Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
44354055 121987 0 None - 1 Human 8.0 pEC50 = 8 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1041 20 8 8 2.8 COc1c(I)cc(C[C@H](NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1I 10.1021/jm00020a029
CHEMBL334510 121987 0 None - 1 Human 8.0 pEC50 = 8 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1041 20 8 8 2.8 COc1c(I)cc(C[C@H](NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1I 10.1021/jm00020a029
CHEMBL1556461 215581 0 None - 1 Human 8.0 pEC50 = 8 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00020a029
11803290 113426 0 None - 1 Human 7.0 pEC50 = 7 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143277 113426 0 None - 1 Human 7.0 pEC50 = 7 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
9962227 106419 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 763 18 9 8 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284285 106419 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 763 18 9 8 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280767 121362 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 577 15 9 8 -1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33377 121362 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 577 15 9 8 -1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9960837 122311 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 629 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33532 122311 0 None - 1 Human 6.0 pEC50 = 6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 629 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL115543 215282 20 None - 1 Human 6.0 pEC50 = 6 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL407378 219437 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm00020a029
44281172 106450 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 589 15 9 9 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1cccs1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284474 106450 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 589 15 9 9 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1cccs1)C(N)=O 10.1016/s0960-894x(99)00197-3
9875337 106023 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2Cl)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL281753 106023 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2Cl)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
10461499 30800 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 617 20 8 7 -0.9 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL133808 30800 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 617 20 8 7 -0.9 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL337126 218371 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280949 109491 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 651 15 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc2c(c1)-c1ccccc1-2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL30484 109491 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 651 15 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc2c(c1)-c1ccccc1-2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9851501 124002 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33946 124002 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL336623 218364 1 None - 1 Human 5.9 pEC50 = 5.9 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CN)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280660 106654 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 617 15 7 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285915 106654 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 617 15 7 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL131912 215476 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280685 106527 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 585 15 7 8 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csnn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285018 106527 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 585 15 7 8 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csnn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL132849 215490 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL132292 215480 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280899 121563 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33394 121563 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281047 174606 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 752 18 10 8 2.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2c[nH]c3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL430734 174606 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 752 18 10 8 2.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2c[nH]c3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44354285 29470 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1147 26 12 10 0.3 C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)NC(Cc1cc(I)c(O)c(I)c1)C(N)=O 10.1021/jm00020a029
CHEMBL132734 29470 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1147 26 12 10 0.3 C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)NC(Cc1cc(I)c(O)c(I)c1)C(N)=O 10.1021/jm00020a029
44354055 121987 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1041 20 8 8 2.8 COc1c(I)cc(C[C@H](NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1I 10.1021/jm00020a029
CHEMBL334510 121987 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1041 20 8 8 2.8 COc1c(I)cc(C[C@H](NC(=O)[C@H](Cc2ccc(Cl)c(Cl)c2)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1I 10.1021/jm00020a029
CHEMBL130147 215464 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL1556461 215581 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00020a029
44280608 106879 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 731 18 9 8 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(F)=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287468 106879 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 731 18 9 8 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(F)=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL2431718 217241 0 None 44 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human PAR1 expressed in African green monkey COS7 cells assessed as stimulation of inositol triphosphate productionAgonist activity at human PAR1 expressed in African green monkey COS7 cells assessed as stimulation of inositol triphosphate production
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(C)C)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(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C 10.1021/jm400638v
10747898 113476 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143683 113476 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44826172 106764 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc([N+](=O)[O-])c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286648 106764 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc([N+](=O)[O-])c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44826171 123644 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2[N+](=O)[O-])n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33818 123644 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2[N+](=O)[O-])n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL134081 215504 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL33473 218179 24 None - 1 Human 6.7 pEC50 = 6.7 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm00020a029
CHEMBL335845 218345 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280804 106453 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284498 106453 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL263369 217350 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm00020a029
44280877 123649 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 589 15 9 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33820 123649 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 589 15 9 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1016/s0960-894x(99)00197-3
9875040 121201 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 713 18 9 8 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33318 121201 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 713 18 9 8 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL337502 218376 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None COc1ccc(C[C@H](NC(=O)[C@H](C)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm00020a029
44280935 106865 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc(Cl)c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287368 106865 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc(Cl)c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL133789 215501 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm00020a029
44281237 123507 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 604 16 7 6 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33742 123507 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 604 16 7 6 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
90663359 113447 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 761 21 8 7 0.8 CC(=O)NCCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143325 113447 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 761 21 8 7 0.8 CC(=O)NCCC(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL334746 218180 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(Cl)c(Cl)c1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL33473 218179 24 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1016/s0960-894x(99)00197-3
44280607 174630 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 789 19 9 8 3.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(=C/c2ccccc2)c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL430930 174630 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 789 19 9 8 3.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(=C/c2ccccc2)c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL130930 215469 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
9810477 105552 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 719 18 9 9 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccs2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL278216 105552 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 719 18 9 9 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccs2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281081 126481 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34738 126481 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44354323 31055 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1021 26 12 10 -0.4 C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)NC(Cc1ccc(O)c(I)c1)C(N)=O 10.1021/jm00020a029
CHEMBL134036 31055 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 1021 26 12 10 -0.4 C[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)NC(Cc1ccc(O)c(I)c1)C(N)=O 10.1021/jm00020a029
CHEMBL334746 218180 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Evaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activity of Radio-ligand Peptides upon the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(Cl)c(Cl)c1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280768 123952 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 569 14 9 8 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(99)00197-3
CHEMBL33940 123952 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 569 14 9 8 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(99)00197-3
CHEMBL434623 220438 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL264249 217389 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/jm00020a029
CHEMBL3143260 217926 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10461499 30800 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 617 20 8 7 -0.9 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL133808 30800 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL 617 20 8 7 -0.9 CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CCN)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
11803426 113475 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 793 20 10 7 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143682 113475 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 793 20 10 7 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
9937578 106733 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 555 15 7 8 0.3 NCCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286430 106733 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 555 15 7 8 0.3 NCCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL133837 215502 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL263319 217346 0 None - 1 Human 4.4 pEC50 = 4.4 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280822 123323 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 594 15 8 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1nccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33629 123323 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 594 15 8 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1nccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9895920 106796 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 656 15 7 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cncc(Br)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286837 106796 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 656 15 7 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cncc(Br)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281079 123998 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(Cl)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33945 123998 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(Cl)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280955 126070 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 611 15 8 6 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc2[nH]cnc2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34387 126070 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 611 15 8 6 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc2[nH]cnc2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL2370701 216696 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm00020a029
CHEMBL337490 218375 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(Cl)c(Cl)c1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280651 122211 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 781 18 9 8 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33506 122211 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 781 18 9 8 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9961058 106727 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 645 15 7 7 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(=O)c2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286382 106727 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 645 15 7 7 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(=O)c2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280650 121897 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(Cl)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33435 121897 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(Cl)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280649 119434 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 743 19 8 9 1.3 COc1ccc(/C=C/C(=O)Nc2n[nH]c(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n2)cc1 10.1016/s0960-894x(99)00197-3
CHEMBL33033 119434 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 743 19 8 9 1.3 COc1ccc(/C=C/C(=O)Nc2n[nH]c(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n2)cc1 10.1016/s0960-894x(99)00197-3
44280667 109723 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 738 18 9 9 1.4 N#Cc1ccc(/C=C/C(=O)Nc2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n[nH]2)cc1 10.1016/s0960-894x(99)00197-3
CHEMBL30635 109723 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 738 18 9 9 1.4 N#Cc1ccc(/C=C/C(=O)Nc2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n[nH]2)cc1 10.1016/s0960-894x(99)00197-3
CHEMBL3143259 217925 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663347 113444 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 781 21 8 9 0.9 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)O 10.1021/jm960455s
CHEMBL3143312 113444 0 None - 1 Human 4.2 pEC50 = 4.2 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL 781 21 8 9 0.9 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)O 10.1021/jm960455s
CHEMBL133449 215498 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
CHEMBL130058 215463 1 None - 1 Human 4.2 pEC50 = 4.2 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(N)=O 10.1021/jm00020a029
CHEMBL2370948 216744 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Effective concentration for stimulation of platelet aggregationEffective concentration for stimulation of platelet aggregation
ChEMBL None None None COc1ccc(C[C@H](NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
9808447 109692 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 583 15 9 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL30612 109692 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 583 15 9 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280585 123757 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 727 18 8 8 1.7 C/C(=C\c1ccccc1)C(=O)Nc1n[nH]c(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)n1 10.1016/s0960-894x(99)00197-3
CHEMBL33873 123757 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 727 18 8 8 1.7 C/C(=C\c1ccccc1)C(=O)Nc1n[nH]c(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)n1 10.1016/s0960-894x(99)00197-3
44280936 123298 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 731 18 9 8 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33617 123298 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 731 18 9 8 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL337875 218378 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00020a029
44280683 106181 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL282733 106181 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL268064 217517 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Evaluated for the activation of human thrombin receptor measured by platelet aggregationEvaluated for the activation of human thrombin receptor measured by platelet aggregation
ChEMBL None None None None 10.1021/jm00020a029
44281070 119125 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 633 15 7 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2s1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL32941 119125 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 633 15 7 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2s1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL3143248 217921 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)CCCN)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44281289 125340 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 599 15 10 9 -0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34156 125340 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Activation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombinActivation of human platelet aggregation (gel-filtered platelets) induced by alpha thrombin
ChEMBL 599 15 10 9 -0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/s0960-894x(99)00197-3
121469330 155403 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 474 4 1 5 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2cc[nH]n2)CC1(F)F 10.1021/acsmedchemlett.6b00327
CHEMBL3939323 155403 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 474 4 1 5 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2cc[nH]n2)CC1(F)F 10.1021/acsmedchemlett.6b00327
155526775 177961 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1309 45 6 19 5.6 NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)nn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)NCc2ccccc2)nn1 10.1021/acsmedchemlett.8b00538
CHEMBL4459024 177961 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1309 45 6 19 5.6 NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)nn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)NCc2ccccc2)nn1 10.1021/acsmedchemlett.8b00538
44306762 209879 0 None - 1 Human 7.0 pIC50 = 7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL63966 209879 0 None - 1 Human 7.0 pIC50 = 7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44306599 210432 1 None - 1 Human 7.0 pIC50 = 7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL67308 210432 1 None - 1 Human 7.0 pIC50 = 7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
51003683 82428 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL2047297 82428 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL4227548 82428 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
44338917 168701 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 409 8 0 4 5.9 Clc1cccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL415325 168701 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 409 8 0 4 5.9 Clc1cccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
44306903 109029 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303157 109029 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306404 209687 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL62775 209687 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44316184 110931 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 397 8 3 6 0.1 COC(=O)C(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL309531 110931 0 None - 1 Human 6.0 pIC50 = 6 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 397 8 3 6 0.1 COC(=O)C(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
51003683 82428 0 None - 1 Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL2047297 82428 0 None - 1 Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL4227548 82428 0 None - 1 Human 6.0 pIC50 = 6 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
137655130 165427 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 489 5 2 4 5.7 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2CCc1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4092540 165427 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 489 5 2 4 5.7 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2CCc1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/acs.jmedchem.7b00951
145971090 171814 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 323 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2N=[N+]=[N-])c1 10.1016/j.bmc.2018.04.016
CHEMBL4226195 171814 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 323 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2N=[N+]=[N-])c1 10.1016/j.bmc.2018.04.016
145967675 171875 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 370 5 2 2 4.1 C#CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL4227184 171875 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 370 5 2 2 4.1 C#CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
44306659 109549 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL305188 109549 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
137661486 166255 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4101591 166255 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
145386428 183876 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 478 6 2 5 4.7 C[C@H]1OC(=O)[C@]2(NCC(=O)O)C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
CHEMBL4633243 183876 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 478 6 2 5 4.7 C[C@H]1OC(=O)[C@]2(NCC(=O)O)C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
44316560 111553 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 375 7 3 5 0.0 O=C(NCCS(=O)(=O)O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL310859 111553 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 375 7 3 5 0.0 O=C(NCCS(=O)(=O)O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
44306660 210602 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL68458 210602 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL3143271 217933 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306894 109489 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304829 109489 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
12018762 116411 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL322282 116411 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
90663563 113477 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 829 22 9 8 2.0 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143684 113477 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 829 22 9 8 2.0 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
44339029 116469 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL322763 116469 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44338929 12617 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107919 12617 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
137632193 163441 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@H]2CC[C@@H]3COC(=O)[C@H]3[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
CHEMBL4069486 163441 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@H]2CC[C@@H]3COC(=O)[C@H]3[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
44339060 16194 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 323 5 2 3 3.5 CC(C)N(CC(O)c1ccc(C#N)cc1)C(=O)Nc1ccccc1 10.1016/s0960-894x(01)00745-4
CHEMBL111689 16194 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 323 5 2 3 3.5 CC(C)N(CC(O)c1ccc(C#N)cc1)C(=O)Nc1ccccc1 10.1016/s0960-894x(01)00745-4
12018759 117976 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL326456 117976 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
155564785 182299 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1786 52 6 24 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4578092 182299 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1786 52 6 24 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
44338929 12617 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107919 12617 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44339173 14996 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL109226 14996 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
10276545 15918 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL110024 15918 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44306349 109379 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304120 109379 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44306337 103612 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL265227 103612 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
44306499 210124 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL65004 210124 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
44328342 214872 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 881 21 8 7 5.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL97780 214872 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 881 21 8 7 5.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)C(=O)O 10.1016/s0960-894x(98)00730-6
44339157 116532 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 451 8 0 6 5.5 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL323054 116532 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 451 8 0 6 5.5 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL5085826 221772 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None CC1=NO[C@@]2(C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@@H](c1ccc(-c3cccc(F)c3)cn1)[C@@H]2C 10.1021/acs.jmedchem.1c02048
CHEMBL5077710 221290 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@@H]1[C@@H](C)[C@@H]2CNC[C@@]23C(=O)O[C@H](C)[C@H]3[C@H]1/C=C/c1ccc(-c2ccccc2C#N)cn1 10.1021/acs.jmedchem.1c02048
155549751 180697 0 None 16 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4540591 180697 0 None 16 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
44339002 16122 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111258 16122 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
12018762 116411 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL322282 116411 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44306500 174695 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL431369 174695 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
137637794 162793 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 5 1 4 5.5 CO[C@@H]1CC[C@@]2(C)[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@@]3(CC[C@@H]2[C@]1(C)CO)CO3 10.1021/acs.jmedchem.7b00951
CHEMBL4062114 162793 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 5 1 4 5.5 CO[C@@H]1CC[C@@]2(C)[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@@]3(CC[C@@H]2[C@]1(C)CO)CO3 10.1021/acs.jmedchem.7b00951
137653750 165507 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 439 5 2 4 4.8 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2CCc1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4093491 165507 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 439 5 2 4 4.8 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2CCc1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
44306337 103612 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL265227 103612 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
137645208 164745 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 421 4 1 3 5.9 C[C@H]1CC[C@H]2[C@@](C)(CC[C@@H](O)[C@@]2(C)C=O)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4084812 164745 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 421 4 1 3 5.9 C[C@H]1CC[C@H]2[C@@](C)(CC[C@@H](O)[C@@]2(C)C=O)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
44306761 175688 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL438551 175688 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44338885 14271 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 405 9 0 5 5.2 COc1cccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL108716 14271 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 405 9 0 5 5.2 COc1cccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL3143270 217932 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143299 217945 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(N)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
137661676 166131 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 450 5 2 4 5.1 CNC[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL4100310 166131 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 450 5 2 4 5.1 CNC[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL3143317 217954 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143311 217950 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL5078821 221367 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1OC(=O)[C@@H]2CC3(NC(=O)NC3=O)[C@@H](C)[C@H](c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
155549751 180697 0 None 16 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4540591 180697 0 None 16 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
145386406 184299 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 459 5 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NCC#N)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
CHEMBL4639789 184299 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 459 5 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NCC#N)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
9919038 173507 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL428311 173507 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL3143290 217943 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
9832212 211728 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL4226137 211728 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL7642 211728 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL3143254 217923 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm960455s
44306697 109509 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304924 109509 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
137638549 163644 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 435 3 1 4 5.3 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H](O)CC[C@]2(C)[C@@H]1CC[C@@H]1COC(=O)[C@H]12 10.1021/acs.jmedchem.7b00951
CHEMBL4071756 163644 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 435 3 1 4 5.3 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H](O)CC[C@]2(C)[C@@H]1CC[C@@H]1COC(=O)[C@H]12 10.1021/acs.jmedchem.7b00951
10161572 12323 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107667 12323 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
1048267 39202 92 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL1411333 39202 92 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
17222599 176549 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 3.8 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL4438936 176549 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 3.8 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL5084411 221693 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1OC(=O)[C@]2(O)CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
9832212 211728 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
CHEMBL4226137 211728 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
CHEMBL7642 211728 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
9832212 211728 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL4226137 211728 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL7642 211728 4 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
9825804 212272 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 466 8 3 5 2.9 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1cnc2ccccc2c1 10.1016/0960-894X(96)00438-6
CHEMBL80623 212272 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 466 8 3 5 2.9 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1cnc2ccccc2c1 10.1016/0960-894X(96)00438-6
10095734 212310 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 459 8 3 6 2.1 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00438-6
CHEMBL80942 212310 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 459 8 3 6 2.1 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1ccc2c(c1)OCO2 10.1016/0960-894X(96)00438-6
CHEMBL3143272 217934 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306698 109488 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304827 109488 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44306404 209687 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL62775 209687 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44338895 16077 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 8 0 4 6.4 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3ccc4ccccc4c3)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL110996 16077 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 8 0 4 6.4 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3ccc4ccccc4c3)on2)cc1 10.1016/s0960-894x(01)00745-4
10771636 113436 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143298 113436 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306696 108906 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL302433 108906 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44316045 109885 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 2 4 0.9 CN1CCC(CCC(=O)N2CCCC(C(=O)NCCC(=O)O)C2)CC1 10.1016/0960-894X(96)00438-6
CHEMBL307684 109885 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 2 4 0.9 CN1CCC(CCC(=O)N2CCCC(C(=O)NCCC(=O)O)C2)CC1 10.1016/0960-894X(96)00438-6
22611792 111903 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 3 4 1.0 CC(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL311426 111903 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 3 4 1.0 CC(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
137639606 163681 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H](OC(N)=O)CC[C@]2(C)[C@@H]1CC[C@@H]1COC(=O)[C@H]12 10.1021/acs.jmedchem.7b00951
CHEMBL4072202 163681 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H](OC(N)=O)CC[C@]2(C)[C@@H]1CC[C@@H]1COC(=O)[C@H]12 10.1021/acs.jmedchem.7b00951
44315780 211855 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 375 8 3 5 0.0 O=C(O)CCNC(=O)C1CCCN(S(=O)(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL77367 211855 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 375 8 3 5 0.0 O=C(O)CCNC(=O)C1CCCN(S(=O)(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL3143291 217944 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306499 210124 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL65004 210124 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
137654212 165456 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@H]2CC[C@@H]3COC(=O)[C@H]3[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
CHEMBL4092965 165456 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 478 4 1 5 5.4 C[C@]1(/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@H]2CC[C@@H]3COC(=O)[C@H]3[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
44338944 118158 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 481 9 0 7 5.5 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
CHEMBL327117 118158 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 481 9 0 7 5.5 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
90663337 113437 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 869 20 9 10 1.1 CC(=O)N(C(=O)c1cc2ccccc2oc1=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143301 113437 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 869 20 9 10 1.1 CC(=O)N(C(=O)c1cc2ccccc2oc1=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
17222599 176549 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 3.8 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL4438936 176549 3 None - 1 Human 6.7 pIC50 = 6.7 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 3.8 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
44339001 116267 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
CHEMBL322093 116267 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 463 9 0 7 5.4 COc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
10276545 15918 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL110024 15918 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44306403 209641 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL62584 209641 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
137647264 164642 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 436 4 2 4 4.8 C[C@@]12CC[C@@H](O)[C@@](C)(CN)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4083850 164642 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 436 4 2 4 4.8 C[C@@]12CC[C@@H](O)[C@@](C)(CN)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
9853816 104112 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL269345 104112 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44306903 109029 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303157 109029 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
90663307 113422 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1ccc(Cl)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143267 113422 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1ccc(Cl)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44338787 13665 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
CHEMBL108428 13665 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
10077130 10779 53 None 29 4 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4047 10779 53 None 29 4 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4870 10779 53 None 29 4 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL493982 10779 53 None 29 4 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
DB09030 10779 53 None 29 4 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
10077130 10779 53 None 29 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2020.127046
4047 10779 53 None 29 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2020.127046
4870 10779 53 None 29 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2020.127046
CHEMBL493982 10779 53 None 29 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2020.127046
DB09030 10779 53 None 29 4 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2020.127046
90663294 113416 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 827 22 8 9 2.1 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143253 113416 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 827 22 8 9 2.1 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
90663318 113428 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 986 28 12 10 0.5 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143280 113428 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 986 28 12 10 0.5 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143309 217948 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)COc1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306500 174695 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL431369 174695 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
12018758 16119 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL111241 16119 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
9853816 104112 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL269345 104112 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL3143321 217957 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(O)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL5094099 222248 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@@H]1[C@@H](C)[C@@H]2CN(C)C[C@@]23C(=O)O[C@H](C)[C@H]3[C@H]1/C=C/c1ccc(-c2ccccc2C#N)cn1 10.1021/acs.jmedchem.1c02048
