM Bind
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
663 11 2 8 7.7 CCCc1nc2c(C)cc(C(=O)Nc3ccccc3OC)cc2n1Cc1ccc(-c2ccccc2S(=O)(=O)Nc2onc(C)c2C)cc1
CHEMBL428298 ednra_rat Rat No 4.9 IC50 = 13800 nM Bind
Inhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenatesInhibitory activity was evaluated against ET- A Binding to Endothelin A receptor in MMQ cell homogenates
551 10 3 6 5.0 CCOC(=O)c1nc([C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CC(C)C)NC(=O)N2CCCCCC2)oc1C
CHEMBL367274 ednra_human Human No 5.9 IC50 = 1385 nM Bind
Inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorInhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
698 14 2 12 4.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(N2CCOCC2)nc1OCCNS(=O)(=O)c1ccc(C)cc1
CHEMBL173689 ednra_human Human No 6.9 IC50 = 139 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
651 11 1 10 6.3 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)(C)C)cc2)nc(-c2ncccn2)nc1OCC#CCOc1ccccc1
CHEMBL321852 ednra_rat Rat No 7.9 IC50 = 14 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL368270 ednra_rat Rat No 7.9 IC50 = 14 nM Bind
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
466 7 1 5 5.5 COc1ccc(C(=O)/C(Cc2cccc3ccccc23)=C(\C(=O)O)c2ccc3c(c2)OCO3)cc1
CHEMBL11106 ednra_human Human No 7.9 IC50 = 14 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
490 6 1 9 3.6 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2cc(OC)c3c(c2)OCO3)cc1
CHEMBL269453 ednra_human Human No 7.9 IC50 = 14 nM Bind
Binding affinity against human cloned endothelin A receptor expressed in LTK-cellsBinding affinity against human cloned endothelin A receptor expressed in LTK-cells
466 5 1 6 5.0 COc1ccc(C2(O)OC(=O)C(c3ccc4c(c3)OCO4)=C2Cc2ccc3ccccc3c2)cc1
CHEMBL449962 ednra_pig Pig No 7.9 IC50 = 14 nM Bind
Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.Binding affinity towards endothelin A receptor in porcine aortic smooth muscle membranes.
601 13 5 4 4.7 CCCCC(NC(=O)[C@@H](Cc1c(Cl)[nH]c2ccccc12)NC(=O)C(CC1CC1)NC(=O)N1[C@@H](C)CCC[C@H]1C)C(=O)O
CHEMBL321852 ednra_rat Rat No 7.9 IC50 = 14 nM Bind
Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
484 12 1 4 5.1 CCCCN(CCCC)C(=O)CN1C[C@H](c2ccc(F)cc2)[C@@H](C(=O)O)[C@@H]1c1ccc(OC)cc1
CHEMBL11528 ednra_human Human No 7.9 IC50 = 14 nM Bind
Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysisDisplacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis
562 9 2 8 5.4 CCCc1nc2c(n1Cc1ccc(-c3ccccc3S(=O)(=O)Nc3onc(C)c3C)c(CO)c1)C(=O)CCCC2
CHEMBL2261364 ednra_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cellsDisplacement of [I125]ET1 from Homo sapiens (human) ETA receptor expressed in CHO cells
510 6 1 7 4.0 COc1cc(C)ccc1S(=O)(=O)NC(=O)C(c1ccc2c(c1)OCO2)c1cn(C)c2cc(F)ccc12
CHEMBL2163713 ednra_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
603 12 1 12 3.5 CCS(=O)(=O)Nc1nc(-c2ncccn2)nc(OCCOc2ncc(Br)cn2)c1Oc1ccccc1OC
CHEMBL2163726 ednra_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysisDisplacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
642 14 2 10 4.6 COc1ccccc1Oc1c(NS(=O)(=O)NCc2ccccc2)nc(C2CC2)nc1OCCOc1ncc(Br)cn1
CHEMBL352536 ednra_rat Rat No 7.9 IC50 = 14 nM Bind
In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.In vitro ability to antagonise the binding of [125I]ET1 to the rat aortic A10 cell membrane endothelin A receptor.
437 7 1 6 4.7 N#Cc1ccc(OCc2ccc3c(c2)OCO3)cc1OC(C(=O)O)c1ccccc1Cl
CHEMBL1206716 ednra_rat Rat No 7.9 IC50 = 14 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
478 8 1 7 4.8 COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1
CHEMBL299521 ednra_rat Rat No 7.9 IC50 = 14 nM Bind
In vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptorIn vitro ability to inhibit specific [125I]ET1 binding to rat aorta membranes Endothelin A receptor
478 8 1 7 4.8 COc1ccc(C(=O)/C(Cc2ccc(OC)c(F)c2)=C(\C(=O)O)c2ccc3nsnc3c2)cc1
CHEMBL49312 ednra_human Human No 7.9 IC50 = 14 nM Bind
In vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptorIn vitro inhibition of [125I]ET1 binding to CHO cells expressing recombinant human Endothelin A receptor
563 11 2 8 4.9 CCOc1ccc2c(c1)[C@H](c1ccc(OC)cc1OCC(C)(C)C(=O)O)N(CC(=O)O)[C@@H]2c1ccc2c(c1)OCO2
CHEMBL314691 ednra_rat Rat Yes 7.9 IC50 = 14 nM Bind
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
None None None None
CHEMBL47706 ednra_human Human No 7.9 IC50 = 14 nM Bind
In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assayIn vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay
484 6 1 8 3.8 Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2ccc3c(c2)OCO3)c1Br
CHEMBL275897 ednra_human Human No 7.9 IC50 = 14 nM Bind
In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptorIn vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor
682 12 2 13 5.1 COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccncc2)nc1OCC#CCOC(=O)Nc1cnccn1
CHEMBL405599 ednra_human