117909194 159015 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 485 4 1 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2n[nH]c(=O)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
CHEMBL3968866 159015 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 485 4 1 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2n[nH]c(=O)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
CHEMBL3143246 217920 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC#Cc1ccccc1C(=O)N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
22611774 212216 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 2 4 0.9 CN(CCC(=O)O)C(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80289 212216 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 2 4 0.9 CN(CCC(=O)O)C(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
145970191 171859 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 870 18 5 7 6.7 C#CCCC(=O)NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL4226980 171859 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 870 18 5 7 6.7 C#CCCC(=O)NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
90663334 113435 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 807 20 9 7 2.0 CC(=O)N(c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143297 113435 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 807 20 9 7 2.0 CC(=O)N(c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
137654568 165714 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 4 2 4 4.9 C[C@]1(C(=O)O)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL4095795 165714 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 4 2 4 4.9 C[C@]1(C(=O)O)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
12018757 115937 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
CHEMBL321437 115937 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 467 8 0 6 6.0 Clc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
CHEMBL5085562 221752 2 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@]4(O)CC(F)(F)[C@H]3C)nc2)c1C#N 10.1021/acs.jmedchem.1c02048
CHEMBL5091232 222077 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1[C@H](c2ccc(-c3cccc(F)c3)cn2)[C@@H]2[C@@H](C)OC(=O)[C@@H]2C[C@@H]1C 10.1021/acs.jmedchem.1c02048
117909768 154124 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 491 4 1 8 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2nnc(N)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
CHEMBL3929336 154124 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 491 4 1 8 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2nnc(N)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
155536026 178884 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1698 46 6 22 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4472608 178884 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1698 46 6 22 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
10350886 185535 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against PAR1 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometryAntagonist activity against PAR1 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometry
ChEMBL 942 27 13 9 -0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O nan
CHEMBL46869 185535 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against PAR1 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometryAntagonist activity against PAR1 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometry
ChEMBL 942 27 13 9 -0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O nan
44328523 113412 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 786 21 10 7 1.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL314325 113412 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 786 21 10 7 1.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1016/s0960-894x(98)00730-6
44306697 109509 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304924 109509 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
10819322 211692 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL7610 211692 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44316522 212277 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80672 212277 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
137632009 163434 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 435 4 1 4 5.1 C[C@]1(C=O)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL4069403 163434 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 435 4 1 4 5.1 C[C@]1(C=O)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
90663339 113439 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 883 21 9 8 3.1 CC(=O)N(C(=O)c1cccc(C2CCCCC2)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143303 113439 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 883 21 9 8 3.1 CC(=O)N(C(=O)c1cccc(C2CCCCC2)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306403 209641 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL62584 209641 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
44316532 212244 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)[C@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80455 212244 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)[C@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
10459564 7305 41 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
4048 7305 41 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
CHEMBL2103856 7305 41 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
DB12046 7305 41 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
57892463 171835 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CCC2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmc.2018.04.016
CHEMBL4226439 171835 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CCC2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmc.2018.04.016
44306402 174987 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL433499 174987 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44328340 103477 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1095 30 12 10 3.0 CCC(=O)NCCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL264099 103477 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1095 30 12 10 3.0 CCC(=O)NCCC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
10328351 214816 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 892 24 10 8 2.9 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CCc1ccc(C(=O)c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL97498 214816 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 892 24 10 8 2.9 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CCc1ccc(C(=O)c2ccccc2)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O 10.1016/s0960-894x(98)00730-6
145970191 171859 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 870 18 5 7 6.7 C#CCCC(=O)NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
CHEMBL4226980 171859 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 870 18 5 7 6.7 C#CCCC(=O)NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/j.bmc.2018.04.016
3109060 177442 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 3 4.5 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1ccco1 10.1016/j.bmc.2019.06.043
CHEMBL4451525 177442 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 3 4.5 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1ccco1 10.1016/j.bmc.2019.06.043
50910548 82429 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 374 5 2 2 4.7 CC(C)CC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL2047299 82429 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 374 5 2 2 4.7 CC(C)CC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
877874 30096 17 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL1332325 30096 17 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
877874 30096 17 None - 1 Human 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL1332325 30096 17 None - 1 Human 5.5 pIC50 = 5.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
57892463 171835 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CCC2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmc.2018.04.016
CHEMBL4226439 171835 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CCC2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmc.2018.04.016
3109060 177442 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 3 4.5 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1ccco1 10.1016/j.bmc.2019.06.043
CHEMBL4451525 177442 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 3 4.5 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1ccco1 10.1016/j.bmc.2019.06.043
10279248 115619 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 511 9 0 8 4.7 CS(=O)(=O)c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL320990 115619 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 511 9 0 8 4.7 CS(=O)(=O)c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
44339002 16122 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111258 16122 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
137633371 163157 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 450 4 1 3 6.9 C[C@H]1CC[C@@H]2C(C)(C)[C@H](OC(N)=O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4066290 163157 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 450 4 1 3 6.9 C[C@H]1CC[C@@H]2C(C)(C)[C@H](OC(N)=O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
90663297 113417 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143256 113417 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44339055 16095 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
CHEMBL111101 16095 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 447 8 0 6 5.7 Cc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
10459564 7305 41 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
4048 7305 41 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
CHEMBL2103856 7305 41 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
DB12046 7305 41 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 10.1016/j.bmc.2018.04.016
877874 30096 17 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL1332325 30096 17 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
44338886 170080 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 391 9 0 5 4.8 COc1cccc(CN(CCCN2CCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL418815 170080 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 391 9 0 5 4.8 COc1cccc(CN(CCCN2CCCC2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL3143288 217941 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@H](Cc1cccs1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306761 175688 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL438551 175688 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44328381 105070 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1265 34 15 12 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCNC(=O)CCCC[C@H]1SC[C@H]2NC(=O)N[C@H]21)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL274769 105070 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1265 34 15 12 3.5 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCNC(=O)CCCC[C@H]1SC[C@H]2NC(=O)N[C@H]21)C(=O)O 10.1016/s0960-894x(98)00730-6
10161572 12323 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107667 12323 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
90663354 113445 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccccc1F)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143319 113445 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccccc1F)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
155549751 180697 0 None 16 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of thrombin-induced intracellular calcium mobilization preincubated for 15 mins followed by thrombin addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of thrombin-induced intracellular calcium mobilization preincubated for 15 mins followed by thrombin addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4540591 180697 0 None 16 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of thrombin-induced intracellular calcium mobilization preincubated for 15 mins followed by thrombin addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of thrombin-induced intracellular calcium mobilization preincubated for 15 mins followed by thrombin addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
44338864 14064 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 439 8 0 4 6.8 c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL108604 14064 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 439 8 0 4 6.8 c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
44306612 108937 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL302603 108937 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
154688307 179627 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cnco1 10.1016/j.bmc.2019.06.043
CHEMBL4514779 179627 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cnco1 10.1016/j.bmc.2019.06.043
10278388 117776 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 495 9 0 7 5.1 C[S+]([O-])c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL326247 117776 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 495 9 0 7 5.1 C[S+]([O-])c1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
155519325 177195 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 2 2 4.6 O=C(CC(F)(F)F)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL4448258 177195 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 2 2 4.6 O=C(CC(F)(F)F)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
90663343 113443 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1cccc2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143308 113443 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1cccc2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306658 108972 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 835 19 6 9 5.0 COC(=O)c1ccc(Cn2cc(CN3CCCC3)c3ccc(NC(=O)N[C@@H](Cc4ccc(OC)cc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC4CCCCC4)cc32)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL302823 108972 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 835 19 6 9 5.0 COC(=O)c1ccc(Cn2cc(CN3CCCC3)c3ccc(NC(=O)N[C@@H](Cc4ccc(OC)cc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC4CCCCC4)cc32)cc1 10.1016/s0960-894x(01)00378-x
90663292 113414 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 857 22 9 9 1.4 COc1ccc(/C=C/C(=O)N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
CHEMBL3143251 113414 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 857 22 9 9 1.4 COc1ccc(/C=C/C(=O)N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
90663333 113434 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 843 23 9 8 2.4 CCCC(=O)c1ccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
CHEMBL3143296 113434 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 843 23 9 8 2.4 CCCC(=O)c1ccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
155519325 177195 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 2 2 4.6 O=C(CC(F)(F)F)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL4448258 177195 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 400 4 2 2 4.6 O=C(CC(F)(F)F)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
154688304 182990 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cocn1 10.1016/j.bmc.2019.06.043
CHEMBL4594058 182990 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cocn1 10.1016/j.bmc.2019.06.043
CHEMBL5069528 220997 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None CCOC(=O)N1C[C@H]2[C@H](C)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@]32C1 10.1021/acs.jmedchem.1c02048
117909666 155528 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 492 4 1 7 4.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2n[nH]c(=O)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
CHEMBL3940415 155528 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assayAntagonist activity at PAR-1 in HEK293 cells incubated for 30 mins followed by Ala-parafluoroPhe-Arg-Cha-Cit-Try-NH2 substrate addition by calcium-5 dye based FLIPR assay
ChEMBL 492 4 1 7 4.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(c2n[nH]c(=O)o2)CC1(F)F 10.1021/acsmedchemlett.6b00327
155512671 176447 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1874 58 6 26 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4437508 176447 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1874 58 6 26 9.3 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
90663313 113423 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 982 27 12 10 -0.3 C#CC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143273 113423 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 982 27 12 10 -0.3 C#CC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
90663314 113424 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 984 28 11 11 0.6 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143274 113424 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 984 28 11 11 0.6 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
44338946 16078 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
CHEMBL110998 16078 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
44306659 109549 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL305188 109549 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44306611 210381 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL66958 210381 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
15887956 212211 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 415 8 3 4 2.3 O=C(O)CC(NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1)c1ccccc1 10.1016/0960-894X(96)00438-6
CHEMBL80232 212211 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 415 8 3 4 2.3 O=C(O)CC(NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1)c1ccccc1 10.1016/0960-894X(96)00438-6
44316106 212227 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 395 9 3 4 2.0 CC(C)CC(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80343 212227 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 395 9 3 4 2.0 CC(C)CC(CC(=O)O)NC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
90663330 113431 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1cccc(F)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143293 113431 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1cccc(F)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
15887960 212311 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 363 7 3 6 -0.1 O=C(NCCc1nnn[nH]1)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80943 212311 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 363 7 3 6 -0.1 O=C(NCCc1nnn[nH]1)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
44306657 109036 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303187 109036 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL3143264 217928 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm960455s
154688304 182990 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cocn1 10.1016/j.bmc.2019.06.043
CHEMBL4594058 182990 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cocn1 10.1016/j.bmc.2019.06.043
12018759 117976 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL326456 117976 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL4764659 220824 0 None 173 2 Human 6.4 pIC50 = 6.4 Functional
Affinity Phenotypic Cellular interaction (Inhibition of platelet aggregation (human plasma, TRAP-6)) EUB0000291b F2RAffinity Phenotypic Cellular interaction (Inhibition of platelet aggregation (human plasma, TRAP-6)) EUB0000291b F2R
ChEMBL None None None O=C(N1CCS(=O)(=O)CC1)N1C[C@@](S)(c2ccc(OC(F)(F)F)cc2)C[C@@](S)(c2nc(C3CC3)no2)C1 10.6019/CHEMBL5209897
10206026 16215 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 479 9 0 7 6.1 CSc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111761 16215 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 479 9 0 7 6.1 CSc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
90663291 113413 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 18 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 18 uM) induced platelet aggregation by 50%
ChEMBL 877 21 9 8 2.7 CC(=O)N(C(=O)c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143250 113413 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 18 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 18 uM) induced platelet aggregation by 50%
ChEMBL 877 21 9 8 2.7 CC(=O)N(C(=O)c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306540 209815 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL63402 209815 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
10164471 15907 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 509 9 0 6 7.0 c1ccc(-c2ccc(-c3cc(N(CCCN4CCCCCC4)Cc4ccc5c(c4)OCO5)on3)cc2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL109946 15907 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 509 9 0 6 7.0 c1ccc(-c2ccc(-c3cc(N(CCCN4CCCCCC4)Cc4ccc5c(c4)OCO5)on3)cc2)cc1 10.1016/s0960-894x(01)00745-4
44306698 109488 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304827 109488 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
90663332 113433 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1ccc2ccccc2c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143295 113433 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1ccc2ccccc2c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44338946 16078 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
CHEMBL110998 16078 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
10077130 10779 53 None 29 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4047 10779 53 None 29 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4870 10779 53 None 29 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL493982 10779 53 None 29 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
DB09030 10779 53 None 29 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL3143275 217935 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm960455s
90663360 113448 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 795 21 9 9 1.2 CC(=O)N(Oc1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143326 113448 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 795 21 9 9 1.2 CC(=O)N(Oc1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306501 109468 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304683 109468 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44306657 109036 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303187 109036 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306402 174987 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL433499 174987 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
9832212 211728 4 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
CHEMBL4226137 211728 4 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
CHEMBL7642 211728 4 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human MDA-MB-231 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/acsmedchemlett.8b00538
CHEMBL5077302 221271 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1OC(=O)[C@@H]2CC(F)(F)[C@@H](C)[C@H](c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
CHEMBL3143281 217937 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44338787 13665 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
CHEMBL108428 13665 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
44338875 116555 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 413 9 0 5 5.6 COc1cccc(CN(CCCN2C=CC=CC=C2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL323221 116555 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 413 9 0 5 5.6 COc1cccc(CN(CCCN2C=CC=CC=C2)c2cc(-c3ccccc3)no2)c1 10.1016/s0960-894x(01)00745-4
44339070 117109 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 8 0 4 6.4 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL323956 117109 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 8 0 4 6.4 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL3143284 217939 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306732 109381 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304128 109381 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44339056 15457 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 453 9 0 4 7.2 c1ccc(-c2cc(N(CCCCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL109564 15457 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 453 9 0 4 7.2 c1ccc(-c2cc(N(CCCCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
44338865 115899 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 7 0 4 6.4 c1ccc(-c2cc(N(CCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL321380 115899 1 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 425 7 0 4 6.4 c1ccc(-c2cc(N(CCN3CCCCCC3)Cc3cccc4ccccc34)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL3143313 217951 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44315792 211834 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 341 6 3 5 0.4 O=C(O)CCNC(=O)C1CCCN(C(=O)OCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL77179 211834 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 341 6 3 5 0.4 O=C(O)CCNC(=O)C1CCCN(C(=O)OCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
154688307 179627 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cnco1 10.1016/j.bmc.2019.06.043
CHEMBL4514779 179627 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 385 4 2 4 3.9 O=C(Nc1cccc(NC(=O)c2ccccc2Br)c1)c1cnco1 10.1016/j.bmc.2019.06.043
9847494 12620 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107920 12620 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL3143249 217922 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663299 113419 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 812 20 10 7 1.9 CC(=O)N(c1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143258 113419 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 812 20 10 7 1.9 CC(=O)N(c1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
145386419 183846 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 474 5 1 5 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cc1 10.1016/j.bmcl.2020.127046
CHEMBL4632907 183846 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 474 5 1 5 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cc1 10.1016/j.bmcl.2020.127046
137644873 164990 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 439 4 3 4 4.8 C[C@]1(O)CC[C@H]2[C@@](C)(CC[C@@H](O)[C@@]2(C)CO)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4088070 164990 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 439 4 3 4 4.8 C[C@]1(O)CC[C@H]2[C@@](C)(CC[C@@H](O)[C@@]2(C)CO)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
9919038 173507 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL428311 173507 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
1048267 39202 92 None - 1 Human 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL1411333 39202 92 None - 1 Human 6.2 pIC50 = 6.2 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL5081773 221546 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1NC(=O)[C@]2(N)CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
90663316 113427 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 1002 28 11 11 0.7 CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143278 113427 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 1002 28 11 11 0.7 CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
44338882 12695 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 419 8 0 6 5.0 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL107971 12695 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 419 8 0 6 5.0 c1ccc(-c2cc(N(CCCN3CCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
44306708 107687 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL293867 107687 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44306336 210326 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL66585 210326 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
44306599 210432 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL67308 210432 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44328562 174858 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 924 23 11 8 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL432578 174858 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 924 23 11 8 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
145386418 183913 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 512 5 1 6 6.1 Cc1ccnc(N[C@@H]2CC[C@@H]3[C@@H](C2)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]3/C=C/c2ccc(-c3cccc(F)c3)cn2)n1 10.1016/j.bmcl.2020.127046
CHEMBL4633888 183913 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 512 5 1 6 6.1 Cc1ccnc(N[C@@H]2CC[C@@H]3[C@@H](C2)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]3/C=C/c2ccc(-c3cccc(F)c3)cn2)n1 10.1016/j.bmcl.2020.127046
44306349 109379 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304120 109379 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44306336 210326 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL66585 210326 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
10077130 10779 53 None 29 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4047 10779 53 None 29 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4870 10779 53 None 29 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
CHEMBL493982 10779 53 None 29 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
DB09030 10779 53 None 29 4 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
44306540 209815 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL63402 209815 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306612 108937 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL302603 108937 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
90663305 113421 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 558 11 5 5 2.3 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(N)=O 10.1021/jm960455s
CHEMBL3143265 113421 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 558 11 5 5 2.3 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(N)=O 10.1021/jm960455s
44339030 16188 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 509 9 0 6 7.0 c1ccc(-c2cccc(-c3cc(N(CCCN4CCCCCC4)Cc4ccc5c(c4)OCO5)on3)c2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111653 16188 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 509 9 0 6 7.0 c1ccc(-c2cccc(-c3cc(N(CCCN4CCCCCC4)Cc4ccc5c(c4)OCO5)on3)c2)cc1 10.1016/s0960-894x(01)00745-4
15887958 112074 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 393 5 2 5 0.5 O=C(O)C1CN(C(=O)C2CCCN(C(=O)CCC3CCNCC3)C2)CCC1=O 10.1016/0960-894X(96)00438-6
CHEMBL311554 112074 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 393 5 2 5 0.5 O=C(O)C1CN(C(=O)C2CCCN(C(=O)CCC3CCNCC3)C2)CCC1=O 10.1016/0960-894X(96)00438-6
90663358 113446 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 903 22 9 8 3.1 CC(=O)N(C(=O)/C=C/c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143324 113446 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 903 22 9 8 3.1 CC(=O)N(C(=O)/C=C/c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663341 113441 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143306 113441 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3144093 217961 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)CSc1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL5081315 221520 2 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1OC(=O)[C@]2(N)CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
CHEMBL5088392 221936 2 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None CCNC(=O)N1C[C@H]2[C@H](C)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@]32C1 10.1021/acs.jmedchem.1c02048
CHEMBL5094869 222295 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None CNC(=O)N1C[C@H]2[C@H](C)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@]32C1 10.1021/acs.jmedchem.1c02048
44338944 118158 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 481 9 0 7 5.5 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
CHEMBL327117 118158 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 481 9 0 7 5.5 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
44306501 109468 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304683 109468 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44306762 209879 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL63966 209879 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
9801767 107106 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL289432 107106 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 339 7 3 4 0.6 O=C(O)CCNC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
137649563 164129 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 465 4 1 5 5.0 COC(=O)[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL4077763 164129 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 465 4 1 5 5.0 COC(=O)[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
44315793 211766 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 340 6 4 4 -0.0 O=C(O)CCNC(=O)C1CCCN(C(=O)NCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL76641 211766 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 340 6 4 4 -0.0 O=C(O)CCNC(=O)C1CCCN(C(=O)NCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
44316059 212317 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 325 7 3 4 0.2 O=C(O)CCNC(=O)C1CCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL80975 212317 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 325 7 3 4 0.2 O=C(O)CCNC(=O)C1CCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
90663340 113440 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1ccsc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143304 113440 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1ccsc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
145386426 184291 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 459 5 1 5 5.1 C[C@H]1OC(=O)[C@]2(NCC#N)C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
CHEMBL4639680 184291 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assayAntagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay
ChEMBL 459 5 1 5 5.1 C[C@H]1OC(=O)[C@]2(NCC#N)C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1016/j.bmcl.2020.127046
CHEMBL3143268 217930 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CCCCC/C=C/CC(=O)N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306696 108906 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL302433 108906 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
1048267 39202 92 None - 1 Human 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL1411333 39202 92 None - 1 Human 6.1 pIC50 = 6.1 Functional
Negative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayNegative allosteric modulation of PAR1 in human EAhy926 cells assessed as reduction in TFLLRN-NH2-induced intracellular calcium mobilization incubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2019.06.043
CHEMBL5093637 222214 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None C[C@H]1OC(=O)[C@]2(O)CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/acs.jmedchem.1c02048
CHEMBL5094241 222262 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysisAntagonist activity at human PAR-1 expressed in HEK293 cells assessed as reduction in TRAP induced calcium signal at 3 uM by FLIPR analysis
ChEMBL None None None CC[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F 10.1021/acs.jmedchem.1c02048
90663298 113418 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 120 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 120 uM) induced platelet aggregation by 50%
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143257 113418 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 120 uM) induced platelet aggregation by 50%Concentration of compound required to inhibit agonist (SFFLRR-NH2, at 120 uM) induced platelet aggregation by 50%
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10741717 109811 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 439 7 3 4 2.0 O=C(O)C[C@@H](C#Cc1ccccc1)NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL307065 109811 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 439 7 3 4 2.0 O=C(O)C[C@@H](C#Cc1ccccc1)NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
10526120 211636 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 419 7 3 4 2.0 CC(C)(C)C#C[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL75636 211636 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 419 7 3 4 2.0 CC(C)(C)C#C[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
44316156 211773 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 355 7 4 5 -0.4 O=C(O)C(O)CNC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL76719 211773 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 355 7 4 5 -0.4 O=C(O)C(O)CNC(=O)C1CCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL3143282 217938 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
22645287 211645 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 3 4 1.0 O=C(O)CCNC(=O)C1CCCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
CHEMBL75688 211645 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 353 7 3 4 1.0 O=C(O)CCNC(=O)C1CCCCN(C(=O)CCC2CCNCC2)C1 10.1016/0960-894X(96)00438-6
137653180 165335 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 5 1 4 5.5 COC[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
CHEMBL4091623 165335 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 451 5 1 4 5.5 COC[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1O 10.1021/acs.jmedchem.7b00951
145967675 171875 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 370 5 2 2 4.1 C#CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL4227184 171875 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 370 5 2 2 4.1 C#CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
10162707 16100 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 478 9 0 8 5.3 O=[N+]([O-])c1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL111109 16100 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 478 9 0 8 5.3 O=[N+]([O-])c1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL3143266 217929 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(C)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663293 113415 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 998 29 11 11 1.0 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CCC(N)=O 10.1021/jm960455s
CHEMBL3143252 113415 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 998 29 11 11 1.0 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CCC(N)=O 10.1021/jm960455s
1048267 39202 92 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL1411333 39202 92 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
44306708 107687 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL293867 107687 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
90663302 113420 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 765 20 9 7 1.1 CC(=O)N(C1CCCC1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143262 113420 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 765 20 9 7 1.1 CC(=O)N(C1CCCC1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
137632975 163127 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 508 5 1 6 5.1 COC(=O)[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
CHEMBL4065905 163127 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 508 5 1 6 5.1 COC(=O)[C@@]1(C)[C@H]2CC[C@@]3(CO3)[C@@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@]2(C)CC[C@H]1OC(N)=O 10.1021/acs.jmedchem.7b00951
CHEMBL3143310 217949 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@H](CCCN)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)/C=C/c1ccccc1 10.1021/jm960455s
137652024 163899 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 485 5 0 4 6.7 C[C@H]1CC[C@@H]2C(C)(C)[C@H](OS(C)(=O)=O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4074902 163899 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 485 5 0 4 6.7 C[C@H]1CC[C@@H]2C(C)(C)[C@H](OS(C)(=O)=O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL3143289 217942 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663338 113438 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 833 22 9 9 1.8 C=CC(=O)c1ccsc1N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143302 113438 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 833 22 9 9 1.8 C=CC(=O)c1ccsc1N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44338791 16098 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111106 16098 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
9847494 12620 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107920 12620 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44338791 16098 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111106 16098 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL3143249 217922 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10622095 212058 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 421 8 3 5 2.4 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1cccs1 10.1016/0960-894X(96)00438-6
CHEMBL79087 212058 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.In vitro inhibition of thrombin-induced human gel-filtered platelet aggregation.
ChEMBL 421 8 3 5 2.4 O=C(O)C[C@H](NC(=O)[C@@H]1CCCN(C(=O)CCC2CCNCC2)C1)c1cccs1 10.1016/0960-894X(96)00438-6
44306894 109489 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304829 109489 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306660 210602 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL68458 210602 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)In vitro inhibition of human platelet aggregation induced by SFLLRN-NH2 (at a concentration of 2 uM)
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
44306732 109381 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304128 109381 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
10819322 211692 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL7610 211692 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
128205 16222 2 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 375 8 0 4 5.2 c1ccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111790 16222 2 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
ChEMBL 375 8 0 4 5.2 c1ccc(CN(CCCN2CCCCC2)c2cc(-c3ccccc3)no2)cc1 10.1016/s0960-894x(01)00745-4
44328197 89159 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1051 28 10 9 5.0 CCC(=O)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL217237 89159 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1051 28 10 9 5.0 CCC(=O)NCCC[C@H](NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)O 10.1016/s0960-894x(98)00730-6
90663321 113429 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 850 23 6 8 1.5 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143283 113429 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 850 23 6 8 1.5 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
12018758 16119 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL111241 16119 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombinInhibition of secretion of radiolabeled serotonin from washed human platelets stimulated by 1 nM thrombin
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
137659611 166231 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 437 4 2 4 4.9 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4101239 166231 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 437 4 2 4 4.9 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
145971090 171814 0 None - 1 Human 4.0 pIC50 = 4.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 323 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2N=[N+]=[N-])c1 10.1016/j.bmc.2018.04.016
CHEMBL4226195 171814 0 None - 1 Human 4.0 pIC50 = 4.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 323 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2N=[N+]=[N-])c1 10.1016/j.bmc.2018.04.016
90663331 113432 0 None - 1 Human 4.0 pIC50 = 4.0 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 773 20 9 7 1.4 CC(=O)N(c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143294 113432 0 None - 1 Human 4.0 pIC50 = 4.0 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 773 20 9 7 1.4 CC(=O)N(c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143266 217929 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(C)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
137631870 163123 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 487 4 2 4 5.7 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4065873 163123 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assayAntagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay
ChEMBL 487 4 2 4 5.7 C[C@@]12CC[C@@H](O)[C@@](C)(CO)[C@H]1CC[C@@]1(CO1)[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/acs.jmedchem.7b00951
155526775 177961 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1309 45 6 19 5.6 NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)nn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)NCc2ccccc2)nn1 10.1021/acsmedchemlett.8b00538
CHEMBL4459024 177961 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by TFLLRN-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1309 45 6 19 5.6 NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)nn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)NCc2ccccc2)nn1 10.1021/acsmedchemlett.8b00538
51003683 82428 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL2047297 82428 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
CHEMBL4227548 82428 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1016/j.bmc.2018.04.016
44328383 165742 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1222 32 12 11 5.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=O)CCCCC1SC[C@H]2NC(=O)N[C@@H]12)C(=O)O 10.1016/s0960-894x(98)00730-6
CHEMBL409602 165742 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Human Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregationHuman Thrombin receptor 1 (PAR-1) antagonistic ability to inhibit SFLLRN-NH2 (2.7 uM)-induced platelet aggregation
ChEMBL 1222 32 12 11 5.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)C(=O)N[C@@H](CCCNC(=O)CCCCC1SC[C@H]2NC(=O)N[C@@H]12)C(=O)O 10.1016/s0960-894x(98)00730-6
44306611 210381 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL66958 210381 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)In vitro inhibition of human platelet aggregation induced by alpha-thrombin (at a concentration of 0.15 nM)
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
90663342 113442 0 None - 1 Human 5.0 pIC50 = 5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 828 21 10 8 1.6 CC(=O)N(Oc1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143307 113442 0 None - 1 Human 5.0 pIC50 = 5 Functional
Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%Concentration required to inhibit agonist (SFFLRR-NH2, at 3 uM) induced platelet aggregation by 50%
ChEMBL 828 21 10 8 1.6 CC(=O)N(Oc1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44264790 105099 0 None - 0 Human 9.4 pKd = 9.4 Functional
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 862 18 7 8 5.8 NC(CCN[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1)C(=O)O 10.1021/jm000506s
CHEMBL275003 105099 0 None - 0 Human 9.4 pKd = 9.4 Functional
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 862 18 7 8 5.8 NC(CCN[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1)C(=O)O 10.1021/jm000506s
19323337 8397 1 None - 1 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl 10.1016/j.bmcl.2010.01.050
9255 8397 1 None - 1 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl 10.1016/j.bmcl.2010.01.050
CHEMBL559808 8397 1 None - 1 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl 10.1016/j.bmcl.2010.01.050
46865538 12909 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 389 5 0 6 2.7 N#Cc1ccccc1/C=C/c1c(N2CCN(Cc3ccsc3)CC2)c(=O)c1=O 10.1016/j.bmcl.2010.01.050
CHEMBL1080910 12909 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 389 5 0 6 2.7 N#Cc1ccccc1/C=C/c1c(N2CCN(Cc3ccsc3)CC2)c(=O)c1=O 10.1016/j.bmcl.2010.01.050
46880808 13106 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 376 4 1 2 4.5 O=C(/C=C\c1ccccc1Cl)N1CCC(Nc2ccc(F)cc2)C(F)C1 10.1016/j.bmcl.2010.01.050
CHEMBL1081998 13106 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 376 4 1 2 4.5 O=C(/C=C\c1ccccc1Cl)N1CCC(Nc2ccc(F)cc2)C(F)C1 10.1016/j.bmcl.2010.01.050
46880668 12937 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 389 5 0 5 3.0 N#Cc1ccccc1/C=C/c1c(N2CCN(CC3CCCCC3)CC2)c(=O)c1=O 10.1016/j.bmcl.2010.01.050
CHEMBL1081077 12937 0 None - 0 Human 6.4 pKd = 6.4 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 389 5 0 5 3.0 N#Cc1ccccc1/C=C/c1c(N2CCN(CC3CCCCC3)CC2)c(=O)c1=O 10.1016/j.bmcl.2010.01.050
46865537 14250 0 None - 0 Human 6.2 pKd = 6.2 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 472 7 0 4 4.7 N#Cc1ccccc1/C=C\C(=O)N1CCC(N(Cc2ccc(F)cc2)Cc2ccccn2)C(F)C1 10.1016/j.bmcl.2010.01.050
CHEMBL1087016 14250 0 None - 0 Human 6.2 pKd = 6.2 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 472 7 0 4 4.7 N#Cc1ccccc1/C=C\C(=O)N1CCC(N(Cc2ccc(F)cc2)Cc2ccccn2)C(F)C1 10.1016/j.bmcl.2010.01.050
44251419 13073 0 None - 0 Human 6.0 pKd = 6.0 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 317 5 1 4 4.2 N#Cc1ccccc1/C=C/C(=O)c1ccc(NC2CCCC2)nc1 10.1016/j.bmcl.2010.01.050
CHEMBL1081797 13073 0 None - 0 Human 6.0 pKd = 6.0 Functional
Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assayAntagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release by FLIPR assay
ChEMBL 317 5 1 4 4.2 N#Cc1ccccc1/C=C/C(=O)c1ccc(NC2CCCC2)nc1 10.1016/j.bmcl.2010.01.050
10077130 10779 53 None 29 4 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium effluxAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4047 10779 53 None 29 4 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium effluxAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4870 10779 53 None 29 4 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium effluxAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL493982 10779 53 None 29 4 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium effluxAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
DB09030 10779 53 None 29 4 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium effluxAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
10077130 10779 53 None 29 4 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporationAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4047 10779 53 None 29 4 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporationAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4870 10779 53 None 29 4 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporationAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL493982 10779 53 None 29 4 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporationAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
DB09030 10779 53 None 29 4 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporationAntagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
10146183 10562 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9315351
3742 10562 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9315351
CHEMBL4065100 10562 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9315351
19323337 8397 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl None
9255 8397 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl None
CHEMBL559808 8397 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 358 4 0 2 3.8 Fc1ccc(cc1)CN1CCN(CC1)C(=O)/C=C/c1ccccc1Cl None
3525 10194 13 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10535908
9853822 10194 13 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10535908
CHEMBL311626 10194 13 None - 1 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10535908
10971 10331 30 None 158 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 11020444
4259181 10331 30 None 158 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 11020444
CHEMBL63426 10331 30 None 158 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 11020444
10459564 7305 41 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 21300059
4048 7305 41 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 21300059
CHEMBL2103856 7305 41 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 21300059
DB12046 7305 41 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC 21300059


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL2370701 216696 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Activation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric methodActivation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1016/j.bmc.2021.116498
CHEMBL5088108 221918 0 None - 0 Human 4.3 pEC50 = 4.3 Binding
Activation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric methodActivation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cc(F)c(F)c(F)c1F)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1016/j.bmc.2021.116498
CHEMBL5081145 221506 0 None - 0 Human 5.1 pEC50 = 5.1 Binding
Activation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric methodActivation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c(F)cc(F)c(F)c1F)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1016/j.bmc.2021.116498
CHEMBL5087962 221910 0 None - 0 Human 4.0 pEC50 = 4 Binding
Activation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric methodActivation of PAR-1 in human platelet-rich plasma assessed as induction of platelet aggregation by turbidimetric method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1016/j.bmc.2021.116498
127053962 157312 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 6 6.2 Cc1nnc(C[C@@]23CC(F)(F)[C@@H](C)[C@H](/C=C/c4ccc(-c5ccccc5Cl)cn4)C2[C@@H](C)OC3=O)o1 nan
CHEMBL3954641 157312 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 6 6.2 Cc1nnc(C[C@@]23CC(F)(F)[C@@H](C)[C@H](/C=C/c4ccc(-c5ccccc5Cl)cn4)C2[C@@H](C)OC3=O)o1 nan
127053955 167211 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cscn2)CC1(F)F nan
CHEMBL4111522 167211 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cscn2)CC1(F)F nan
127053997 155729 0 None - 0 Human 9.0 pIC50 = 9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 7 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nnnn2C)CC1(F)F nan
CHEMBL3942006 155729 0 None - 0 Human 9.0 pIC50 = 9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 7 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nnnn2C)CC1(F)F nan
10077130 10779 53 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4047 10779 53 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4870 10779 53 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
CHEMBL493982 10779 53 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
DB09030 10779 53 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
127053960 154430 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 499 5 0 6 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2ncon2)CC1(F)F nan
CHEMBL3931589 154430 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 499 5 0 6 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2ncon2)CC1(F)F nan
127053994 158717 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 1 5 4.7 Cc1cccc(-c2ccc(/C=C/[C@@H]3C4[C@@H](C)OC(=O)[C@]4(CN)CC(F)(F)[C@H]3C)nc2)c1C#N nan
CHEMBL3966338 158717 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 1 5 4.7 Cc1cccc(-c2ccc(/C=C/[C@@H]3C4[C@@H](C)OC(=O)[C@]4(CN)CC(F)(F)[C@H]3C)nc2)c1C#N nan
127053955 167211 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cscn2)CC1(F)F nan
CHEMBL4111522 167211 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cscn2)CC1(F)F nan
127053956 167489 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2nccs2)CC1(F)F nan
CHEMBL4113709 167489 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2nccs2)CC1(F)F nan
127053958 167637 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ncco2)CC1(F)F nan
CHEMBL4114937 167637 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ncco2)CC1(F)F nan
72547307 110646 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
CHEMBL3091980 110646 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
127053975 150080 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cncs2)CC1(F)F nan
CHEMBL3897109 150080 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cncs2)CC1(F)F nan
127053965 166652 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 489 4 0 7 4.8 Cc1cn([C@@]23CC(F)(F)C(C)[C@H](/C=C/c4ccc(-c5ccccc5C#N)cn4)C2[C@@H](C)OC3=O)nn1 nan
CHEMBL4106770 166652 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 489 4 0 7 4.8 Cc1cn([C@@]23CC(F)(F)C(C)[C@H](/C=C/c4ccc(-c5ccccc5C#N)cn4)C2[C@@H](C)OC3=O)nn1 nan
10077130 10779 53 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4047 10779 53 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4870 10779 53 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
CHEMBL493982 10779 53 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
DB09030 10779 53 None - 1 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
127053995 154619 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 407 3 1 3 4.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2C(CC1(F)F)C(=O)N[C@@H]2C nan
CHEMBL3933019 154619 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 407 3 1 3 4.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2C(CC1(F)F)C(=O)N[C@@H]2C nan
127053938 155203 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 408 3 0 4 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3937747 155203 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 408 3 0 4 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
127053976 158948 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cscn2)CC1(F)F nan
CHEMBL3968240 158948 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cscn2)CC1(F)F nan
127053985 167474 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 545 5 1 5 5.8 C[C@H]1OC(=O)[C@]2(NC(=O)c3ccc(F)cc3)CC(F)(F)[C@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]12 nan
CHEMBL4113548 167474 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 545 5 1 5 5.8 C[C@H]1OC(=O)[C@]2(NC(=O)c3ccc(F)cc3)CC(F)(F)[C@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]12 nan
127053957 167100 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cocn2)CC1(F)F nan
CHEMBL4110608 167100 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cocn2)CC1(F)F nan
CHEMBL4764659 220824 0 None - 0 Human 8.0 pIC50 = 8 Binding
Affinity On-target Cellular interaction (Functional cellular assay in HEK cells expressing F2R) EUB0000291b F2RAffinity On-target Cellular interaction (Functional cellular assay in HEK cells expressing F2R) EUB0000291b F2R
ChEMBL None None None O=C(N1CCS(=O)(=O)CC1)N1C[C@@](S)(c2ccc(OC(F)(F)F)cc2)C[C@@](S)(c2nc(C3CC3)no2)C1 10.6019/CHEMBL5210121
127050657 147598 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 486 7 2 5 2.9 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCc2cccc(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3819038 147598 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 486 7 2 5 2.9 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCc2cccc(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
44432773 93803 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232534 93803 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
9889179 94747 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 5.9 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL234190 94747 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 5.9 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
44432790 104060 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL269006 104060 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
9931987 79340 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL199201 79340 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm0502236
71736052 153610 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 493 5 1 5 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC(C)(C)C)CC1(F)F nan
CHEMBL3924976 153610 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 493 5 1 5 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC(C)(C)C)CC1(F)F nan
121335751 155489 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 479 5 1 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC2COC2)CC1(F)F nan
CHEMBL3940064 155489 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 479 5 1 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC2COC2)CC1(F)F nan
44428104 151201 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
CHEMBL390630 151201 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
127053947 157068 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 445 4 1 4 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)O)CC1(F)F nan
CHEMBL3952737 157068 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 445 4 1 4 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)O)CC1(F)F nan
127049415 147631 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 473 5 2 6 2.7 N#C/N=C(/Nc1cccc(OC(F)F)c1)N1CC(N2CNCC2=O)C(c2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01890
CHEMBL3819515 147631 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 473 5 2 6 2.7 N#C/N=C(/Nc1cccc(OC(F)F)c1)N1CC(N2CNCC2=O)C(c2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01890
72547556 110659 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091993 110659 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44408851 82182 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL204009 82182 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44409253 82807 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 418 3 1 4 5.2 CC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL205683 82807 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 418 3 1 4 5.2 CC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
11576348 78797 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 466 4 1 5 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(S(N)(=O)=O)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL197523 78797 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 466 4 1 5 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(S(N)(=O)=O)c4)cn3)[C@H]12 10.1021/jm0502236
44305948 107375 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 399 4 1 5 5.3 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N5CCCCC5)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL291807 107375 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 399 4 1 5 5.3 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N5CCCCC5)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
44305954 169352 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 359 4 1 5 4.4 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL416862 169352 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 359 4 1 5 4.4 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL3143263 217927 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)c1ccccc1N)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
9805672 213876 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 491 5 3 3 5.8 C[C@H]1CC[C@@H]([C@@H](O)c2ccc(Cl)c(Cl)c2)N1C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL91987 213876 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 491 5 3 3 5.8 C[C@H]1CC[C@@H]([C@@H](O)c2ccc(Cl)c(Cl)c2)N1C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
44409265 81790 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 434 5 1 5 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(N)=O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL203376 81790 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 434 5 1 5 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(N)=O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44306404 209687 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL62775 209687 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 813 20 6 7 5.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
11502697 141201 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(Cl)cc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371751 141201 0 None - 0 Human 6.0 pIC50 = 6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(Cl)cc4)cn3)[C@H]12 10.1021/jm0502236
752812 9352 50 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 10.1016/j.bmcl.2014.08.021
9459 9352 50 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 10.1016/j.bmcl.2014.08.021
CHEMBL1609104 9352 50 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 10.1016/j.bmcl.2014.08.021
44187282 131921 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 482 11 1 8 4.0 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OC)cc(OCC2CCCCC2)c1 nan
CHEMBL3644439 131921 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 482 11 1 8 4.0 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OC)cc(OCC2CCCCC2)c1 nan
44290104 185340 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 735 19 7 8 2.8 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL46702 185340 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 735 19 7 8 2.8 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
44280898 106539 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 566 15 8 5 1.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285075 106539 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 566 15 8 5 1.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280876 106691 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 507 13 8 8 -2.0 C[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286141 106691 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 507 13 8 8 -2.0 C[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280731 107058 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 597 16 9 8 -0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CCc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL289020 107058 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 597 16 9 8 -0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CCc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281047 174606 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 752 18 10 8 2.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2c[nH]c3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL430734 174606 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 752 18 10 8 2.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2c[nH]c3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
23631377 99971 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 512 6 0 5 4.8 CCCS(=O)(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
CHEMBL244503 99971 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 512 6 0 5 4.8 CCCS(=O)(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
10162707 16100 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 478 9 0 8 5.3 O=[N+]([O-])c1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL111109 16100 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 478 9 0 8 5.3 O=[N+]([O-])c1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
90663347 113444 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 781 21 8 9 0.9 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)O 10.1021/jm960455s
CHEMBL3143312 113444 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 781 21 8 9 0.9 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)O 10.1021/jm960455s
58046056 140060 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 469 10 2 9 3.4 CCC(CC)Oc1cc(C)c2nn(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704461 140060 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 469 10 2 9 3.4 CCC(CC)Oc1cc(C)c2nn(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)c(=N)n2n1 nan
66760759 134049 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 394 7 1 3 3.9 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)CCOC)C2)cc1 nan
CHEMBL3658402 134049 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 394 7 1 3 3.9 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)CCOC)C2)cc1 nan
66761545 134056 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 399 4 2 2 4.2 CCc1ccc(C2CC(NC(=O)NC(C)(C)C)CN(C(=O)C3CCCC3)C2)cc1 nan
CHEMBL3658409 134056 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 399 4 2 2 4.2 CCc1ccc(C2CC(NC(=O)NC(C)(C)C)CN(C(=O)C3CCCC3)C2)cc1 nan
9804049 140341 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL371069 140341 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1016/j.bmcl.2006.06.042
44418858 90064 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 3 6.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218935 90064 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 3 6.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm061043e
9804049 140341 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL371069 140341 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
23631187 166251 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 528 4 0 5 6.1 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
CHEMBL410157 166251 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 528 4 0 5 6.1 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
44432714 93469 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 393 3 0 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccsc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231727 93469 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 393 3 0 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccsc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
9804049 140341 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL371069 140341 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
11553497 140229 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
CHEMBL370656 140229 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
9804049 140341 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371069 140341 2 None - 1 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
66701293 134062 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 469 5 1 4 4.4 O=C(NC1CC(c2ccc(OC(F)(F)F)cc2)CN(C(=O)c2ccncc2)C1)c1ccccc1 nan
CHEMBL3658414 134062 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 469 5 1 4 4.4 O=C(NC1CC(c2ccc(OC(F)(F)F)cc2)CN(C(=O)c2ccncc2)C1)c1ccccc1 nan
46931523 134311 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 474 5 1 4 4.2 CCc1ccc(C2CC(NC(=O)c3cccc(OC)c3)CN(C(=O)N3CCC(C#N)CC3)C2)cc1 nan
CHEMBL3662512 134311 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 474 5 1 4 4.2 CCc1ccc(C2CC(NC(=O)c3cccc(OC)c3)CN(C(=O)N3CCC(C#N)CC3)C2)cc1 nan
90663334 113435 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 807 20 9 7 2.0 CC(=O)N(c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143297 113435 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 807 20 9 7 2.0 CC(=O)N(c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143264 217928 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm960455s
44183021 140055 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 465 10 1 8 4.5 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(OCC4CC4)cc(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704456 140055 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 465 10 1 8 4.5 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(OCC4CC4)cc(C(C)(C)C)c3)c(=N)n2n1 nan
10184176 213782 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 477 5 3 3 5.4 CC(C)(C)C(=O)NCc1ccc(NC(=O)N2CCC[C@H]2[C@@H](O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL91441 213782 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 477 5 3 3 5.4 CC(C)(C)C(=O)NCc1ccc(NC(=O)N2CCC[C@H]2[C@@H](O)c2ccc(Cl)c(Cl)c2)cc1 10.1016/s0960-894x(01)00538-8
72547305 110649 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 335 3 0 2 5.3 O=C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091983 110649 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 335 3 0 2 5.3 O=C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44306349 109379 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304120 109379 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 804 18 7 8 5.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
11652756 139600 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
CHEMBL370151 139600 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
17187534 66775 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 316 5 2 2 4.3 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Cl)c1 10.1021/ml2002696
CHEMBL1734760 66775 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 316 5 2 2 4.3 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Cl)c1 10.1021/ml2002696
23631375 149392 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 449 3 1 4 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(N)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL389148 149392 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 449 3 1 4 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(N)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL3143317 217954 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
807100 82430 13 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 5 2 2 4.2 Cc1ccccc1C(=O)Nc1cccc(NC(=O)CC(C)C)c1 10.1021/ml2002696
CHEMBL2047300 82430 13 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 5 2 2 4.2 Cc1ccccc1C(=O)Nc1cccc(NC(=O)CC(C)C)c1 10.1021/ml2002696
44306659 109549 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL305188 109549 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 820 16 4 6 8.2 CSCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
58136855 140079 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 526 10 2 10 2.4 CCNC(=O)c1nn2/c(=N/C)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704480 140079 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 526 10 2 10 2.4 CCNC(=O)c1nn2/c(=N/C)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
23631810 99728 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 526 4 0 4 6.1 CC(C)C(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
CHEMBL244107 99728 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 526 4 0 4 6.1 CC(C)C(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
44187280 131920 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 412 9 1 7 3.2 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OC)cc(C(C)C)c1 nan
CHEMBL3644438 131920 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 412 9 1 7 3.2 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OC)cc(C(C)C)c1 nan
44432707 153441 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 379 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(C4CCCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL392370 153441 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 379 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(C4CCCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
12018758 16119 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL111241 16119 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 467 8 0 6 6.0 Clc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL3143269 217931 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None COc1ccc(C[C@H](NC(=O)[C@H](Cc2ccc(F)cc2)N(C(C)=O)C(=O)/C=C/c2ccccc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
58046049 140070 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 512 11 2 10 3.4 CCN(CC)c1nn2c(=N)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704471 140070 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 512 11 2 10 3.4 CCN(CC)c1nn2c(=N)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3143284 217939 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44418855 143338 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 3 6.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL373836 143338 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 3 6.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm061043e
44432711 94334 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 377 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccco4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL233546 94334 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 377 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccco4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44432843 94922 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 371 3 0 4 4.4 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)OC[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL234690 94922 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 371 3 0 4 4.4 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)OC[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
44309477 109995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 803 16 5 6 6.8 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCc1ccccc1 10.1016/s0960-894x(03)00325-1
CHEMBL308435 109995 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 803 16 5 6 6.8 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCc1ccccc1 10.1016/s0960-894x(03)00325-1
10077130 10779 53 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4047 10779 53 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
4870 10779 53 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
CHEMBL493982 10779 53 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
DB09030 10779 53 None - 1 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400235c
10300275 213652 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 493 8 3 3 6.0 CC[C@@H](C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL90698 213652 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 493 8 3 3 6.0 CC[C@@H](C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
44432774 152482 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL391625 152482 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
76313663 110642 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 424 4 0 3 6.0 CN(C)C(=S)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091976 110642 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 424 4 0 3 6.0 CN(C)C(=S)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
10120960 213647 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 578 9 4 5 4.5 CC(C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)c2ccc(S(N)(=O)=O)cc2)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL90682 213647 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 578 9 4 5 4.5 CC(C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)c2ccc(S(N)(=O)=O)cc2)cc1 10.1016/s0960-894x(01)00538-8
44338946 16078 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
CHEMBL110998 16078 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 493 10 0 8 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1OC 10.1016/s0960-894x(01)00745-4
44280936 123298 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 731 18 9 8 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33617 123298 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 731 18 9 8 1.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44432831 151696 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 291 2 0 3 3.2 O=C1OC[C@H]2[C@H](/C=C/c3ccccn3)c3ccccc3C[C@@H]12 10.1016/j.bmcl.2007.04.061
CHEMBL391025 151696 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 291 2 0 3 3.2 O=C1OC[C@H]2[C@H](/C=C/c3ccccn3)c3ccccc3C[C@@H]12 10.1016/j.bmcl.2007.04.061
44306065 210220 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 345 2 2 5 4.1 CC(C)(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL65778 210220 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 345 2 2 5 4.1 CC(C)(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
44409082 145271 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 405 4 0 4 5.7 CCOc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL377486 145271 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 405 4 0 4 5.7 CCOc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
44409083 83315 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 467 5 0 4 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL206110 83315 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 467 5 0 4 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
11559190 78878 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 340 3 1 4 4.1 CNc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197782 78878 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 340 3 1 4 4.1 CNc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44305882 209797 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 387 5 0 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N(C)C)nc(N(C)C)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL63305 209797 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 387 5 0 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N(C)C)nc(N(C)C)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
58045963 140069 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 499 11 2 10 3.4 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704470 140069 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 499 11 2 10 3.4 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
90663333 113434 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 843 23 9 8 2.4 CCCC(=O)c1ccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
CHEMBL3143296 113434 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 843 23 9 8 2.4 CCCC(=O)c1ccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
50910547 82571 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 350 5 2 2 4.7 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2C(F)(F)F)c1 10.1021/ml2002696
CHEMBL2048420 82571 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 350 5 2 2 4.7 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2C(F)(F)F)c1 10.1021/ml2002696
44432779 93464 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1cc(F)ccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL231713 93464 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1cc(F)ccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
23631185 99887 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 423 3 0 4 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244294 99887 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 423 3 0 4 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm070704k
59110452 80025 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(Cl)c2Cl)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012497 80025 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(Cl)c2Cl)cn1 10.1016/j.bmcl.2012.01.138
11611061 78845 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
CHEMBL197686 78845 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
44310323 211054 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 791 16 6 7 5.9 NCCCNC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL71246 211054 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 791 16 6 7 5.9 NCCCNC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
127050672 147590 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 491 5 2 5 3.8 CCN(C(=O)CN)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3818932 147590 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 491 5 2 5 3.8 CCN(C(=O)CN)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
90663321 113429 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 850 23 6 8 1.5 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143283 113429 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 850 23 6 8 1.5 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663342 113442 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 828 21 10 8 1.6 CC(=O)N(Oc1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143307 113442 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 828 21 10 8 1.6 CC(=O)N(Oc1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44432704 93807 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 399 3 0 3 6.0 Cc1nc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)ccc1-c1ccccc1 10.1016/j.bmcl.2007.06.002
CHEMBL232539 93807 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 399 3 0 3 6.0 Cc1nc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)ccc1-c1ccccc1 10.1016/j.bmcl.2007.06.002
44306708 107687 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL293867 107687 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 20 6 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44306698 109488 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304827 109488 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 826 15 5 6 7.4 O=C(Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)NC(Cc1c[nH]cn1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
10819322 211692 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL7610 211692 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44280804 106453 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284498 106453 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281069 124856 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 653 16 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34055 124856 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 653 16 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44186917 131918 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 466 10 1 7 4.1 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OCC2CC2)cc(C(C)(C)C)c1 nan
CHEMBL3644436 131918 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 466 10 1 7 4.1 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OCC2CC2)cc(C(C)(C)C)c1 nan
44432716 93471 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 377 3 1 4 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ncc[nH]4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231729 93471 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 377 3 1 4 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ncc[nH]4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44328579 214739 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 537 5 2 5 7.5 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(Cc3ccc(Cl)c(Cl)c3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
CHEMBL97110 214739 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 537 5 2 5 7.5 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(Cc3ccc(Cl)c(Cl)c3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
58136992 131917 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 484 11 1 8 4.1 CCOc1cc(C(=O)C[n+]2nc(N)n3nc(OC(CC)CC)ccc32)cc(C(C)(C)C)c1OCC nan
CHEMBL3644435 131917 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 484 11 1 8 4.1 CCOc1cc(C(=O)C[n+]2nc(N)n3nc(OC(CC)CC)ccc32)cc(C(C)(C)C)c1OCC nan
44432770 93718 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 469 3 0 3 6.6 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232332 93718 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 469 3 0 3 6.6 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
44418847 90203 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4C[C@H](O)CC[C@H]43)nc2)cc1 10.1021/jm061043e
CHEMBL219701 90203 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4C[C@H](O)CC[C@H]43)nc2)cc1 10.1021/jm061043e
11567556 175403 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
CHEMBL436130 175403 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
44432798 152239 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL391436 152239 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1ccc(Cl)cc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
44432817 161496 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 401 3 0 3 5.5 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL399820 161496 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 401 3 0 3 5.5 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
66701509 134308 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 473 3 1 2 5.3 C[C@@H]1CC[C@@H](C)N1C(=O)N1CC(NC(=O)c2ccccc2)CC(c2ccc(C(F)(F)F)cc2)C1 nan
CHEMBL3662509 134308 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 473 3 1 2 5.3 C[C@@H]1CC[C@@H](C)N1C(=O)N1CC(NC(=O)c2ccccc2)CC(c2ccc(C(F)(F)F)cc2)C1 nan
72547554 110655 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091989 110655 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
58136847 140061 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 471 11 2 10 2.3 COCCCOc1cc(C(=O)Cn2nc3c(C)cc(OCCO)nn3c2=N)cc(C(C)(C)C)c1 nan
CHEMBL3704462 140061 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 471 11 2 10 2.3 COCCCOc1cc(C(=O)Cn2nc3c(C)cc(OCCO)nn3c2=N)cc(C(C)(C)C)c1 nan
58136785 140078 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 483 9 2 10 2.3 Cc1cc(OCC2(C)COC2)nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc12 nan
CHEMBL3704479 140078 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 483 9 2 10 2.3 Cc1cc(OCC2(C)COC2)nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc12 nan
58137006 131925 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 551 10 1 9 4.1 CCC(CC)Oc1nn2c(N)n[n+](CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c2cc1C1CC1 nan
CHEMBL3644443 131925 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 551 10 1 9 4.1 CCC(CC)Oc1nn2c(N)n[n+](CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c2cc1C1CC1 nan
9875337 106023 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2Cl)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL281753 106023 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2Cl)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280650 121897 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(Cl)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33435 121897 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(Cl)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
3378161 82671 7 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 360 4 2 2 4.3 CC(C)C(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL2049121 82671 7 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 360 4 2 2 4.3 CC(C)C(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
11603083 77153 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 367 5 0 3 5.4 CCCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL194526 77153 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 367 5 0 3 5.4 CCCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44432717 153021 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 391 3 0 5 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cncn4C)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL392046 153021 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 391 3 0 5 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cncn4C)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44418844 90128 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4C[C@H](O)CC[C@H]43)nc2)c1 10.1021/jm061043e
CHEMBL219282 90128 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4C[C@H](O)CC[C@H]43)nc2)c1 10.1021/jm061043e
58045908 140071 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 513 12 2 10 3.5 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(CC)c1CC nan
CHEMBL3704472 140071 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 513 12 2 10 3.5 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)nc2c(CC)c1CC nan
44408873 83485 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL206502 83485 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
44408873 83485 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL206502 83485 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
44418850 90176 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 441 3 0 3 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL219522 90176 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 441 3 0 3 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm061043e
23631812 99908 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 484 4 0 5 4.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(S(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244315 99908 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 484 4 0 5 4.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(S(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
9886874 80019 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 393 4 0 3 5.8 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012491 80019 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 393 4 0 3 5.8 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2012.01.138
66761741 134309 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 509 3 1 4 3.1 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCS(=O)(=O)CC2)C1)c1ccccc1 nan
CHEMBL3662510 134309 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 509 3 1 4 3.1 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCS(=O)(=O)CC2)C1)c1ccccc1 nan
44432783 93736 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 437 3 0 3 5.8 O=C1OC[C@H]2[C@@H]1Cc1c(ccc(F)c1F)[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232348 93736 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 437 3 0 3 5.8 O=C1OC[C@H]2[C@@H]1Cc1c(ccc(F)c1F)[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
23631374 99731 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244109 99731 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
127053988 151257 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 486 4 0 6 4.3 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(S(C)(=O)=O)CC1(F)F nan
CHEMBL3906737 151257 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 486 4 0 6 4.3 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(S(C)(=O)=O)CC1(F)F nan
66761350 134063 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 405 4 2 3 3.3 Cc1ccc(C2CC(NC(=O)c3ccccc3)CN(C(=O)C3(N)CCC3)C2)cc1C nan
CHEMBL3658415 134063 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 405 4 2 3 3.3 Cc1ccc(C2CC(NC(=O)c3ccccc3)CN(C(=O)C3(N)CCC3)C2)cc1C nan
44416562 86778 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 373 2 0 3 5.6 CC1(C)OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL212788 86778 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 373 2 0 3 5.6 CC1(C)OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@@H]21 10.1016/j.bmcl.2006.06.042
44416690 87874 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 359 2 0 3 5.2 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL215579 87874 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 359 2 0 3 5.2 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
9847494 12620 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107920 12620 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 469 8 0 6 5.6 Fc1cc(F)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
44408616 81205 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 375 2 0 3 5.6 Cc1ccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL202678 81205 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 375 2 0 3 5.6 Cc1ccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2c1 10.1016/j.bmcl.2005.12.042
44416690 87874 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 359 2 0 3 5.2 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL215579 87874 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 359 2 0 3 5.2 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2007.06.002
11537143 78554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL196727 78554 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
11544606 78816 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 337 3 0 3 4.7 C=Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197618 78816 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 337 3 0 3 4.7 C=Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44416541 89242 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 373 3 0 3 5.6 CC[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL217611 89242 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 373 3 0 3 5.6 CC[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
11515660 78201 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 341 3 1 4 3.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(CO)n3)[C@H]12 10.1021/jm0502236
CHEMBL196002 78201 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 341 3 1 4 3.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(CO)n3)[C@H]12 10.1021/jm0502236
10925413 147478 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@H]3CCCC[C@@H]3C[C@@H]3C(=O)O[C@@H](C)[C@@H]32)n1 10.1021/jm0502236
CHEMBL381628 147478 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@H]3CCCC[C@@H]3C[C@@H]3C(=O)O[C@@H](C)[C@@H]32)n1 10.1021/jm0502236
44328728 214415 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 379 3 2 5 4.8 CC(C)(C)c1cc(C(=O)Cn2c(N)nc3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
CHEMBL95216 214415 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 379 3 2 5 4.8 CC(C)(C)c1cc(C(=O)Cn2c(N)nc3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
44280935 106865 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc(Cl)c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287368 106865 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 747 18 9 8 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc(Cl)c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44189604 131916 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 454 10 1 7 3.9 CCOCc1cc(C(=O)C[n+]2nc(N)n3nc(OC(CC)CC)ccc32)cc(C(C)(C)C)c1 nan
CHEMBL3644434 131916 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 454 10 1 7 3.9 CCOCc1cc(C(=O)C[n+]2nc(N)n3nc(OC(CC)CC)ccc32)cc(C(C)(C)C)c1 nan
23631639 99967 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.3 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
CHEMBL244485 99967 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.3 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
90663358 113446 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 903 22 9 8 3.1 CC(=O)N(C(=O)/C=C/c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143324 113446 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 903 22 9 8 3.1 CC(=O)N(C(=O)/C=C/c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
58045767 140075 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 9 2 9 2.8 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c(CC)c1C nan
CHEMBL3704476 140075 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 9 2 9 2.8 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c(CC)c1C nan
44408874 147026 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 395 2 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(Cl)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL380544 147026 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 395 2 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(Cl)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44432712 94335 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 393 3 0 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccs4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL233548 94335 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 393 3 0 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccs4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44418849 143748 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 6.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4Cl)cn3)[C@H]12 10.1021/jm061043e
CHEMBL374503 143748 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 6.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4Cl)cn3)[C@H]12 10.1021/jm061043e
23631813 156193 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 508 6 0 6 4.8 COCCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
CHEMBL394576 156193 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 508 6 0 6 4.8 COCCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
90663314 113424 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 984 28 11 11 0.6 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143274 113424 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 984 28 11 11 0.6 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
44309750 110350 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 779 15 5 7 6.3 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccco1 10.1016/s0960-894x(03)00325-1
CHEMBL308588 110350 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 779 15 5 7 6.3 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccco1 10.1016/s0960-894x(03)00325-1
90663330 113431 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1cccc(F)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143293 113431 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1cccc(F)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
137661486 166255 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4101591 166255 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
9810474 107933 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 719 19 7 8 2.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
CHEMBL295437 107933 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 719 19 7 8 2.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
9961058 106727 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 645 15 7 7 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(=O)c2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286382 106727 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 645 15 7 7 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(=O)c2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44826171 123644 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2[N+](=O)[O-])n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33818 123644 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2[N+](=O)[O-])n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280684 105914 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 594 15 7 6 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C1C=CC=NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL281079 105914 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 594 15 7 6 0.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C1C=CC=NC1=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9962227 106419 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 763 18 9 8 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284285 106419 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 763 18 9 8 2.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc3ccccc23)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280954 123326 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 633 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C1=COc2ccccc2O1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33630 123326 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 633 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C1=COc2ccccc2O1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
90663343 113443 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1cccc2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143308 113443 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1cccc2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
68075447 134058 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 375 3 1 4 2.2 CCc1ccc(C2CC(NC(=O)OC)CN(C(=O)N3CCOCC3)C2)cc1 nan
CHEMBL3658410 134058 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 375 3 1 4 2.2 CCc1ccc(C2CC(NC(=O)OC)CN(C(=O)N3CCOCC3)C2)cc1 nan
877874 30096 17 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL1332325 30096 17 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 346 4 2 2 4.1 CCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL3143254 217923 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm960455s
44137613 161303 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3978297 161303 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990813 161303 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
9890926 90063 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218933 90063 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
23631103 150935 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 4 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL390399 150935 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 4 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
127053948 153617 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 488 6 2 5 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NCCO)CC1(F)F nan
CHEMBL3925032 153617 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 488 6 2 5 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NCCO)CC1(F)F nan
66701371 134306 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 461 3 1 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCOCC2)C1)c1ccccc1 nan
CHEMBL3662507 134306 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 461 3 1 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCOCC2)C1)c1ccccc1 nan
66761956 134054 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 420 4 2 2 4.4 CCc1ccc(C2CC(NC(=O)Nc3ccccc3)CN(C(=O)N3CCCC3)C2)cc1 nan
CHEMBL3658407 134054 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 420 4 2 2 4.4 CCc1ccc(C2CC(NC(=O)Nc3ccccc3)CN(C(=O)N3CCCC3)C2)cc1 nan
CHEMBL3143310 217949 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@H](CCCN)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)NC(=O)/C=C/c1ccccc1 10.1021/jm960455s
117072551 147562 36 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 524 7 2 6 3.8 CCN(C(=O)CO)[C@H]1CN(/C(=N\C#N)Nc2cccc(OC(F)F)c2)N=C1c1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.5b01890
CHEMBL3818617 147562 36 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 524 7 2 6 3.8 CCN(C(=O)CO)[C@H]1CN(/C(=N\C#N)Nc2cccc(OC(F)F)c2)N=C1c1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.5b01890
58137003 131924 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 511 8 1 9 3.1 CCOc1nn2c(NC)n[n+](CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c2c(C)c1C nan
CHEMBL3644442 131924 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 511 8 1 9 3.1 CCOc1nn2c(NC)n[n+](CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c2c(C)c1C nan
9895920 106796 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 656 15 7 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cncc(Br)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286837 106796 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 656 15 7 6 1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cncc(Br)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
58045926 140073 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 512 9 2 10 2.0 CCNC(=O)c1nn2/c(=N/C)n(CC(=O)c3cc(OCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704474 140073 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 512 9 2 10 2.0 CCNC(=O)c1nn2/c(=N/C)n(CC(=O)c3cc(OCCO)c(OC)c(C(C)(C)C)c3)nc2c(C)c1C nan
44305942 209781 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 353 2 2 5 4.3 Cc1ccc2cc(Cn3ccc4c5c(N)nc(N)nc5ccc43)ccc2c1 10.1016/s0960-894x(99)00339-x
CHEMBL63192 209781 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 353 2 2 5 4.3 Cc1ccc2cc(Cn3ccc4c5c(N)nc(N)nc5ccc43)ccc2c1 10.1016/s0960-894x(99)00339-x
16046150 172632 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 459 5 2 3 6.2 C[C@@H](O)[C@@H]1[C@H](CO)C[C@@H]2CCCC[C@H]2[C@@H]1/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2006.06.042
CHEMBL424893 172632 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 459 5 2 3 6.2 C[C@@H](O)[C@@H]1[C@H](CO)C[C@@H]2CCCC[C@H]2[C@@H]1/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2006.06.042
70687427 80033 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(OC)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012506 80033 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(OC)c2)cn1 10.1016/j.bmcl.2012.01.138
68074840 134060 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 437 4 1 4 4.1 CCc1ccc(C2CC(OC(=O)Nc3ccccc3)CN(C(=O)N3CCOCC3)C2)cc1 nan
CHEMBL3658412 134060 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 437 4 1 4 4.1 CCc1ccc(C2CC(OC(=O)Nc3ccccc3)CN(C(=O)N3CCOCC3)C2)cc1 nan
23631376 159697 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 477 4 1 4 4.8 CCNC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
CHEMBL397480 159697 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 477 4 1 4 4.8 CCNC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
16214871 25090 3 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of PAR1-mediated aggregation of TRAP-stimulated human plateletInhibition of PAR1-mediated aggregation of TRAP-stimulated human platelet
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270738 25090 3 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of PAR1-mediated aggregation of TRAP-stimulated human plateletInhibition of PAR1-mediated aggregation of TRAP-stimulated human platelet
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cn1 10.1016/j.bmcl.2010.09.009
44306696 108906 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL302433 108906 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 16 5 6 6.7 NC(=O)CCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
17222608 82426 15 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 316 5 2 2 3.7 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Cl)c1 10.1021/ml2002696
CHEMBL2047284 82426 15 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 316 5 2 2 3.7 CCCNC(=O)c1cccc(NC(=O)c2ccccc2Cl)c1 10.1021/ml2002696
44281174 118246 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 498 11 6 7 0.2 C[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL32762 118246 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 498 11 6 7 0.2 C[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
58045878 140067 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 11 2 10 2.9 CCOc1cc(CC)c2nn(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704469 140067 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 11 2 10 2.9 CCOc1cc(CC)c2nn(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
10771636 113436 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143298 113436 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143281 217937 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3144093 217961 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)CSc1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
23631184 99726 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 423 3 0 4 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244103 99726 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 423 3 0 4 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm070704k
11690507 78879 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 429 4 0 3 6.9 CC(C)c1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
CHEMBL197783 78879 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 429 4 0 3 6.9 CC(C)c1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
11647382 141495 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 5 0 4 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(OCc4ccccc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371850 141495 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 5 0 4 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(OCc4ccccc4)cn3)[C@H]12 10.1021/jm0502236
46931634 134052 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 549 6 1 3 6.6 CCc1ccc(C2CC(NC(=O)c3ccc(-c4cccc(C(F)(F)F)c4)cn3)CN(C(=O)C3CCCC3)C2)cc1 nan
CHEMBL3658405 134052 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 549 6 1 3 6.6 CCc1ccc(C2CC(NC(=O)c3ccc(-c4cccc(C(F)(F)F)c4)cn3)CN(C(=O)C3CCCC3)C2)cc1 nan
9808447 109692 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 583 15 9 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL30612 109692 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 583 15 9 8 -0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
127053943 150179 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 424 3 1 5 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
CHEMBL3897962 150179 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 424 3 1 5 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
127053963 154274 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 7 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nnn(C)n2)CC1(F)F nan
CHEMBL3930471 154274 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 513 5 0 7 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nnn(C)n2)CC1(F)F nan
72547307 110646 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
CHEMBL3091980 110646 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
127053957 167100 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cocn2)CC1(F)F nan
CHEMBL4110608 167100 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2cocn2)CC1(F)F nan
127053971 167167 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2nccs2)CC1(F)F nan
CHEMBL4111197 167167 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 6 1 7 5.5 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2nccs2)CC1(F)F nan
127053993 153907 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 437 4 1 5 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CN)CC1(F)F nan
CHEMBL3927578 153907 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 437 4 1 5 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CN)CC1(F)F nan
121335547 154602 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 527 5 1 5 5.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccccc2)CC1(F)F nan
CHEMBL3932907 154602 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 527 5 1 5 5.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccccc2)CC1(F)F nan
127053974 167025 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 504 6 1 7 5.0 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2cocn2)CC1(F)F nan
CHEMBL4109959 167025 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 504 6 1 7 5.0 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2cocn2)CC1(F)F nan
117826535 160911 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 438 4 0 5 4.9 CO[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]1[C@@H](C)OC2=O nan
CHEMBL3985342 160911 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 438 4 0 5 4.9 CO[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]1[C@@H](C)OC2=O nan
127053956 167489 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2nccs2)CC1(F)F nan
CHEMBL4113709 167489 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 7 5.7 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2nccs2)CC1(F)F nan
72547556 110659 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091993 110659 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
127053981 151359 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 477 6 1 5 5.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC2CC2)CC1(F)F nan
CHEMBL3907652 151359 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 477 6 1 5 5.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC2CC2)CC1(F)F nan
127053950 154271 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 438 4 1 5 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CO)CC1(F)F nan
CHEMBL3930467 154271 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 438 4 1 5 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CO)CC1(F)F nan
121335737 158141 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 552 5 1 6 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2cccc(C#N)c2)CC1(F)F nan
CHEMBL3961310 158141 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 552 5 1 6 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2cccc(C#N)c2)CC1(F)F nan
127053940 160401 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 417 3 0 3 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3980810 160401 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 417 3 0 3 5.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
121335758 152473 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 534 5 1 7 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2nccs2)CC1(F)F nan
CHEMBL3916203 152473 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 534 5 1 7 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2nccs2)CC1(F)F nan
72547556 110659 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091993 110659 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 394 4 1 3 5.6 CC1(OC(N)=O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
121335739 151470 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 552 5 1 6 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccc(C#N)cc2)CC1(F)F nan
CHEMBL3908486 151470 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 552 5 1 6 5.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccc(C#N)cc2)CC1(F)F nan
CHEMBL3143249 217922 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
70685279 80022 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 389 4 0 3 5.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2C)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012494 80022 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 389 4 0 3 5.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2C)cn1 10.1016/j.bmcl.2012.01.138
70683199 80031 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 416 4 1 5 4.6 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012503 80031 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 416 4 1 5 4.6 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1016/j.bmcl.2012.01.138
10246587 78881 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197791 78881 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44432791 161416 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL399407 161416 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
44416542 148490 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 345 2 0 3 4.8 O=C1OC[C@H]2[C@@H](/C=C/c3ccc4ccccc4n3)[C@@H]3CCCCC3=C[C@@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL385694 148490 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 345 2 0 3 4.8 O=C1OC[C@H]2[C@@H](/C=C/c3ccc4ccccc4n3)[C@@H]3CCCCC3=C[C@@H]12 10.1016/j.bmcl.2006.06.042
23630914 150659 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 505 3 0 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CS(=O)(=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL390182 150659 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 505 3 0 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CS(=O)(=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
44309450 210838 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1cccc2c1c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
CHEMBL70013 210838 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1cccc2c1c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
44416588 87974 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 363 2 1 3 5.0 C[C@H]1O[C@@H](O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL215837 87974 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 363 2 1 3 5.0 C[C@H]1O[C@@H](O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
76309942 110654 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 3 5.8 CCOC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091988 110654 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 408 5 1 3 5.8 CCOC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44280767 121362 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 577 15 9 8 -1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33377 121362 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 577 15 9 8 -1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280877 123649 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 589 15 9 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33820 123649 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 589 15 9 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1016/s0960-894x(99)00197-3
9851501 124002 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33946 124002 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281081 126481 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34738 126481 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccc(N)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44584152 21669 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]thrombin from thrombin receptor in human platelet membraneDisplacement of [125I]thrombin from thrombin receptor in human platelet membrane
ChEMBL 602 7 5 9 3.3 O=S(=O)(O)OC(=C\c1cc(O)c(O)c(Br)c1)/C(=C\c1ccc(O)c(Br)c1)OS(=O)(=O)O 10.1021/np50120a023
CHEMBL1207950 21669 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]thrombin from thrombin receptor in human platelet membraneDisplacement of [125I]thrombin from thrombin receptor in human platelet membrane
ChEMBL 602 7 5 9 3.3 O=S(=O)(O)OC(=C\c1cc(O)c(O)c(Br)c1)/C(=C\c1ccc(O)c(Br)c1)OS(=O)(=O)O 10.1021/np50120a023
CHEMBL462733 21669 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]thrombin from thrombin receptor in human platelet membraneDisplacement of [125I]thrombin from thrombin receptor in human platelet membrane
ChEMBL 602 7 5 9 3.3 O=S(=O)(O)OC(=C\c1cc(O)c(O)c(Br)c1)/C(=C\c1ccc(O)c(Br)c1)OS(=O)(=O)O 10.1021/np50120a023
11611425 79019 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)cc1 10.1021/jm0502236
CHEMBL198175 79019 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)cc1 10.1021/jm0502236
58045970 140072 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 511 12 2 10 3.4 COc1c(OCCCCO)cc(C(=O)Cn2nc3c(C)cc(OCC4CC4)nn3c2=N)cc1C(C)(C)C nan
CHEMBL3704473 140072 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 511 12 2 10 3.4 COc1c(OCCCCO)cc(C(=O)Cn2nc3c(C)cc(OCC4CC4)nn3c2=N)cc1C(C)(C)C nan
44432720 154088 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 404 3 0 4 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc[n+]([O-])c4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL392905 154088 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 404 3 0 4 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc[n+]([O-])c4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44137613 161303 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3978297 161303 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990813 161303 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 584 11 2 8 4.2 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC(=O)O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3143309 217948 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)COc1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
23631186 99888 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 4 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4Cl)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244295 99888 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 457 3 0 4 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4Cl)cn3)[C@H]12 10.1021/jm070704k
70687424 80024 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 400 4 0 4 5.5 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012496 80024 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 400 4 0 4 5.5 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1016/j.bmcl.2012.01.138
46931416 134313 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 467 3 2 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)C1CCCC1 nan
CHEMBL3662514 134313 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 467 3 2 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)C1CCCC1 nan
9869359 93570 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 471 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1c(F)cc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232172 93570 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 471 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1c(F)cc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
90663293 113415 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 998 29 11 11 1.0 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CCC(N)=O 10.1021/jm960455s
CHEMBL3143252 113415 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 998 29 11 11 1.0 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CCC(N)=O 10.1021/jm960455s
72547551 110647 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
CHEMBL3091981 110647 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
72547308 110657 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091991 110657 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
11544845 140346 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 351 3 0 3 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(C4CC4)n3)[C@H]12 10.1021/jm0502236
CHEMBL371109 140346 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 351 3 0 3 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(C4CC4)n3)[C@H]12 10.1021/jm0502236
44187825 131923 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 453 6 1 8 2.2 CCc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(N2CCOCC2)c(OC)c(C(C)(C)C)c1 nan
CHEMBL3644441 131923 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 453 6 1 8 2.2 CCc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(N2CCOCC2)c(OC)c(C(C)(C)C)c1 nan
10227544 213305 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 477 7 3 3 5.4 CC(C)(C)C(=O)NCc1ccc(NC(=O)N(C[C@@H](O)c2ccc(Cl)c(Cl)c2)C2CC2)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL88513 213305 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 477 7 3 3 5.4 CC(C)(C)C(=O)NCc1ccc(NC(=O)N(C[C@@H](O)c2ccc(Cl)c(Cl)c2)C2CC2)cc1 10.1016/s0960-894x(01)00538-8
76309941 110638 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3091972 110638 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
11688420 142044 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1ccnc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)c1 10.1021/jm0502236
CHEMBL372591 142044 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1ccnc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)c1 10.1021/jm0502236
44338787 13665 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
CHEMBL108428 13665 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 469 8 0 6 5.6 Fc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1F 10.1016/s0960-894x(01)00745-4
44432719 93514 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccncc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231944 93514 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccncc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44409039 148058 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 460 3 1 4 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(NC(=O)C(C)(C)C)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL383216 148058 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 460 3 1 4 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(NC(=O)C(C)(C)C)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44416654 87191 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 407 4 0 4 5.7 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)O[C@@H](OC)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL214575 87191 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 407 4 0 4 5.7 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)O[C@@H](OC)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
58045981 140074 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 8 2 9 3.0 Cc1c(OC(C)C)nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c1C nan
CHEMBL3704475 140074 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 8 2 9 3.0 Cc1c(OC(C)C)nn2c(=N)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c1C nan
44409077 83377 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 480 4 1 4 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(NC(=O)c5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL206325 83377 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 480 4 1 4 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(NC(=O)c5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
23630913 99886 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 473 3 0 4 6.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CSCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244290 99886 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 473 3 0 4 6.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CSCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
59110450 80018 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 393 4 0 3 5.8 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2F)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012490 80018 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 393 4 0 3 5.8 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2F)cn1 10.1016/j.bmcl.2012.01.138
44432718 93512 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccn4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231942 93512 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccn4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
9908345 93513 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccnc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231943 93513 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 388 3 0 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccnc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
9844209 79122 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm0502236
CHEMBL198473 79122 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm0502236
90663360 113448 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 795 21 9 9 1.2 CC(=O)N(Oc1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143326 113448 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 795 21 9 9 1.2 CC(=O)N(Oc1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
72547306 110639 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 337 3 1 2 5.1 OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091973 110639 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 337 3 1 2 5.1 OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
9853816 104112 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL269345 104112 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
49766546 82575 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 358 6 2 2 5.3 CCCC(=O)Nc1cccc(NC(=O)c2cccc(-c3ccccc3)c2)c1 10.1021/ml2002696
CHEMBL2048430 82575 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 358 6 2 2 5.3 CCCC(=O)Nc1cccc(NC(=O)c2cccc(-c3ccccc3)c2)c1 10.1021/ml2002696
44280608 106879 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 731 18 9 8 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(F)=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287468 106879 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 731 18 9 8 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(F)=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44309838 103327 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1cccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c12)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
CHEMBL262932 103327 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1cccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c12)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
44339001 116267 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
CHEMBL322093 116267 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1ccccc1-c1cc(N(CCCN2CCCCCC2)Cc2ccc3c(c2)OCO3)on1 10.1016/s0960-894x(01)00745-4
23631554 99966 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.3 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
CHEMBL244484 99966 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.3 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
44432842 152091 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 399 3 0 4 5.2 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)OC(C)(C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL391324 152091 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 399 3 0 4 5.2 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)OC(C)(C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
44432771 161613 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 469 3 0 3 6.6 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL400435 161613 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 469 3 0 3 6.6 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
70687423 80015 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 445 5 0 3 6.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1CCc1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012487 80015 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 445 5 0 3 6.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1CCc1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2012.01.138
53245483 82667 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 394 5 2 2 5.1 CCCC(=O)Nc1cccc(NC(=O)c2c(Cl)cccc2Br)c1 10.1021/ml2002696
CHEMBL2049116 82667 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 394 5 2 2 5.1 CCCC(=O)Nc1cccc(NC(=O)c2c(Cl)cccc2Br)c1 10.1021/ml2002696
90663338 113438 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 833 22 9 9 1.8 C=CC(=O)c1ccsc1N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143302 113438 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 833 22 9 9 1.8 C=CC(=O)c1ccsc1N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143246 217920 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC#Cc1ccccc1C(=O)N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143249 217922 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
9934461 143537 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL374106 143537 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
44309461 210590 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 795 15 5 7 6.8 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1cccs1 10.1016/s0960-894x(03)00325-1
CHEMBL68372 210590 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 795 15 5 7 6.8 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1cccs1 10.1016/s0960-894x(03)00325-1
76331784 110653 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 336 3 1 2 5.1 NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091987 110653 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 336 3 1 2 5.1 NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
76324547 110656 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 404 5 1 2 5.6 O=C(NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)C1CC1 10.1021/ml400235c
CHEMBL3091990 110656 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 404 5 1 2 5.6 O=C(NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)C1CC1 10.1021/ml400235c
44306903 109029 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303157 109029 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 809 18 6 7 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44280683 106181 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL282733 106181 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 593 15 8 7 0.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281070 119125 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 633 15 7 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2s1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL32941 119125 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 633 15 7 6 2.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2s1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
90663339 113439 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 883 21 9 8 3.1 CC(=O)N(C(=O)c1cccc(C2CCCCC2)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143303 113439 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 883 21 9 8 3.1 CC(=O)N(C(=O)c1cccc(C2CCCCC2)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
58045960 140077 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 453 7 1 8 4.1 CCOc1nn2c(=N)n(CC(=O)c3cc(C(C)(C)C)cc(C(C)(C)OC)c3)nc2c(C)c1C nan
CHEMBL3704478 140077 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 453 7 1 8 4.1 CCOc1nn2c(=N)n(CC(=O)c3cc(C(C)(C)C)cc(C(C)(C)OC)c3)nc2c(C)c1C nan
46931633 134055 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 433 5 1 2 5.0 CCc1ccc(C2CC(NC(=O)N(C)c3ccccc3)CN(C(=O)C3CCCC3)C2)cc1 nan
CHEMBL3658408 134055 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 433 5 1 2 5.0 CCc1ccc(C2CC(NC(=O)N(C)c3ccccc3)CN(C(=O)C3CCCC3)C2)cc1 nan
10557086 113425 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143276 113425 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccsc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10747898 113476 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143683 113476 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 798 20 11 7 1.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143311 217950 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143320 217956 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None C/C=C/C=C/CC(=O)N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
60003490 80016 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012488 80016 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2012.01.138
9804049 140341 2 None - 1 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371069 140341 2 None - 1 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
44306697 109509 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304924 109509 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 846 17 6 6 6.9 NC(=O)NCCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44280949 109491 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 651 15 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc2c(c1)-c1ccccc1-2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL30484 109491 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 651 15 7 5 3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc2c(c1)-c1ccccc1-2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44281079 123998 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(Cl)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33945 123998 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(Cl)nc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
58045994 140057 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 458 5 1 9 2.7 COc1c(N2CCOCC2)cc(C(=O)Cn2nc3ccc(Cl)nn3c2=N)cc1C(C)(C)C nan
CHEMBL3704458 140057 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 458 5 1 9 2.7 COc1c(N2CCOCC2)cc(C(=O)Cn2nc3ccc(Cl)nn3c2=N)cc1C(C)(C)C nan
44290206 180321 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 763 20 7 8 3.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(C)c2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL45317 180321 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 763 20 7 8 3.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(C)c2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
44290207 180324 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 729 19 7 8 2.1 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL45318 180324 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 729 19 7 8 2.1 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL3143313 217951 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
46931630 134059 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 454 7 1 3 4.2 CCc1ccc(C2CC(NS(=O)(=O)Cc3ccccc3)CN(C(=O)C3CCCC3)C2)cc1 nan
CHEMBL3658411 134059 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 454 7 1 3 4.2 CCc1ccc(C2CC(NS(=O)(=O)Cc3ccccc3)CN(C(=O)C3CCCC3)C2)cc1 nan
9897054 109934 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 773 16 5 7 5.9 CSCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN 10.1016/s0960-894x(03)00325-1
CHEMBL308050 109934 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 773 16 5 7 5.9 CSCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN 10.1016/s0960-894x(03)00325-1
11803290 113426 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143277 113426 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 10 8 0.8 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663316 113427 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 1002 28 11 11 0.7 CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143278 113427 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 1002 28 11 11 0.7 CC(=O)N(C(=O)/C=C/c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
70854697 134312 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 476 3 1 4 3.4 Cc1cccc(C(=O)NC2CC(c3ccc(C(F)(F)F)cc3)CN(C(=O)N3CCOCC3)C2)n1 nan
CHEMBL3662513 134312 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 476 3 1 4 3.4 Cc1cccc(C(=O)NC2CC(c3ccc(C(F)(F)F)cc3)CN(C(=O)N3CCOCC3)C2)n1 nan
44409057 147976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 510 6 1 5 6.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)Nc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL382830 147976 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 510 6 1 5 6.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)Nc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
23631105 148799 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 407 3 0 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm070704k
CHEMBL387603 148799 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 407 3 0 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm070704k
23631464 159706 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 590 5 0 5 7.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)OCc4ccccc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL397491 159706 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 590 5 0 5 7.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)OCc4ccccc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
59110475 80020 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 0 3 6.3 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2Cl)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012492 80020 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 0 3 6.3 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2Cl)cn1 10.1016/j.bmcl.2012.01.138
11583548 79090 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 465 3 0 3 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Br)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL198375 79090 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 465 3 0 3 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Br)c4)cn3)[C@H]12 10.1021/jm0502236
11502485 175845 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 412 3 0 4 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL439681 175845 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 412 3 0 4 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@H]12 10.1021/jm0502236
44339173 14996 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL109226 14996 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
11610042 140382 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 353 4 0 3 5.1 CCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL371294 140382 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 353 4 0 3 5.1 CCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
58045796 140063 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 11 1 10 2.9 CCOc1cc(C)c2nn(CC(=O)c3cc(OC(COC)COC)cc(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704464 140063 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 11 1 10 2.9 CCOc1cc(C)c2nn(CC(=O)c3cc(OC(COC)COC)cc(C(C)(C)C)c3)c(=N)n2n1 nan
44306657 109036 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL303187 109036 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 861 19 6 8 6.2 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306403 209641 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL62584 209641 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2ccccc2C)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
44280805 106552 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 567 15 7 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccoc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285186 106552 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 567 15 7 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccoc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
58045925 140066 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 515 11 3 11 2.6 CCOc1cc(C(C)(C)O)c2nn(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704468 140066 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 515 11 3 11 2.6 CCOc1cc(C(C)(C)O)c2nn(CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
11803426 113475 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 793 20 10 7 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143682 113475 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 793 20 10 7 1.4 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccc(Cl)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10459564 7305 41 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
4048 7305 41 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
CHEMBL2103856 7305 41 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
DB12046 7305 41 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
23631104 99635 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 407 3 0 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL243913 99635 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 407 3 0 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm070704k
23631106 99725 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 425 3 0 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4F)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244102 99725 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 425 3 0 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3COCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4F)cn3)[C@H]12 10.1021/jm070704k
72547552 110660 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3091994 110660 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
127053982 152445 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 465 4 1 5 4.4 CC(=O)N[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)C1[C@@H](C)OC2=O nan
CHEMBL3915979 152445 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 465 4 1 5 4.4 CC(=O)N[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)C1[C@@H](C)OC2=O nan
11582568 147673 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm0502236
CHEMBL382104 147673 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 421 3 0 3 6.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4Cl)cn3)[C@H]12 10.1021/jm0502236
90663297 113417 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143256 113417 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1cccs1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
10276545 15918 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL110024 15918 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 463 9 0 7 5.4 COc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
1048267 39202 92 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL1411333 39202 92 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 360 5 2 2 4.4 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
44306540 209815 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL63402 209815 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 795 18 6 7 5.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44306499 210124 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL65004 210124 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 815 22 6 7 5.9 CCN(CC)Cc1cn(Cc2cccc(C)c2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc3ccccc3)ccc12 10.1016/s0960-894x(01)00378-x
44280905 106853 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 646 15 7 6 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc(Cl)c(Cl)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287270 106853 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 646 15 7 6 2.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc(Cl)c(Cl)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44306066 107411 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 333 4 2 6 3.2 CCOc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL292032 107411 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 333 4 2 6 3.2 CCOc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
44432706 93511 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 339 3 0 3 4.7 CCc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1016/j.bmcl.2007.06.002
CHEMBL231938 93511 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 339 3 0 3 4.7 CCc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1016/j.bmcl.2007.06.002
50910549 82427 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 362 4 2 3 4.3 CCOC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL2047286 82427 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 362 4 2 3 4.3 CCOC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
59110483 80027 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 1 4 4.9 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012499 80027 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 1 4 4.9 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2012.01.138
9865055 78073 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 387 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL195729 78073 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 387 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
9865055 78073 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 387 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL195729 78073 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 387 3 0 3 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL3143248 217921 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)CCCN)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44290102 108085 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 820 21 8 9 2.5 CC(C)C(N)C(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL296565 108085 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 820 21 8 9 2.5 CC(C)C(N)C(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
44290300 185275 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 798 21 8 9 2.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC2CCCCC2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL46658 185275 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 798 21 8 9 2.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC2CCCCC2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
44280835 106880 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 573 15 10 9 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287469 106880 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 573 15 10 9 -1.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1c[nH]cn1)C(N)=O 10.1016/s0960-894x(99)00197-3
44409228 147449 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 520 6 1 6 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCCNC(=O)OC(C)(C)C)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL381506 147449 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 520 6 1 6 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCCNC(=O)OC(C)(C)C)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44182739 131257 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 510 9 1 10 3.6 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3640033 131257 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 510 9 1 10 3.6 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
11432492 161342 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3912154 161342 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3991167 161342 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3143271 217933 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143282 217938 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44409034 82179 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 446 5 1 4 6.0 CCCC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL203992 82179 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 446 5 1 4 6.0 CCCC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
44418854 89447 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 441 3 0 3 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm061043e
CHEMBL217958 89447 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 441 3 0 3 6.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm061043e
44418838 90196 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL219643 90196 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm061043e
16100352 143709 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@H]3[C@@H](CCC[C@H]3O)[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL374265 143709 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@H]3[C@@H](CCC[C@H]3O)[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
59110442 80021 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 0 3 6.3 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012493 80021 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 409 4 0 3 6.3 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2012.01.138
11661666 147349 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
CHEMBL381226 147349 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 417 4 0 4 5.8 COc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)c1 10.1021/jm0502236
76317165 110640 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 427 6 0 2 7.3 Fc1cccc(-c2ccc(/C=C/[C@H]3C(OCc4ccccc4)C[C@@H]4CCCC[C@@H]43)nc2)c1 10.1021/ml400235c
CHEMBL3091974 110640 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 427 6 0 2 7.3 Fc1cccc(-c2ccc(/C=C/[C@H]3C(OCc4ccccc4)C[C@@H]4CCCC[C@@H]43)nc2)c1 10.1021/ml400235c
44432705 93969 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 413 4 0 3 6.2 CCc1nc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)ccc1-c1ccccc1 10.1016/j.bmcl.2007.06.002
CHEMBL232726 93969 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 413 4 0 3 6.2 CCc1nc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)ccc1-c1ccccc1 10.1016/j.bmcl.2007.06.002
1047178 214938 5 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 490 6 2 6 5.6 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(CCN3CCCCC3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
CHEMBL98231 214938 5 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 490 6 2 6 5.6 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(CCN3CCCCC3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
10628873 113411 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 749 20 10 8 0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccoc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143247 113411 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 749 20 10 8 0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)c1ccoc1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
66761216 134048 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 410 6 1 2 4.8 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)C(C)(C)CF)C2)cc1 nan
CHEMBL3658401 134048 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 410 6 1 2 4.8 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)C(C)(C)CF)C2)cc1 nan
11249717 161218 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3903962 161218 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990074 161218 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
44432775 93804 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232536 93804 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
11618945 147473 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 435 5 1 5 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL381593 147473 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 435 5 1 5 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44432708 94161 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 380 3 0 4 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL233343 94161 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 380 3 0 4 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44339002 16122 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111258 16122 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 447 8 0 6 5.7 Cc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
44409278 84411 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 6 1 5 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)NC5CC5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL208835 84411 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 6 1 5 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)NC5CC5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
50910548 82429 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 374 5 2 2 4.7 CC(C)CC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL2047299 82429 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 374 5 2 2 4.7 CC(C)CC(=O)Nc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
44281080 106698 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286211 106698 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 592 15 8 6 1.3 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(N)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
90663332 113433 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1ccc2ccccc2c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143295 113433 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 865 21 9 8 2.1 CC(=O)N(C(=O)Cc1ccc2ccccc2c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
23631640 175530 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 485 4 0 6 5.1 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
CHEMBL437171 175530 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 485 4 0 6 5.1 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
127053980 150173 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 517 6 1 7 4.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2nccn2C)CC1(F)F nan
CHEMBL3897916 150173 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 517 6 1 7 4.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2nccn2C)CC1(F)F nan
121335755 151760 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 562 5 1 6 5.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccc(Cl)nc2)CC1(F)F nan
CHEMBL3910807 151760 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 562 5 1 6 5.7 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2ccc(Cl)nc2)CC1(F)F nan
121335757 160993 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 545 5 1 5 5.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2cccc(F)c2)CC1(F)F nan
CHEMBL3985965 160993 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 545 5 1 5 5.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)c2cccc(F)c2)CC1(F)F nan
127053954 167486 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 5 1 6 5.6 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ccccn2)CC1(F)F nan
CHEMBL4113629 167486 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 5 1 6 5.6 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ccccn2)CC1(F)F nan
127053978 151281 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2ccccn2)CC1(F)F nan
CHEMBL3906932 151281 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2ccccn2)CC1(F)F nan
127053964 156220 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 476 4 0 8 3.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(n2cnnn2)CC1(F)F nan
CHEMBL3945945 156220 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 476 4 0 8 3.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(n2cnnn2)CC1(F)F nan
127053958 167637 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ncco2)CC1(F)F nan
CHEMBL4114937 167637 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 7 5.2 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(O)c2ncco2)CC1(F)F nan
127053959 151606 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 456 4 0 4 6.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(CC#N)CC1(F)F nan
CHEMBL3909563 151606 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 456 4 0 4 6.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(CC#N)CC1(F)F nan
127053990 159273 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 437 3 1 5 4.5 Cc1cccc(-c2ccc(/C=C/[C@@H]3C4[C@@H](C)OC(=O)[C@]4(N)CC(F)(F)[C@H]3C)nc2)c1C#N nan
CHEMBL3971211 159273 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 437 3 1 5 4.5 Cc1cccc(-c2ccc(/C=C/[C@@H]3C4[C@@H](C)OC(=O)[C@]4(N)CC(F)(F)[C@H]3C)nc2)c1C#N nan
127053953 167579 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 5 5.1 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NC2CCC2)CC1(F)F nan
CHEMBL4114406 167579 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 505 5 1 5 5.1 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NC2CCC2)CC1(F)F nan
121335756 160063 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 532 5 1 7 5.0 Cc1cc(C(=O)N[C@@]23CC(F)(F)[C@@H](C)[C@H](/C=C/c4ccc(-c5ccccc5C#N)cn4)[C@@H]2[C@@H](C)OC3=O)no1 nan
CHEMBL3977807 160063 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 532 5 1 7 5.0 Cc1cc(C(=O)N[C@@]23CC(F)(F)[C@@H](C)[C@H](/C=C/c4ccc(-c5ccccc5C#N)cn4)[C@@H]2[C@@H](C)OC3=O)no1 nan
127053946 160380 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 459 4 0 5 4.9 COC(=O)[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)C1[C@@H](C)OC2=O nan
CHEMBL3980639 160380 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 459 4 0 5 4.9 COC(=O)[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)C1[C@@H](C)OC2=O nan
121335541 149501 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 491 5 1 5 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)C2CC2)CC1(F)F nan
CHEMBL3892331 149501 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 491 5 1 5 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)C2CC2)CC1(F)F nan
127053986 166718 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 531 5 1 7 4.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@@]2(NC(=O)c2ccn(C)n2)CC1(F)F nan
CHEMBL4107269 166718 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 531 5 1 7 4.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@@]2(NC(=O)c2ccn(C)n2)CC1(F)F nan
127053972 167676 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2ccncc2)CC1(F)F nan
CHEMBL4115204 167676 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2ccncc2)CC1(F)F nan
127050673 147556 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 506 6 1 5 4.5 CCN(C(=O)COC)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3818510 147556 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 506 6 1 5 4.5 CCN(C(=O)COC)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
127050934 147586 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 404 7 2 5 1.8 CCCCN/C(=N/C#N)N1CC(N(CC)C(=O)CO)C(c2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01890
CHEMBL3818898 147586 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 404 7 2 5 1.8 CCCCN/C(=N/C#N)N1CC(N(CC)C(=O)CO)C(c2ccc(Cl)cc2)=N1 10.1021/acs.jmedchem.5b01890
11432492 161342 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3912154 161342 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3991167 161342 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 526 9 2 7 4.4 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCNCC3)c(OC)c(C(C)(C)C)c1)C2 nan
44409232 82686 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 376 2 1 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(N)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL204955 82686 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 376 2 1 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(N)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44305776 107416 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR1 (unknown origin) assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 (unknown origin) assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 331 3 2 5 3.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1039/c4md00485j
CHEMBL292089 107416 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR1 (unknown origin) assessed as inhibition of thrombin-induced platelet aggregationAntagonist activity at PAR1 (unknown origin) assessed as inhibition of thrombin-induced platelet aggregation
ChEMBL 331 3 2 5 3.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1039/c4md00485j
11537143 78554 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
CHEMBL196727 78554 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
44409076 147329 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 443 3 0 4 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5cccs5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL381121 147329 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 443 3 0 4 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5cccs5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44409033 148104 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 505 3 0 3 7.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5cccc(C(F)(F)F)c5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL383479 148104 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 505 3 0 3 7.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5cccc(C(F)(F)F)c5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44306762 209879 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL63966 209879 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 817 17 5 6 7.5 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
11537143 78554 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL196727 78554 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 325 2 0 3 4.4 Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44305776 107416 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 331 3 2 5 3.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL292089 107416 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 331 3 2 5 3.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
50910530 82669 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 5 2 2 4.3 CCCC(=O)Nc1cccc(NC(=O)c2c(C)cccc2C)c1 10.1021/ml2002696
CHEMBL2049118 82669 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 5 2 2 4.3 CCCC(=O)Nc1cccc(NC(=O)c2c(C)cccc2C)c1 10.1021/ml2002696
44280660 106654 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 617 15 7 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285915 106654 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 617 15 7 6 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2o1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280651 122211 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 781 18 9 8 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33506 122211 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 781 18 9 8 2.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccc(C(F)(F)F)cc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
9831601 107259 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 704 17 6 7 3.5 CC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
CHEMBL290927 107259 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 704 17 6 7 3.5 CC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
10077130 10779 53 None - 1 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4047 10779 53 None - 1 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4870 10779 53 None - 1 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
CHEMBL493982 10779 53 None - 1 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
DB09030 10779 53 None - 1 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
44432767 93766 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 453 3 0 3 6.0 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232372 93766 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 453 3 0 3 6.0 O=C1OC[C@H]2[C@@H]1Cc1ccc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
44309777 211094 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 810 17 5 7 6.0 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
CHEMBL71444 211094 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 810 17 5 7 6.0 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
90663340 113440 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1ccsc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143304 113440 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 779 20 9 8 1.4 CC(=O)N(c1ccsc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306660 210602 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
CHEMBL68458 210602 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 797 20 6 7 5.6 CCN(CC)Cc1cn(Cc2ccc(F)cc2)c2cc(NC(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC3CCCCC3)ccc12 10.1016/s0960-894x(01)00378-x
9960837 122311 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 629 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33532 122311 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 629 15 7 7 1.7 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cnc2ccccc2n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280607 174630 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 789 19 9 8 3.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(=C/c2ccccc2)c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL430930 174630 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 789 19 9 8 3.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C(=C/c2ccccc2)c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280667 109723 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 738 18 9 9 1.4 N#Cc1ccc(/C=C/C(=O)Nc2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n[nH]2)cc1 10.1016/s0960-894x(99)00197-3
CHEMBL30635 109723 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 738 18 9 9 1.4 N#Cc1ccc(/C=C/C(=O)Nc2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n[nH]2)cc1 10.1016/s0960-894x(99)00197-3
1361448 82668 7 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 350 5 2 2 5.0 CCCC(=O)Nc1cccc(NC(=O)c2cccc(Cl)c2Cl)c1 10.1021/ml2002696
CHEMBL2049117 82668 7 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 350 5 2 2 5.0 CCCC(=O)Nc1cccc(NC(=O)c2cccc(Cl)c2Cl)c1 10.1021/ml2002696
44432840 94921 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)O[C@@H](C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL234688 94921 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)O[C@@H](C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL3143270 217932 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306894 109489 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304829 109489 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 806 18 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4cccc(C)c4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
44305944 109014 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 373 5 1 5 4.9 CNc1nc(N(C)C)nc2ccc3c(ccn3Cc3ccc(C(C)C)cc3)c12 10.1016/s0960-894x(99)00339-x
CHEMBL303084 109014 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 373 5 1 5 4.9 CNc1nc(N(C)C)nc2ccc3c(ccn3Cc3ccc(C(C)C)cc3)c12 10.1016/s0960-894x(99)00339-x
11509594 76453 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)cc1 10.1021/jm0502236
CHEMBL193537 76453 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 3 0 3 6.1 Cc1ccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc2)cc1 10.1021/jm0502236
11702885 77168 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 341 3 0 4 4.1 COc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
CHEMBL194533 77168 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 341 3 0 4 4.1 COc1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
44432778 152755 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL391833 152755 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 435 3 0 3 6.2 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
76328107 110658 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 351 3 1 2 5.5 CC1(O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091992 110658 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 351 3 1 2 5.5 CC1(O)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
59110479 80029 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 405 4 1 4 5.0 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2C)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012501 80029 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 405 4 1 4 5.0 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2C)cn1 10.1016/j.bmcl.2012.01.138
2858257 119379 12 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 483 5 2 5 6.5 Cc1ccc(Cn2c(=N)n(CC(=O)c3cc(C(C)(C)C)c(O)c(C(C)(C)C)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00555-8
CHEMBL330204 119379 12 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 483 5 2 5 6.5 Cc1ccc(Cn2c(=N)n(CC(=O)c3cc(C(C)(C)C)c(O)c(C(C)(C)C)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00555-8
71736053 150652 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 532 5 1 7 5.0 Cc1oncc1C(=O)N[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]1[C@@H](C)OC2=O nan
CHEMBL3901770 150652 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 532 5 1 7 5.0 Cc1oncc1C(=O)N[C@@]12CC(F)(F)[C@@H](C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)[C@@H]1[C@@H](C)OC2=O nan
23631275 99889 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 461 4 0 6 4.4 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3ccccn3)cn2)C1 10.1021/jm070704k
CHEMBL244298 99889 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 461 4 0 6 4.4 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3ccccn3)cn2)C1 10.1021/jm070704k
66761314 134307 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 475 3 2 3 3.9 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)c1ccccc1 nan
CHEMBL3662508 134307 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 475 3 2 3 3.9 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)c1ccccc1 nan
44309751 109935 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccn1 10.1016/s0960-894x(03)00325-1
CHEMBL308052 109935 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccn1 10.1016/s0960-894x(03)00325-1
44432786 93472 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1cccc(F)c1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL231732 93472 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1cccc(F)c1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
44432710 161642 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 471 4 0 5 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCN(c5ccccc5)CC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL400634 161642 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 471 4 0 5 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCN(c5ccccc5)CC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44306611 210381 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL66958 210381 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 775 18 6 7 4.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL3143266 217929 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(C)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143279 217936 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCN=C(N(C)C)N(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143315 217952 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
51003683 82428 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL2047297 82428 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL4227548 82428 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 346 6 2 2 4.9 CCCCNc1cccc(NC(=O)c2ccccc2Br)c1 10.1021/ml2002696
CHEMBL3143287 217940 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@H](Cc1cccnc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
127053992 157381 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 1 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3-c3nnn[nH]3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3955189 157381 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 1 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3-c3nnn[nH]3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
44309958 211088 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 795 15 5 7 6.5 NCCNC(=O)[C@H](Cc1cccs1)NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL71411 211088 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 795 15 5 7 6.5 NCCNC(=O)[C@H](Cc1cccs1)NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL3143268 217930 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CCCCC/C=C/CC(=O)N(C(C)=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
70685280 80030 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 405 4 1 4 5.0 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012502 80030 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 405 4 1 4 5.0 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C)c2)cn1 10.1016/j.bmcl.2012.01.138
11697104 78918 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL197903 78918 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm0502236
90663341 113441 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143306 113441 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccc(F)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44432692 95013 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 323 2 0 3 4.3 Cc1cccc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)n1 10.1016/j.bmcl.2007.06.002
CHEMBL234804 95013 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 323 2 0 3 4.3 Cc1cccc(/C=C/[C@H]2[C@@H]3CCCCC3=C[C@H]3C(=O)O[C@H](C)[C@@H]23)n1 10.1016/j.bmcl.2007.06.002
44416563 145191 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 341 3 1 3 4.5 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)O[C@@H](O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
CHEMBL377378 145191 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 341 3 1 3 4.5 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)O[C@@H](O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
44306658 108972 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 835 19 6 9 5.0 COC(=O)c1ccc(Cn2cc(CN3CCCC3)c3ccc(NC(=O)N[C@@H](Cc4ccc(OC)cc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC4CCCCC4)cc32)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL302823 108972 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 835 19 6 9 5.0 COC(=O)c1ccc(Cn2cc(CN3CCCC3)c3ccc(NC(=O)N[C@@H](Cc4ccc(OC)cc4)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC4CCCCC4)cc32)cc1 10.1016/s0960-894x(01)00378-x
11703925 147902 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 395 7 0 3 6.2 CCCCCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL382733 147902 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 395 7 0 3 6.2 CCCCCCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
66701444 134053 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 384 4 1 2 4.3 CCc1ccc(C2CC(NC(=O)C(C)(C)C)CN(C(=O)C3CCCC3)C2)cc1 nan
CHEMBL3658406 134053 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 384 4 1 2 4.3 CCc1ccc(C2CC(NC(=O)C(C)(C)C)CN(C(=O)C3CCCC3)C2)cc1 nan
3751851 214895 10 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 435 6 2 5 5.9 CCCCn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
CHEMBL97952 214895 10 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 435 6 2 5 5.9 CCCCn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
44432713 152758 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 427 3 0 4 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(Cl)s4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL391834 152758 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 427 3 0 4 6.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(Cl)s4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
76317166 110652 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 456 5 1 3 7.3 O=C(Nc1ccccc1)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091986 110652 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 456 5 1 3 7.3 O=C(Nc1ccccc1)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44432691 95012 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 309 2 0 3 4.0 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccccn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL234803 95012 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 309 2 0 3 4.0 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccccn3)[C@H]12 10.1016/j.bmcl.2007.06.002
58136821 140065 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 8 1 9 2.6 CCOc1nn2/c(=N/C)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704467 140065 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 455 8 1 9 2.6 CCOc1nn2/c(=N/C)n(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL4115741 219690 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL None None None None nan
11718309 77356 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 4 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(Cc4ccccc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL194920 77356 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 4 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(Cc4ccccc4)cn3)[C@H]12 10.1021/jm0502236
16100350 143553 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 491 3 0 3 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL374122 143553 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 491 3 0 3 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC(F)(F)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
23631279 150232 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 524 4 0 4 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL389835 150232 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 524 4 0 4 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
90663302 113420 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 9 7 1.1 CC(=O)N(C1CCCC1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143262 113420 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 765 20 9 7 1.1 CC(=O)N(C1CCCC1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143259 217925 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
23630915 99965 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 489 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[S+]([O-])CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244483 99965 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 489 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[S+]([O-])CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
44416717 87354 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 343 5 2 3 4.1 CCc1cccc(/C=C/[C@@H]2[C@H]([C@@H](C)O)[C@H](CO)C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
CHEMBL214956 87354 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 343 5 2 3 4.1 CCc1cccc(/C=C/[C@@H]2[C@H]([C@@H](C)O)[C@H](CO)C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
44418842 144661 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 437 3 1 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL376285 144661 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 437 3 1 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(Cl)c4)cn3)[C@H]12 10.1021/jm061043e
127053952 167335 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 579 4 1 7 5.5 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C2(O)CN(C(=O)OC(C)(C)C)C2)CC1(F)F nan
CHEMBL4112571 167335 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 579 4 1 7 5.5 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C2(O)CN(C(=O)OC(C)(C)C)C2)CC1(F)F nan
44306500 174695 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL431369 174695 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 833 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccccc4Cl)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
53245451 82666 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 394 5 2 2 5.1 CCCC(=O)Nc1cccc(NC(=O)c2cc(Cl)ccc2Br)c1 10.1021/ml2002696
CHEMBL2049115 82666 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 394 5 2 2 5.1 CCCC(=O)Nc1cccc(NC(=O)c2cc(Cl)ccc2Br)c1 10.1021/ml2002696
CHEMBL3143290 217943 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44408711 82190 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 375 2 0 3 5.6 Cc1cccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc12 10.1016/j.bmcl.2005.12.042
CHEMBL204064 82190 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 375 2 0 3 5.6 Cc1cccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc12 10.1016/j.bmcl.2005.12.042
53245435 82664 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 378 5 2 2 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccc(F)cc2Br)c1 10.1021/ml2002696
CHEMBL2049113 82664 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 378 5 2 2 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccc(F)cc2Br)c1 10.1021/ml2002696
72547554 110655 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091989 110655 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
56671606 69965 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 834 22 8 9 2.9 CC[C@@H](C)[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL1790240 69965 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 834 22 8 9 2.9 CC[C@@H](C)[C@H](N)C(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
90663313 113423 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 982 27 12 10 -0.3 C#CC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143273 113423 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 982 27 12 10 -0.3 C#CC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
127053969 159335 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 477 5 1 5 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NC2CCC2)CC1(F)F nan
CHEMBL3971706 159335 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 477 5 1 5 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NC2CCC2)CC1(F)F nan
117826532 157063 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 7 2 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC(O)CCl)CC1(F)F nan
CHEMBL3952681 157063 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 7 2 6 4.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCC(O)CCl)CC1(F)F nan
127053968 157480 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 439 4 2 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NO)CC1(F)F nan
CHEMBL3956004 157480 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 439 4 2 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NO)CC1(F)F nan
127053977 160374 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 6 1 7 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cnccn2)CC1(F)F nan
CHEMBL3980605 160374 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 6 1 7 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cnccn2)CC1(F)F nan
127053944 159044 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 483 4 1 5 5.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3OC(F)(F)F)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
CHEMBL3969151 159044 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 483 4 1 5 5.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3OC(F)(F)F)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
57404484 80036 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 397 4 1 5 4.8 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccsc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012509 80036 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 397 4 1 5 4.8 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccsc2)cn1 10.1016/j.bmcl.2012.01.138
127053941 158604 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 467 4 0 4 6.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3OC(F)(F)F)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3965348 158604 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 467 4 0 4 6.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3OC(F)(F)F)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
127053970 166911 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2cccnc2)CC1(F)F nan
CHEMBL4108966 166911 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 514 6 1 6 5.4 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2cccnc2)CC1(F)F nan
127053989 158021 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 486 3 0 4 5.6 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(Br)CC1(F)F nan
CHEMBL3960140 158021 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 486 3 0 4 5.6 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(Br)CC1(F)F nan
127050971 147606 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 416 7 2 5 1.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCC2CC2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3819204 147606 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 416 7 2 5 1.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCC2CC2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
90663292 113414 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 857 22 9 9 1.4 COc1ccc(/C=C/C(=O)N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
CHEMBL3143251 113414 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 857 22 9 9 1.4 COc1ccc(/C=C/C(=O)N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm960455s
71735886 150867 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 479 4 2 6 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(C2(O)CNC2)CC1(F)F nan
CHEMBL3903446 150867 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 479 4 2 6 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(C2(O)CNC2)CC1(F)F nan
44403839 78184 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@H]3CCCC[C@@H]3C[C@@H]3C(=O)O[C@@H](C)[C@@H]32)n1 10.1021/jm0502236
CHEMBL195909 78184 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@H]3CCCC[C@@H]3C[C@@H]3C(=O)O[C@@H](C)[C@@H]32)n1 10.1021/jm0502236
11645276 78541 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 311 2 0 3 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccccn3)[C@H]12 10.1021/jm0502236
CHEMBL196683 78541 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 311 2 0 3 4.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccccn3)[C@H]12 10.1021/jm0502236
44280649 119434 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 743 19 8 9 1.3 COc1ccc(/C=C/C(=O)Nc2n[nH]c(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n2)cc1 10.1016/s0960-894x(99)00197-3
CHEMBL33033 119434 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 743 19 8 9 1.3 COc1ccc(/C=C/C(=O)Nc2n[nH]c(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)n2)cc1 10.1016/s0960-894x(99)00197-3
44281172 106450 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 589 15 9 9 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1cccs1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL284474 106450 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 589 15 9 9 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1cccs1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280955 126070 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 611 15 8 6 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc2[nH]cnc2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34387 126070 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 611 15 8 6 0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc2[nH]cnc2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
10459564 7305 41 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
4048 7305 41 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
CHEMBL2103856 7305 41 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
DB12046 7305 41 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 527 9 1 7 4.8 CCOc1c(OCC)cc2c(c1F)C(=N)N(C2)CC(=O)c1cc(N2CCOCC2)c(c(c1)C(C)(C)C)OC nan
90663298 113418 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143257 113418 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1cccc(Cl)c1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
16100342 90024 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3[C@@H](O)CCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218726 90024 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3[C@@H](O)CCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
72547552 110660 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3091994 110660 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
72547552 110660 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3091994 110660 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
44290166 176533 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 808 21 9 10 1.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL44387 176533 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 808 21 9 10 1.4 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
58046052 140076 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 457 9 1 8 3.9 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCF)cc(C(C)(C)C)c3)nc2c(C)c1C nan
CHEMBL3704477 140076 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 457 9 1 8 3.9 CCOc1nn2c(=N)n(CC(=O)c3cc(OCCCF)cc(C(C)(C)C)c3)nc2c(C)c1C nan
90663563 113477 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 829 22 9 8 2.0 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143684 113477 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 829 22 9 8 2.0 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143288 217941 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@H](Cc1cccs1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44280585 123757 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 727 18 8 8 1.7 C/C(=C\c1ccccc1)C(=O)Nc1n[nH]c(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)n1 10.1016/s0960-894x(99)00197-3
CHEMBL33873 123757 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 727 18 8 8 1.7 C/C(=C\c1ccccc1)C(=O)Nc1n[nH]c(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)n1 10.1016/s0960-894x(99)00197-3
44416466 148294 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 441 3 0 2 7.3 C[C@H]1OC[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL384562 148294 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 441 3 0 2 7.3 C[C@H]1OC[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL3143266 217929 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(C)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
72547555 110648 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 365 4 0 2 6.1 COC1(C)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091982 110648 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 365 4 0 2 6.1 COC1(C)C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44432693 152479 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 385 3 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL391624 152479 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 385 3 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C=C3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44309776 109907 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 754 16 6 7 5.3 NCCCNC(=O)[C@H](CCN)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL307831 109907 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 754 16 6 7 5.3 NCCCNC(=O)[C@H](CCN)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
90663337 113437 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 869 20 9 10 1.1 CC(=O)N(C(=O)c1cc2ccccc2oc1=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143301 113437 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 869 20 9 10 1.1 CC(=O)N(C(=O)c1cc2ccccc2oc1=O)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663294 113416 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 827 22 8 9 2.1 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
CHEMBL3143253 113416 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 827 22 8 9 2.1 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)CC(N)=O 10.1021/jm960455s
9804049 140341 2 None - 1 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371069 140341 2 None - 1 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
11691128 148127 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 459 5 0 5 5.9 CCOC(=O)c1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
CHEMBL383606 148127 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 459 5 0 5 5.9 CCOC(=O)c1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)nc1 10.1021/jm0502236
3525 10194 13 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10.1016/s0960-894x(03)00325-1
9853822 10194 13 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10.1016/s0960-894x(03)00325-1
CHEMBL311626 10194 13 None - 0 Human 6.4 pIC50 = 6.4 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 789 15 5 6 6.8 NCC[C@@H](C(=O)NCc1ccccc1)NC(=O)[C@H](Cc1ccc(c(c1)F)F)NC(=O)Nc1ccc2c(c1)n(Cc1c(Cl)cccc1Cl)cc2CN1CCCC1 10.1016/s0960-894x(03)00325-1
44432756 93518 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 396 3 0 5 3.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCOCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231971 93518 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 396 3 0 5 3.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(N4CCOCC4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44306761 175688 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL438551 175688 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 789 15 5 6 6.8 NCCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
9810477 105552 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 719 18 9 9 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccs2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL278216 105552 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 719 18 9 9 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccs2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280899 121563 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33394 121563 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccccn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
11284457 161304 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3939315 161304 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990814 161304 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting methodDisplacement of [3H] Ala-(4fluoro)Phe-Arg-(cy- clohexyl)Ala-(homo)Arg-Tyr-NH2 from thrombin receptor in human platelet membranes after 1 hr by liquid scintillation counting method
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
70693686 80023 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 389 4 0 3 5.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C)c2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012495 80023 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 389 4 0 3 5.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccc(C)c2)cn1 10.1016/j.bmcl.2012.01.138
44305939 210170 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 317 3 2 5 3.4 CCc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL65425 210170 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 317 3 2 5 3.4 CCc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
70695800 80034 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccc(OC)cc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012507 80034 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccc(OC)cc2)cn1 10.1016/j.bmcl.2012.01.138
90663291 113413 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 877 21 9 8 2.7 CC(=O)N(C(=O)c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143250 113413 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 877 21 9 8 2.7 CC(=O)N(C(=O)c1ccc(-c2ccccc2)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
11503433 142325 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4C(F)(F)F)cn3)[C@H]12 10.1021/jm0502236
CHEMBL372886 142325 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4C(F)(F)F)cn3)[C@H]12 10.1021/jm0502236
44432772 93719 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 437 3 0 3 5.8 O=C1OC[C@H]2[C@@H]1Cc1c(F)cc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232333 93719 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 437 3 0 3 5.8 O=C1OC[C@H]2[C@@H]1Cc1c(F)cc(F)cc1[C@@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1016/j.bmcl.2007.04.061
44280878 106838 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 501 13 8 8 -2.7 C[C@H](NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL287156 106838 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 501 13 8 8 -2.7 C[C@H](NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
11682882 79306 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(F)cc4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL199101 79306 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 405 3 0 3 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(F)cc4)cn3)[C@H]12 10.1021/jm0502236
44432715 93470 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 394 3 0 5 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4nccs4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL231728 93470 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 394 3 0 5 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4nccs4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL3143260 217926 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44338791 16098 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL111106 16098 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 559 8 0 6 5.9 Ic1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
76335370 110637 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3091971 110637 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 3 0 3 5.5 Fc1cccc(-c2ccc(/C=C/[C@@H]3[C@H]4CCCC[C@@H]4CC34OCCO4)nc2)c1 10.1021/ml400235c
CHEMBL3143318 217955 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44309730 210735 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 819 16 5 7 6.8 COc1ccc(CNC(=O)[C@H](CCN)NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)cc1 10.1016/s0960-894x(03)00325-1
CHEMBL69359 210735 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 819 16 5 7 6.8 COc1ccc(CNC(=O)[C@H](CCN)NC(=O)[C@H](Cc2ccc(F)c(F)c2)NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)cc1 10.1016/s0960-894x(03)00325-1
53245434 82663 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 374 5 2 2 4.7 CCCC(=O)Nc1cccc(NC(=O)c2cc(C)ccc2Br)c1 10.1021/ml2002696
CHEMBL2049112 82663 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 374 5 2 2 4.7 CCCC(=O)Nc1cccc(NC(=O)c2cc(C)ccc2Br)c1 10.1021/ml2002696
16100353 89827 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC[C@@H](O)C[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218168 89827 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC[C@@H](O)C[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
68058674 134050 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 420 6 1 3 4.2 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)C3(CC)COC3)C2)cc1 nan
CHEMBL3658403 134050 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 420 6 1 3 4.2 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)C3(CC)COC3)C2)cc1 nan
58046031 140080 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 10 2 10 3.1 CC(C)Oc1cc(OC(C)C)c2nn(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704481 140080 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 485 10 2 10 3.1 CC(C)Oc1cc(OC(C)C)c2nn(CC(=O)c3cc(OCCO)cc(C(C)(C)C)c3)c(=N)n2n1 nan
70685282 80035 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 392 4 1 5 4.1 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccnc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012508 80035 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 392 4 1 5 4.1 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cccnc2)cn1 10.1016/j.bmcl.2012.01.138
44305953 108876 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 375 6 3 6 3.7 CC(C)c1ccc(Cn2ccc3c4c(N)nc(NCCO)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL302226 108876 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 375 6 3 6 3.7 CC(C)c1ccc(Cn2ccc3c4c(N)nc(NCCO)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
127053939 160980 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 401 3 0 3 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3985900 160980 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 401 3 0 3 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
127053949 149537 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 447 4 0 5 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CC#N)CC1(F)F nan
CHEMBL3892564 149537 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 447 4 0 5 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(CC#N)CC1(F)F nan
127053998 166655 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 0 5 4.8 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(N(C)C)CC1(F)F nan
CHEMBL4106780 166655 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 451 4 0 5 4.8 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(N(C)C)CC1(F)F nan
72547308 110657 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091991 110657 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
127053979 159038 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 6 1 7 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cncnc2)CC1(F)F nan
CHEMBL3969105 159038 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 515 6 1 7 4.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NCc2cncnc2)CC1(F)F nan
127053996 159315 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 423 3 2 4 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)NC(=O)[C@]2(O)CC1(F)F nan
CHEMBL3971586 159315 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 423 3 2 4 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)NC(=O)[C@]2(O)CC1(F)F nan
127050658 147548 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 458 7 2 5 2.3 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCCC(F)(F)F)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3818421 147548 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 458 7 2 5 2.3 CCN(C(=O)CO)C1CN(/C(=N\C#N)NCCCC(F)(F)F)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
11684648 147612 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 492 5 2 5 3.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3819237 147612 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 492 5 2 5 3.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(Cl)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
44409074 82204 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 443 3 0 4 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5ccsc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL204157 82204 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 443 3 0 4 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(-c5ccsc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44409248 83923 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 4 0 5 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1OC 10.1016/j.bmcl.2005.12.042
CHEMBL207791 83923 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 4 0 5 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1OC 10.1016/j.bmcl.2005.12.042
72547554 110655 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091989 110655 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 414 5 1 3 4.6 CS(=O)(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
44309472 211034 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 804 16 5 7 6.2 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCc1ccccn1 10.1016/s0960-894x(03)00325-1
CHEMBL71140 211034 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 804 16 5 7 6.2 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCc1ccccn1 10.1016/s0960-894x(03)00325-1
90663299 113419 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 812 20 10 7 1.9 CC(=O)N(c1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143258 113419 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 812 20 10 7 1.9 CC(=O)N(c1c[nH]c2ccccc12)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44409029 83265 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 504 5 0 6 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)N5CCOCC5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL205987 83265 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 504 5 0 6 4.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OCC(=O)N5CCOCC5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44409062 175770 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 538 6 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OC(C)(C)C(=O)Nc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL439157 175770 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 538 6 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OC(C)(C)C(=O)Nc5ccccc5)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44306599 210432 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL67308 210432 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 803 16 5 6 7.1 NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44416724 87327 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 379 3 1 3 4.7 C[C@H]1O[C@H](Cc2ccc3ccccc3n2)C2[C@H]1[C@H](C(=O)O)C[C@@H]1CCCC[C@@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL214862 87327 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 379 3 1 3 4.7 C[C@H]1O[C@H](Cc2ccc3ccccc3n2)C2[C@H]1[C@H](C(=O)O)C[C@@H]1CCCC[C@@H]21 10.1016/j.bmcl.2006.06.042
9831828 173179 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 733 19 7 8 2.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
CHEMBL42769 173179 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 733 19 7 8 2.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
44290181 180073 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 806 22 8 9 2.1 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL45259 180073 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 806 22 8 9 2.1 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
44281263 106618 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 603 16 7 5 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285685 106618 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 603 16 7 5 2.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
70687425 80026 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cc(Cl)ccc2Cl)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012498 80026 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 443 4 0 3 6.9 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2cc(Cl)ccc2Cl)cn1 10.1016/j.bmcl.2012.01.138
10000177 210174 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometryAntagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometry
ChEMBL 385 5 1 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C5CC5)nc4ccc32)cc1 10.1039/c4md00485j
CHEMBL65476 210174 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometryAntagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometry
ChEMBL 385 5 1 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C5CC5)nc4ccc32)cc1 10.1039/c4md00485j
10000177 210174 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 385 5 1 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C5CC5)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL65476 210174 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 385 5 1 5 4.9 CC(C)c1ccc(Cn2ccc3c4c(N)nc(N(C)C5CC5)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
44338929 12617 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107919 12617 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 493 10 0 8 5.4 COc1cc(OC)cc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
49766539 66360 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 386 4 2 2 4.8 O=C(Nc1cccc(NC(=O)C2CCCC2)c1)c1ccccc1Br 10.1021/ml2002696
CHEMBL1718628 66360 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 386 4 2 2 4.8 O=C(Nc1cccc(NC(=O)C2CCCC2)c1)c1ccccc1Br 10.1021/ml2002696
50910534 82572 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 6 2 2 4.2 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2CC)c1 10.1021/ml2002696
CHEMBL2048423 82572 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 310 6 2 2 4.2 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2CC)c1 10.1021/ml2002696
44305897 109615 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 359 5 2 5 4.8 CCNc1nc(N)c2c(ccc3c2ccn3Cc2ccc(C(C)C)cc2)n1 10.1016/s0960-894x(99)00339-x
CHEMBL305557 109615 2 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 359 5 2 5 4.8 CCNc1nc(N)c2c(ccc3c2ccn3Cc2ccc(C(C)C)cc2)n1 10.1016/s0960-894x(99)00339-x
16100351 89566 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 491 3 0 3 7.0 C[C@H]1OC(=O)[C@@H]2C[C@H]3[C@@H](CCCC3(F)F)[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218000 89566 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 491 3 0 3 7.0 C[C@H]1OC(=O)[C@@H]2C[C@H]3[C@@H](CCCC3(F)F)[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
76328106 110645 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 378 4 1 2 5.2 CC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091979 110645 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 378 4 1 2 5.2 CC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
66761604 134310 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 474 3 2 3 2.8 O=C1CN(C(=O)N2CC(NC(=O)c3ccccc3)CC(c3ccc(C(F)(F)F)cc3)C2)CCN1 nan
CHEMBL3662511 134310 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 474 3 2 3 2.8 O=C1CN(C(=O)N2CC(NC(=O)c3ccccc3)CC(c3ccc(C(F)(F)F)cc3)C2)CCN1 nan
44306501 109468 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL304683 109468 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 834 17 7 7 6.3 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
44290276 171678 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 748 19 8 9 1.7 Cc1oc([C@H](Cc2ccc(F)cc2)NC(=O)C(N)CN)nc1C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc1ccccc1 10.1016/s0960-894x(98)00292-3
CHEMBL42224 171678 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 748 19 8 9 1.7 Cc1oc([C@H](Cc2ccc(F)cc2)NC(=O)C(N)CN)nc1C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc1ccccc1 10.1016/s0960-894x(98)00292-3
44290058 185776 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 705 18 7 8 2.1 NCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
CHEMBL47090 185776 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 705 18 7 8 2.1 NCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
9937578 106733 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 555 15 7 8 0.3 NCCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286430 106733 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 555 15 7 8 0.3 NCCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
23631278 99729 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 498 3 0 4 5.5 CC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
CHEMBL244108 99729 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 498 3 0 4 5.5 CC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm070704k
11639231 79112 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 367 4 0 3 5.3 CC(C)Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL198451 79112 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 367 4 0 3 5.3 CC(C)Cc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL33473 218179 24 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1016/s0960-894x(99)00197-3
44281237 123507 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 604 16 7 6 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33742 123507 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 604 16 7 6 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)/C=C/c1cccnc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL4764659 220824 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Affinity Biochemical interaction (Binding assay (platelet membranes)) EUB0000291b F2RAffinity Biochemical interaction (Binding assay (platelet membranes)) EUB0000291b F2R
ChEMBL None None None O=C(N1CCS(=O)(=O)CC1)N1C[C@@](S)(c2ccc(OC(F)(F)F)cc2)C[C@@](S)(c2nc(C3CC3)no2)C1 10.6019/CHEMBL5210307
10971 10331 30 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometryAntagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometry
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1039/c4md00485j
4259181 10331 30 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometryAntagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometry
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1039/c4md00485j
CHEMBL63426 10331 30 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometryAntagonist activity at PAR1 in human platelet membranes assessed as inhibition of interaction of PAR1 with [Ala-Phe(p-F)-Arg-Cha-HArg-Tyr-NH2] by Chronolog aggregometry
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1039/c4md00485j
10971 10331 30 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1016/s0960-894x(99)00339-x
4259181 10331 30 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1016/s0960-894x(99)00339-x
CHEMBL63426 10331 30 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 371 5 2 5 4.9 CC(c1ccc(cc1)Cn1ccc2c1ccc1c2c(N)nc(n1)NC1CC1)C 10.1016/s0960-894x(99)00339-x
90663354 113445 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccccc1F)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143319 113445 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 791 20 9 7 1.5 CC(=O)N(c1ccccc1F)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306612 108937 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL302603 108937 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 875 19 6 8 6.6 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC2CCCCC2)cc1 10.1016/s0960-894x(01)00378-x
9831948 185707 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 749 20 7 8 2.9 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL47023 185707 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 749 20 7 8 2.9 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCc2ccccc2)cs1 10.1016/s0960-894x(98)00292-3
44281264 122047 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 616 15 8 5 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33487 122047 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 616 15 8 5 2.2 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc2ccccc2[nH]1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
11284457 161304 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3939315 161304 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990814 161304 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 565 10 1 8 4.6 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCN(CC#N)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
44290231 107050 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 792 21 8 9 1.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL288976 107050 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 792 21 8 9 1.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
44432833 93459 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)O[C@H](C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL231695 93459 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@@H]3c4ccccc4C[C@H]4C(=O)O[C@H](C)[C@@H]34)ccc2c1 10.1016/j.bmcl.2007.04.061
72547553 110641 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 415 5 0 4 5.1 CS(=O)(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091975 110641 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 415 5 0 4 5.1 CS(=O)(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
121335735 159336 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 5 5.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)CC(C)(C)C)CC1(F)F nan
CHEMBL3971708 159336 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 521 5 1 5 5.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)[C@@H]2[C@@H](C)OC(=O)[C@]2(NC(=O)CC(C)(C)C)CC1(F)F nan
9951647 147354 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 377 2 1 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL381265 147354 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 377 2 1 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
127053984 167547 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 522 5 2 5 4.9 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@@]2(NC(=S)NC2CC2)CC1(F)F nan
CHEMBL4114149 167547 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 522 5 2 5 4.9 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@@]2(NC(=S)NC2CC2)CC1(F)F nan
72547553 110641 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 415 5 0 4 5.1 CS(=O)(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091975 110641 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 415 5 0 4 5.1 CS(=O)(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
57404504 80028 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 391 4 1 4 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012500 80028 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 391 4 1 4 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2)cn1 10.1016/j.bmcl.2012.01.138
127053964 156220 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 476 4 0 8 3.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(n2cnnn2)CC1(F)F nan
CHEMBL3945945 156220 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 476 4 0 8 3.9 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(n2cnnn2)CC1(F)F nan
127053967 166977 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 490 4 0 8 4.2 Cc1nnnn1[C@@]12CC(F)(F)C(C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)C1[C@@H](C)OC2=O nan
CHEMBL4109515 166977 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 490 4 0 8 4.2 Cc1nnnn1[C@@]12CC(F)(F)C(C)[C@H](/C=C/c3ccc(-c4ccccc4C#N)cn3)C1[C@@H](C)OC2=O nan
127053973 166936 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 504 6 1 7 5.0 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2ncco2)CC1(F)F nan
CHEMBL4109166 166936 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 504 6 1 7 5.0 CC1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NCc2ncco2)CC1(F)F nan
CHEMBL3143275 217935 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm960455s
44310308 174666 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 759 15 5 7 5.5 CSC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN 10.1016/s0960-894x(03)00325-1
CHEMBL431164 174666 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 759 15 5 7 5.5 CSC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN 10.1016/s0960-894x(03)00325-1
127051545 147511 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 476 5 2 5 3.3 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(F)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3817930 147511 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 476 5 2 5 3.3 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(F)c(Cl)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
127050656 147619 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 490 7 2 6 3.1 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(OC(F)F)cc2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3819343 147619 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 490 7 2 6 3.1 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc(OC(F)F)cc2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
44408851 82182 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
CHEMBL204009 82182 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2006.06.042
44408851 82182 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL204009 82182 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 361 2 0 3 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
10161572 12323 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL107667 12323 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 458 8 0 7 5.2 N#Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
23631809 99968 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 456 3 1 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CNCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244487 99968 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 456 3 1 4 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CNCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
23631900 149691 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 5 5.5 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4ccccc4C)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
CHEMBL389382 149691 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 5 5.5 CCOC(=O)N1CCC[C@H]2[C@H](/C=C/c3ccc(-c4ccccc4C)cn3)[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]21 10.1021/jm070704k
53245432 82665 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 378 5 2 2 4.6 CCCC(=O)Nc1cccc(NC(=O)c2cc(F)ccc2Br)c1 10.1021/ml2002696
CHEMBL2049114 82665 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 378 5 2 2 4.6 CCCC(=O)Nc1cccc(NC(=O)c2cc(F)ccc2Br)c1 10.1021/ml2002696
44281289 125340 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 599 15 10 9 -0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL34156 125340 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 599 15 10 9 -0.9 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44290110 108022 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 715 19 7 8 2.5 CNCC(=O)N[C@@H](Cc1ccccc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
CHEMBL296147 108022 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 715 19 7 8 2.5 CNCC(=O)N[C@@H](Cc1ccccc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)c(C)o1 10.1016/s0960-894x(98)00292-3
44187102 131919 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 404 8 1 7 2.7 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(Cl)cc(OC)c1 nan
CHEMBL3644437 131919 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 404 8 1 7 2.7 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(Cl)cc(OC)c1 nan
CHEMBL3143299 217945 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(N)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143321 217957 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccc(O)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44416691 88131 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 393 3 1 4 5.1 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)O[C@@H](O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL215924 88131 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 393 3 1 4 5.1 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)O[C@@H](O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
44408873 83485 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL206502 83485 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
44290059 108228 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 615 16 7 8 0.3 NCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)co1 10.1016/s0960-894x(98)00292-3
CHEMBL297640 108228 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 615 16 7 8 0.3 NCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)co1 10.1016/s0960-894x(98)00292-3
44416567 145418 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 377 3 0 3 5.7 COc1ccc2nc(/C=C/[C@@H]3[C@H]4[C@H](CO[C@@H]4C)C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL377594 145418 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 377 3 0 3 5.7 COc1ccc2nc(/C=C/[C@@H]3[C@H]4[C@H](CO[C@@H]4C)C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
66760951 134314 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 476 3 1 3 4.5 N#CC1CCN(C(=O)N2CC(NC(=O)C3CCCC3)CC(c3ccc(C(F)(F)F)cc3)C2)CC1 nan
CHEMBL3662515 134314 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 476 3 1 3 4.5 N#CC1CCN(C(=O)N2CC(NC(=O)C3CCCC3)CC(c3ccc(C(F)(F)F)cc3)C2)CC1 nan
44432795 93516 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL231957 93516 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 419 3 0 3 5.7 O=C1OC[C@H]2[C@@H]1Cc1c(Cl)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL3143300 217946 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](CCc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44183746 140056 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 469 11 1 9 3.8 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(OCCOC)cc(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704457 140056 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 469 11 1 9 3.8 CCC(CC)Oc1ccc2nn(CC(=O)c3cc(OCCOC)cc(C(C)(C)C)c3)c(=N)n2n1 nan
70683207 80038 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 384 4 1 5 3.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(N2CCCC2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012511 80038 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 384 4 1 5 3.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(N2CCCC2)cn1 10.1016/j.bmcl.2012.01.138
44306336 210326 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL66585 210326 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 780 17 6 7 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc(C#N)cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
9875040 121201 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 713 18 9 8 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33318 121201 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 713 18 9 8 1.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2ccccc2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44432763 93569 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 453 3 0 3 6.0 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232171 93569 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 453 3 0 3 6.0 O=C1OC[C@H]2[C@@H]1Cc1c(F)cccc1[C@@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1016/j.bmcl.2007.04.061
2858875 215034 10 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 469 5 2 5 6.2 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(Cc3ccccc3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
CHEMBL98805 215034 10 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 469 5 2 5 6.2 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(Cc3ccccc3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
137661486 166255 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
CHEMBL4101591 166255 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 407 3 1 2 6.8 C[C@H]1CC[C@@H]2C(C)(C)[C@H](O)CC[C@@]2(C)[C@@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/acs.jmedchem.7b00951
10204371 213678 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 451 6 3 3 4.9 CN(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL90864 213678 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 451 6 3 3 4.9 CN(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
76313664 110650 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 351 4 0 2 5.7 COC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091984 110650 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 351 4 0 2 5.7 COC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
76335372 110651 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 4 0 3 5.7 CC(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091985 110651 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 379 4 0 3 5.7 CC(=O)OC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
9810475 108315 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 719 19 7 8 2.5 NCCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
CHEMBL298273 108315 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 719 19 7 8 2.5 NCCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)co1 10.1016/s0960-894x(98)00292-3
44409259 147472 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 432 4 1 4 5.6 CCC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
CHEMBL381569 147472 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 432 4 1 4 5.6 CCC(=O)Nc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2005.12.042
90663331 113432 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 773 20 9 7 1.4 CC(=O)N(c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143294 113432 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 773 20 9 7 1.4 CC(=O)N(c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44306076 209808 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 335 3 2 6 3.5 CSc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL63381 209808 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 335 3 2 6 3.5 CSc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
44432803 151788 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 421 3 0 3 5.3 O=C1OC[C@H]2[C@@H]1Cc1c(ccc(F)c1F)[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL391098 151788 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 421 3 0 3 5.3 O=C1OC[C@H]2[C@@H]1Cc1c(ccc(F)c1F)[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
127053987 150587 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 501 5 1 6 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NS(C)(=O)=O)CC1(F)F nan
CHEMBL3901289 150587 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 501 5 1 6 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NS(C)(=O)=O)CC1(F)F nan
66761456 134061 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 500 4 1 4 4.5 N#CC1CCN(C(=O)N2CC(NC(=O)c3ccccc3)CC(c3ccc(OC(F)(F)F)cc3)C2)CC1 nan
CHEMBL3658413 134061 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 500 4 1 4 4.5 N#CC1CCN(C(=O)N2CC(NC(=O)c3ccccc3)CC(c3ccc(OC(F)(F)F)cc3)C2)CC1 nan
127053983 155542 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 5 2 5 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NC(=O)NC2CCC2)CC1(F)F nan
CHEMBL3940503 155542 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 520 5 2 5 5.1 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(NC(=O)NC2CCC2)CC1(F)F nan
72547551 110647 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
CHEMBL3091981 110647 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
127053942 150206 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 423 3 1 5 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(N)CC1(F)F nan
CHEMBL3898141 150206 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 423 3 1 5 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(N)CC1(F)F nan
CHEMBL3143291 217944 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44432814 94791 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 3 5.0 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL234397 94791 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 3 5.0 O=C1OC[C@H]2[C@@H]1Cc1ccccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
127053961 158490 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 499 5 1 6 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nn[nH]n2)CC1(F)F nan
CHEMBL3964337 158490 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 499 5 1 6 5.0 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3Cl)cn2)C2[C@@H](C)OC(=O)[C@]2(Cc2nn[nH]n2)CC1(F)F nan
10350886 185535 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 942 27 13 9 -0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1016/s0960-894x(98)00292-3
CHEMBL46869 185535 1 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 942 27 13 9 -0.3 CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1016/s0960-894x(98)00292-3
23628249 94020 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1cc(F)ccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL232955 94020 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1cc(F)ccc1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL3143272 217934 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44309471 108935 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
CHEMBL302594 108935 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 796 16 5 7 5.6 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCCN1CCCC1 10.1016/s0960-894x(03)00325-1
44309959 175989 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 772 15 5 7 5.7 NCCNC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](Cc1ccccc1F)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL440808 175989 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 772 15 5 7 5.7 NCCNC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](Cc1ccccc1F)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
127051546 147614 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 490 7 2 6 3.1 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2cccc(OC(F)F)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3819277 147614 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 490 7 2 6 3.1 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2cccc(OC(F)F)c2)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
44418846 90011 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3C[C@H](O)CC[C@H]32)nc1 10.1021/jm061043e
CHEMBL218670 90011 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 417 3 1 4 5.0 Cc1ccccc1-c1ccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3C[C@H](O)CC[C@H]32)nc1 10.1021/jm061043e
10246587 78881 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197791 78881 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44324193 112932 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 479 7 3 3 5.6 CC(C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
CHEMBL313645 112932 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity against platelet thrombin receptorBinding affinity against platelet thrombin receptor
ChEMBL 479 7 3 3 5.6 CC(C)N(C[C@@H](O)c1ccc(Cl)c(Cl)c1)C(=O)Nc1ccc(CNC(=O)C(C)(C)C)cc1 10.1016/s0960-894x(01)00538-8
44408709 148156 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1cccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc12 10.1016/j.bmcl.2005.12.042
CHEMBL383832 148156 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 391 3 0 4 5.3 COc1cccc2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)nc12 10.1016/j.bmcl.2005.12.042
44416634 87860 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 377 3 0 3 5.7 CO[C@@H]1O[C@H](C)[C@H]2[C@@H](/C=C/c3ccc4ccccc4n3)[C@@H]3CCCC[C@H]3C[C@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL215524 87860 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 377 3 0 3 5.7 CO[C@@H]1O[C@H](C)[C@H]2[C@@H](/C=C/c3ccc4ccccc4n3)[C@@H]3CCCC[C@H]3C[C@H]21 10.1016/j.bmcl.2006.06.042
44416487 172788 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 321 3 0 2 5.9 COc1ccc2nc(/C=C/[C@@H]3CCC[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL425437 172788 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 321 3 0 2 5.9 COc1ccc2nc(/C=C/[C@@H]3CCC[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
44280703 123574 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33781 123574 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 578 15 7 6 1.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccncc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280768 123952 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 569 14 9 8 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(99)00197-3
CHEMBL33940 123952 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 569 14 9 8 -0.5 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(N)n1)C(=O)N[C@H](C(N)=O)c1ccccc1 10.1016/s0960-894x(99)00197-3
50910535 82573 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 366 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2OC(F)(F)F)c1 10.1021/ml2002696
CHEMBL2048425 82573 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 366 6 2 3 4.6 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2OC(F)(F)F)c1 10.1021/ml2002696
44418839 90201 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm061043e
CHEMBL219698 90201 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm061043e
11674764 79054 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 353 3 0 3 5.2 CC(C)c1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL198273 79054 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 353 3 0 3 5.2 CC(C)c1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44408615 81204 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 379 2 0 3 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(F)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL202677 81204 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 379 2 0 3 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(F)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44306402 174987 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL433499 174987 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 827 20 6 7 6.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCCC4)cn(Cc4ccccc4C)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCCCc2ccccc2)cc1 10.1016/s0960-894x(01)00378-x
CHEMBL33473 218179 24 None - 0 Human 4.1 pIC50 = 4.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1016/s0960-894x(98)00292-3
44328647 119574 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 525 5 2 5 7.5 CC(C)(C)c1ccc(Cn2c(=N)n(CC(=O)c3cc(C(C)(C)C)c(O)c(C(C)(C)C)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00555-8
CHEMBL330643 119574 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 525 5 2 5 7.5 CC(C)(C)c1ccc(Cn2c(=N)n(CC(=O)c3cc(C(C)(C)C)c(O)c(C(C)(C)C)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00555-8
44416740 148772 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 395 5 2 4 4.7 COc1ccc2nc(/C=C/[C@@H]3[C@H]([C@@H](C)O)[C@H](CO)C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL387441 148772 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 395 5 2 4 4.7 COc1ccc2nc(/C=C/[C@@H]3[C@H]([C@@H](C)O)[C@H](CO)C[C@@H]4CCCC[C@H]43)ccc2c1 10.1016/j.bmcl.2006.06.042
CHEMBL3143316 217953 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44280522 105977 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL281443 105977 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 612 15 7 6 1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cccnc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
23631277 150227 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 470 3 0 4 5.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL389834 150227 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 470 3 0 4 5.5 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
12018762 116411 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL322282 116411 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 451 8 0 6 5.5 Fc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
17187522 66423 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 296 5 2 2 4.0 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2C)c1 10.1021/ml2002696
CHEMBL1721173 66423 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 296 5 2 2 4.0 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2C)c1 10.1021/ml2002696
90663305 113421 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 558 11 5 5 2.3 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(N)=O 10.1021/jm960455s
CHEMBL3143265 113421 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 558 11 5 5 2.3 CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(N)=O 10.1021/jm960455s
76331783 110644 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 436 4 1 3 6.6 CC(C)(C)OC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091978 110644 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 436 4 1 3 6.6 CC(C)(C)OC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
66761321 134305 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 435 4 1 3 3.9 CC(C)c1cccc(C2CC(NC(=O)c3ccccc3)CN(C(=O)N3CCOCC3)C2)c1 nan
CHEMBL3662506 134305 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 435 4 1 3 3.9 CC(C)c1cccc(C2CC(NC(=O)c3ccccc3)CN(C(=O)N3CCOCC3)C2)c1 nan
23631188 99727 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3ccccc3F)cn2)C1 10.1021/jm070704k
CHEMBL244105 99727 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3ccccc3F)cn2)C1 10.1021/jm070704k
23631811 99890 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244299 99890 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 474 4 0 4 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CN(C(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccccc4F)cn3)[C@H]12 10.1021/jm070704k
127053951 156320 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 480 4 1 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C2(O)COC2)CC1(F)F nan
CHEMBL3946656 156320 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 480 4 1 6 4.2 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3C#N)cn2)C2[C@@H](C)OC(=O)[C@]2(C2(O)COC2)CC1(F)F nan
57404483 80032 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012505 80032 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 421 5 1 5 4.7 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2012.01.138
127053945 151285 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 417 3 1 4 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
CHEMBL3906979 151285 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 417 3 1 4 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
72547551 110647 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
CHEMBL3091981 110647 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 392 3 1 3 5.2 O=C1NCC2(C[C@@H]3CCCC[C@@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)O1 10.1021/ml400235c
70683205 80037 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 381 4 1 5 4.3 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccoc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012510 80037 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 381 4 1 5 4.3 CC[C@@H]1[C@@H](C)C[C@@]2(O)C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccoc2)cn1 10.1016/j.bmcl.2012.01.138
70681077 80017 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 375 4 0 3 5.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2)cn1 10.1016/j.bmcl.2012.01.138
CHEMBL2012489 80017 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation countingDisplacement of [3H]haTRAP from human PAR1 after 1 hr by TopCount scintillation counting
ChEMBL 375 4 0 3 5.6 CC[C@@H]1[C@@H](C)C[C@H]2C(=O)O[C@H](C)[C@H]2[C@H]1/C=C/c1ccc(-c2ccccc2)cn1 10.1016/j.bmcl.2012.01.138
127051547 147571 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 504 5 2 7 2.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc3c(c2)OC(F)(F)O3)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
CHEMBL3818750 147571 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 (unknown origin)Antagonist activity at PAR1 (unknown origin)
ChEMBL 504 5 2 7 2.8 CCN(C(=O)CO)C1CN(/C(=N\C#N)Nc2ccc3c(c2)OC(F)(F)O3)N=C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.5b01890
23630915 99965 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 489 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[S+]([O-])CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
CHEMBL244483 99965 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 489 3 0 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[S+]([O-])CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm070704k
44418837 148360 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 437 3 0 3 6.3 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CC(F)(F)CC[C@H]43)nc2)c1 10.1021/jm061043e
CHEMBL384982 148360 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 437 3 0 3 6.3 Cc1cccc(-c2ccc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CC(F)(F)CC[C@H]43)nc2)c1 10.1021/jm061043e
44409289 81420 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 425 3 0 4 5.9 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1Cl 10.1016/j.bmcl.2005.12.042
CHEMBL203012 81420 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 425 3 0 4 5.9 COc1ccc2nc(/C=C/[C@@H]3[C@@H]4[C@@H](C)OC(=O)[C@@H]4C[C@@H]4CCCC[C@H]43)ccc2c1Cl 10.1016/j.bmcl.2005.12.042
44409050 147858 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 462 5 1 5 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OC(C)(C)C(N)=O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
CHEMBL382581 147858 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 462 5 1 5 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4cc(OC(C)(C)C(N)=O)ccc4n3)[C@H]12 10.1016/j.bmcl.2005.12.042
44306337 103612 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
CHEMBL265227 103612 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 800 18 6 8 5.1 Cc1ccccc1Cn1cc(CN2CCCC2)c2ccc(NC(=O)N[C@@H](Cc3ccc([N+](=O)[O-])cc3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc3ccccc3)cc21 10.1016/s0960-894x(01)00378-x
44416672 173233 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 347 2 0 2 5.7 C[C@H]1OC[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@@H]21 10.1016/j.bmcl.2006.06.042
CHEMBL427783 173233 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 347 2 0 2 5.7 C[C@H]1OC[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc4ccccc4n3)[C@@H]21 10.1016/j.bmcl.2006.06.042
44289954 108148 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 721 18 7 8 2.3 NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csc([C@@H](N)Cc2ccc(F)cc2)n1 10.1016/s0960-894x(98)00292-3
CHEMBL297091 108148 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 721 18 7 8 2.3 NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csc([C@@H](N)Cc2ccc(F)cc2)n1 10.1016/s0960-894x(98)00292-3
10077130 10779 53 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4047 10779 53 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
4870 10779 53 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
CHEMBL493982 10779 53 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
DB09030 10779 53 None - 1 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysisAntagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/acs.jmedchem.7b00951
46931416 134313 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 467 3 2 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)C1CCCC1 nan
CHEMBL3662514 134313 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 467 3 2 3 3.7 O=C(NC1CC(c2ccc(C(F)(F)F)cc2)CN(C(=O)N2CCC(O)CC2)C1)C1CCCC1 nan
9919038 173507 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL428311 173507 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
44290234 185294 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 832 22 8 10 2.4 COc1ccc(C[C@H](NC(=O)C(N)C(C)C)c2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cs2)cc1 10.1016/s0960-894x(98)00292-3
CHEMBL46670 185294 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 832 22 8 10 2.4 COc1ccc(C[C@H](NC(=O)C(N)C(C)C)c2nc(C(=O)N[C@@H](CC3CCCCC3)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc3ccccc3)C(N)=O)cs2)cc1 10.1016/s0960-894x(98)00292-3
58045917 140064 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 496 8 1 10 3.0 CCOc1nn2c(=N)n(CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)nc2cc1CC nan
CHEMBL3704465 140064 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 496 8 1 10 3.0 CCOc1nn2c(=N)n(CC(=O)c3cc(N4CCOCC4)c(OC)c(C(C)(C)C)c3)nc2cc1CC nan
44418840 90202 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(F)cc4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL219699 90202 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 421 3 1 4 4.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4ccc(F)cc4)cn3)[C@H]12 10.1021/jm061043e
11249717 161218 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3903962 161218 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
CHEMBL3990074 161218 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometerAntagonist activity at thrombin receptor in human platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation preincubated for 3 mins followed by thrombin addition measured after 6 mins by aggregometer
ChEMBL 541 9 2 7 4.9 CCOc1cc2c(c(F)c1OCC)C(=N)N(CC(=O)c1cc(N3CCC(O)CC3)c(OC)c(C(C)(C)C)c1)C2 nan
58137009 131926 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 486 11 2 9 2.5 CCOc1nn2c(N)n[n+](CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c2cc1CC nan
CHEMBL3644444 131926 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 486 11 2 9 2.5 CCOc1nn2c(N)n[n+](CC(=O)c3cc(OCCCO)c(OC)c(C(C)(C)C)c3)c2cc1CC nan
16100343 144935 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC[C@H](O)C[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL376890 144935 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CC[C@H](O)C[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
44187647 131922 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 470 11 1 8 3.4 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OCCOC)cc(C(C)(C)C)c1 nan
CHEMBL3644440 131922 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997).The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at RT for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB microtiter filtration.
ChEMBL 470 11 1 8 3.4 CCC(CC)Oc1ccc2n(n1)c(N)n[n+]2CC(=O)c1cc(OCCOC)cc(C(C)(C)C)c1 nan
10246587 78881 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
CHEMBL197791 78881 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to PAR1 in human platelet membraneBinding affinity to PAR1 in human platelet membrane
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1016/j.bmcl.2006.06.042
10246587 78881 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197791 78881 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44432806 94060 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1cccc(F)c1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
CHEMBL233163 94060 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 403 3 0 3 5.2 O=C1OC[C@H]2[C@@H]1Cc1cccc(F)c1[C@@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1016/j.bmcl.2007.04.061
11508687 78670 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 355 4 0 4 4.2 COCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197133 78670 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 355 4 0 4 4.2 COCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
44826172 106764 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc([N+](=O)[O-])c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL286648 106764 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to Thrombin receptor 1 (PAR-1) on membranes from CHRF cells
ChEMBL 758 19 9 10 1.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1n[nH]c(NC(=O)/C=C/c2cccc([N+](=O)[O-])c2)n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44280822 123323 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 594 15 8 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1nccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33629 123323 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 594 15 8 8 0.1 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1nccnc1N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL3143255 217924 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm960455s
44305896 109574 3 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 345 4 2 5 4.4 CNc1nc(N)c2c(ccc3c2ccn3Cc2ccc(C(C)C)cc2)n1 10.1016/s0960-894x(99)00339-x
CHEMBL305329 109574 3 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 345 4 2 5 4.4 CNc1nc(N)c2c(ccc3c2ccn3Cc2ccc(C(C)C)cc2)n1 10.1016/s0960-894x(99)00339-x
127053991 150449 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 466 4 2 7 3.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3-c3nnn[nH]3)cn2)C2[C@@H](C)OC(=O)[C@]2(N)CC1(F)F nan
CHEMBL3900057 150449 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 466 4 2 7 3.5 C[C@H]1[C@H](/C=C/c2ccc(-c3ccccc3-c3nnn[nH]3)cn2)C2[C@@H](C)OC(=O)[C@]2(N)CC1(F)F nan
44432721 93557 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 389 3 0 5 4.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cnccn4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
CHEMBL232140 93557 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from human PAR1 receptor in platelet membraneDisplacement of [3H]haTRAP from human PAR1 receptor in platelet membrane
ChEMBL 389 3 0 5 4.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cnccn4)cn3)[C@H]12 10.1016/j.bmcl.2007.06.002
44339029 116469 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 447 8 0 6 5.7 Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
CHEMBL322763 116469 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 447 8 0 6 5.7 Cc1cccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)c1 10.1016/s0960-894x(01)00745-4
72547308 110657 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091991 110657 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 392 4 0 2 5.6 CC(=O)N(C)C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3143305 217947 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(NC(=N)N)cc1)NC(=O)[C@H](Cc1ccc(F)cc1)NS(=O)(=O)c1cccs1)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
90663318 113428 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 986 28 12 10 0.5 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
CHEMBL3143280 113428 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 986 28 12 10 0.5 CCC(=O)c1cccc(N(C(C)=O)[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](Cc2ccc(NC(=N)N)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)c1 10.1021/jm960455s
127053966 167713 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 580 6 1 8 6.2 CNc1ccc(-c2cn([C@@]34CC(F)(F)C(C)[C@H](/C=C/c5ccc(-c6ccccc6C#N)cn5)C3[C@@H](C)OC4=O)nn2)cc1 nan
CHEMBL4115431 167713 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.
ChEMBL 580 6 1 8 6.2 CNc1ccc(-c2cn([C@@]34CC(F)(F)C(C)[C@H](/C=C/c5ccc(-c6ccccc6C#N)cn5)C3[C@@H](C)OC4=O)nn2)cc1 nan
44310191 211323 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 770 17 6 7 5.2 CCNCCNC(=O)[C@H](CCN)NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
CHEMBL72854 211323 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cellsAbility to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells
ChEMBL 770 17 6 7 5.2 CCNCCNC(=O)[C@H](CCN)NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1 10.1016/s0960-894x(03)00325-1
44432836 94814 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@H]3c4ccccc4C[C@@H]4C(=O)O[C@H](C)[C@@H]43)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL234483 94814 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@H]3c4ccccc4C[C@@H]4C(=O)O[C@H](C)[C@@H]43)ccc2c1 10.1016/j.bmcl.2007.04.061
11516923 78709 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 4 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(Cc4ccccc4)n3)[C@H]12 10.1021/jm0502236
CHEMBL197248 78709 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligandIn vitro inhibitory concentration against human protease activated receptor 1 using [3H]-haTRAP as radioligand
ChEMBL 401 4 0 3 5.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3cccc(Cc4ccccc4)n3)[C@H]12 10.1021/jm0502236
1047175 214853 12 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 393 3 2 5 4.6 Cn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
CHEMBL97706 214853 12 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 393 3 2 5 4.6 Cn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
44281173 122051 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 544 16 7 6 -0.5 NCCC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL33489 122051 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 544 16 7 6 -0.5 NCCC(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44432839 152088 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@H]3c4ccccc4C[C@@H]4C(=O)O[C@@H](C)[C@@H]43)ccc2c1 10.1016/j.bmcl.2007.04.061
CHEMBL391323 152088 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]haTRAP from PAR1Displacement of [3H]haTRAP from PAR1
ChEMBL 385 3 0 4 4.8 COc1ccc2nc(/C=C/[C@H]3c4ccccc4C[C@@H]4C(=O)O[C@@H](C)[C@@H]43)ccc2c1 10.1016/j.bmcl.2007.04.061
44306732 109381 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL304128 109381 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cellsIn vitro displacement of [3H]S-(p-F-Phe)-homoarginine-K Y-NH2 (at a concentration of 10 uM) from thrombin receptor (PAR-1) on the membranes of CHRF-288-11 cells
ChEMBL 775 14 5 6 6.4 NCC(NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1016/s0960-894x(01)00378-x
CHEMBL3143289 217942 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL None None None CC(=O)N(C(=O)/C=C/c1ccccc1)[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
44280685 106527 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 585 15 7 8 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csnn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
CHEMBL285018 106527 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cellsInhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to thrombin receptor (PAR-1) on membranes from CHRF cells
ChEMBL 585 15 7 8 0.6 N=C(N)NCCC[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1csnn1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/s0960-894x(99)00197-3
44290251 107985 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 792 21 8 9 1.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
CHEMBL295849 107985 0 None - 0 Human 4.0 pIC50 = 4.0 Binding
Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.Inhibition of [3H]S-(p-F-Phe)-Har-L-Har-KY-NH2 binding to a thrombin receptor (PAR-1) membrane preparation.
ChEMBL 792 21 8 9 1.7 CNCC(=O)N[C@@H](Cc1ccc(F)cc1)c1nc(C(=O)N[C@H](CC2CCCCC2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cs1 10.1016/s0960-894x(98)00292-3
90663329 113430 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 774 20 9 8 0.8 CC(=O)N(c1cccnc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143292 113430 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 774 20 9 8 0.8 CC(=O)N(c1cccnc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
58045928 140058 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 439 8 1 8 4.1 CCC(CC)Oc1nn2c(=N)n(CC(=O)c3cc(OC)cc(C(C)(C)C)c3)nc2cc1C nan
CHEMBL3704459 140058 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 439 8 1 8 4.1 CCC(CC)Oc1nn2c(=N)n(CC(=O)c3cc(OC)cc(C(C)(C)C)c3)nc2cc1C nan
44305955 107804 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 315 3 2 5 3.4 C=Cc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
CHEMBL294544 107804 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)Inhibitory activity against binding to Thrombin receptor 1 (PAR-1)
ChEMBL 315 3 2 5 3.4 C=Cc1ccc(Cn2ccc3c4c(N)nc(N)nc4ccc32)cc1 10.1016/s0960-894x(99)00339-x
4314709 214449 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 477 9 2 5 7.1 CCCCCCCn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
CHEMBL95359 214449 1 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 477 9 2 5 7.1 CCCCCCCn1c(=N)n(CC(=O)c2cc(C(C)(C)C)c(O)c(C(C)(C)C)c2)c2ccccc21 10.1016/s0960-894x(01)00555-8
72547307 110646 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
CHEMBL3091980 110646 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysisAntagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis
ChEMBL 428 5 0 3 5.0 CN(C1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1)S(C)(=O)=O 10.1021/ml400235c
44418848 89969 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 6.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cc(Cl)ccc4Cl)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218449 89969 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 6.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cc(Cl)ccc4Cl)cn3)[C@H]12 10.1021/jm061043e
17187609 66648 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 300 5 2 2 3.8 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2F)c1 10.1021/ml2002696
CHEMBL1729550 66648 2 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometryInhibition of SFLLRN-NH2-stimulated PAR1-mediated platelet activation in platelet-rich human plasma assessed as surface expression of P-selectin after 20 mins by flow cytometry
ChEMBL 300 5 2 2 3.8 CCCC(=O)Nc1cccc(NC(=O)c2ccccc2F)c1 10.1021/ml2002696
58046023 140062 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 499 11 2 10 3.4 CCC(CC)Oc1cc(C)c2nn(CC(=O)c3cc(OCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
CHEMBL3704463 140062 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL 499 11 2 10 3.4 CCC(CC)Oc1cc(C)c2nn(CC(=O)c3cc(OCCO)c(OC)c(C(C)(C)C)c3)c(=N)n2n1 nan
1047179 214495 5 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 492 6 2 7 4.4 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(CCN3CCOCC3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
CHEMBL95632 214495 5 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against potent thrombin receptor-1 (PAR-1) on human plateletsInhibitory concentration against potent thrombin receptor-1 (PAR-1) on human platelets
ChEMBL 492 6 2 7 4.4 CC(C)(C)c1cc(C(=O)Cn2c(=N)n(CCN3CCOCC3)c3ccccc32)cc(C(C)(C)C)c1O 10.1016/s0960-894x(01)00555-8
68058705 134051 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 433 5 1 4 4.9 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)c3scnc3C)C2)cc1 nan
CHEMBL3658404 134051 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.Binding Assay: Platelet membranes are incubated with 12 nM [3H]haTRAP and test substance in different concentrations in a buffer (50 mM Tris pH 7.5, 10 mM magnesium chloride, 1 mM EGTA, 0.1% BSA) at room temperature for 80 min. Then the mixture is transferred to a filter plate and washed twice with buffer. After addition of scintillation liquid, the radioactivity on the filter is measured in a beta counter.
ChEMBL 433 5 1 4 4.9 CCc1ccc(C2CC(C(=O)Nc3ccccc3)CN(C(=O)c3scnc3C)C2)cc1 nan
76335371 110643 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 394 4 1 3 5.5 COC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL3091977 110643 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysisDisplacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis
ChEMBL 394 4 1 3 5.5 COC(=O)NC1C[C@@H]2CCCC[C@@H]2[C@H]1/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400235c
CHEMBL4115732 219685 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.Binding Assay: The synthesized substances were examined in a PAR1 binding test. This tested whether the substances can inhibit the binding of a radioactively labeled PAR1 agonist known from the literature at the PAR1 receptor (Ho-Sam Ahn, Mol Pharm, 51:350-356, 1997). The human PAR1 receptor was expressed transiently in High Five insect cells. From these cells, after 48 hours, a membrane preparation was produced by standard methods, aliquoted into 10 mM Tris-HCl; 0.3 mM EDTA; 1 mM EGTA; 250 mM sucrose pH 7.5, and stored at -80 C.The substances were preincubated with the membrane at room temperature for 15 minutes, then the radioligand (ALA-(para-F-Phe)-Arg-ChA-homoArg-(3,4-3H-Tyr)-NH2; approx. 40 Ci/mMol) was added. The end concentration of the radioligand in the test buffer (50 mM Tris-HCl; 10 mM MgCl2; 1 mM EGTA; 0.1% BSA; 2% DMSO) was 20 nM, that of the membrane 1 mg/ml. After an incubation time of 60 minutes, 25 uL of the mixture were transferred to a 96-well MultiScreenHTS FB.
ChEMBL None None None None nan
90663307 113422 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1ccc(Cl)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
CHEMBL3143267 113422 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assayAntagonistic activity against tritiated agonist (SFFLRR-NH2, at 25 nM) binding to human platelet membranes measured by the GTPase assay
ChEMBL 861 21 9 8 2.1 CC(=O)N(C(=O)/C=C/c1ccc(Cl)cc1)[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1ccc(NC(=N)N)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm960455s
12018759 117976 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
CHEMBL326456 117976 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1Displacement of [3H]SFFLRR-NH2 from human thrombin receptor PAR-1
ChEMBL 467 8 0 6 6.0 Clc1ccc(-c2cc(N(CCCN3CCCCCC3)Cc3ccc4c(c3)OCO4)on2)cc1 10.1016/s0960-894x(01)00745-4
44264856 103829 0 None - 1 Human 10.4 pKd = 10.4 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 846 17 7 7 6.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccncc1 10.1021/jm000506s
CHEMBL267059 103829 0 None - 1 Human 10.4 pKd = 10.4 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 846 17 7 7 6.1 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccncc1 10.1021/jm000506s
9832212 211728 4 None - 1 Human 9.8 pKd = 9.8 Binding
Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
CHEMBL4226137 211728 4 None - 1 Human 9.8 pKd = 9.8 Binding
Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
CHEMBL7642 211728 4 None - 1 Human 9.8 pKd = 9.8 Binding
Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding Affinity of ligand against Protease-activated Receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 790 15 5 7 6.1 NCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)nn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
10509332 105260 0 None - 1 Human 9.2 pKd = 9.2 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 759 17 7 6 5.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
CHEMBL275946 105260 0 None - 1 Human 9.2 pKd = 9.2 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 759 17 7 6 5.2 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3ccc(F)cc3)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
9919038 173507 0 None - 1 Human 9.1 pKd = 9.1 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
CHEMBL428311 173507 0 None - 1 Human 9.1 pKd = 9.1 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 845 17 7 6 6.7 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)Nc1ccc2c(CN3CCCC3)cn(Cc3c(Cl)cccc3Cl)c2c1)C(=O)NCc1ccccc1 10.1021/jm000506s
10819322 211692 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
CHEMBL7610 211692 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 839 18 7 7 6.4 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4c(Cl)cccc4Cl)c3c2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
10747940 211708 0 None - 1 Human 8.0 pKd = 8.0 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 803 19 7 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CNC4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
CHEMBL7627 211708 0 None - 1 Human 8.0 pKd = 8.0 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 803 19 7 7 5.5 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CNC4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
9853816 104112 0 None - 1 Human 8.7 pKd = 8.7 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
CHEMBL269345 104112 0 None - 1 Human 8.7 pKd = 8.7 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 789 18 6 7 5.0 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
10724264 103966 0 None - 1 Human 8.6 pKd = 8.6 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 855 19 6 8 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
CHEMBL268328 103966 0 None - 1 Human 8.6 pKd = 8.6 Binding
Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)Binding affinity against Protease-activated receptor (PAR-1) using [3H]-s-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2, 10 nM (Kd= 15 nM)
ChEMBL 855 19 6 8 5.8 COc1ccc(C[C@H](NC(=O)Nc2ccc3c(CN4CCCC4)cn(Cc4ccc(OC(F)(F)F)cc4)c3c2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCc2ccccc2)cc1 10.1021/jm000506s
24879036 176219 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 499 5 1 6 5.4 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1021/jm800180e
CHEMBL442649 176219 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 499 5 1 6 5.4 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C#N)c2)cn1 10.1021/jm800180e
24878928 179232 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 548 5 1 5 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm800180e
CHEMBL447996 179232 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 548 5 1 5 5.3 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm800180e
9890926 90063 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
CHEMBL218933 90063 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 471 3 1 4 5.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm061043e
24878927 194237 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 498 5 1 5 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
CHEMBL493975 194237 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 498 5 1 5 4.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
24878984 194511 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2F)cn1 10.1021/jm800180e
CHEMBL495422 194511 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2F)cn1 10.1021/jm800180e
24879079 195687 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 5 1 5 5.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C)c2F)cn1 10.1021/jm800180e
CHEMBL507697 195687 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 5 1 5 5.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C)c2F)cn1 10.1021/jm800180e
24879037 199383 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 508 5 1 5 6.1 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1021/jm800180e
CHEMBL521531 199383 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 508 5 1 5 6.1 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(Cl)c2)cn1 10.1021/jm800180e
76310288 111586 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 476 5 1 4 5.3 CC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109583 111586 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 476 5 1 4 5.3 CC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
52947767 25075 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 504 6 1 6 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270636 25075 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 504 6 1 6 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2OC)cn1 10.1016/j.bmcl.2010.09.009
10246587 78881 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against Protease-activated receptor 1Inhibitory constant against Protease-activated receptor 1
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
CHEMBL197791 78881 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibitory constant against Protease-activated receptor 1Inhibitory constant against Protease-activated receptor 1
ChEMBL 339 3 0 3 4.7 CCc1cccc(/C=C/[C@@H]2[C@@H]3[C@@H](C)OC(=O)[C@@H]3C[C@@H]3CCCC[C@H]32)n1 10.1021/jm0502236
76317514 111587 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 490 6 1 4 5.7 CCC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109584 111587 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 490 6 1 4 5.7 CCC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
76335713 111593 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 505 6 2 4 5.5 CCNC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109590 111593 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 505 6 2 4 5.5 CCNC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
24878827 179411 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 542 5 1 5 6.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/jm800180e
CHEMBL449425 179411 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 542 5 1 5 6.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/jm800180e
76324857 111590 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 545 6 2 5 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNC(=O)C4CCNCC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109587 111590 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 545 6 2 5 5.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNC(=O)C4CCNCC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
58939091 111585 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 506 6 1 5 5.9 CCOC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109582 111585 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 506 6 1 5 5.9 CCOC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
76328415 111592 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 526 7 1 5 5.1 CCS(=O)(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109589 111592 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 526 7 1 5 5.1 CCS(=O)(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
76335711 111577 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 575 5 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)Nc4ccncc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109574 111577 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 575 5 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)Nc4ccncc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
44264660 211872 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 519 8 2 5 4.4 CNc1ccc(C#CC[C@H](NS(=O)(=O)c2ccc3cc(OC)ccc3c2)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
CHEMBL7758 211872 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 519 8 2 5 4.4 CNc1ccc(C#CC[C@H](NS(=O)(=O)c2ccc3cc(OC)ccc3c2)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
52940892 25140 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 489 5 1 6 5.2 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccc(C)cn2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1271149 25140 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 489 5 1 6 5.2 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccc(C)cn2)cn1 10.1016/j.bmcl.2010.09.009
76332097 111591 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 512 6 1 5 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109588 111591 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 512 6 1 5 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNS(C)(=O)=O)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
52949514 25063 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 499 5 1 6 5.4 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2C#N)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270537 25063 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 499 5 1 6 5.4 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccc2C#N)cn1 10.1016/j.bmcl.2010.09.009
90644637 118752 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288436 118752 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
24830436 194394 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 6 1 5 6.0 CCCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL494816 194394 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 6 1 5 6.0 CCCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
76335712 111579 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 568 4 1 5 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)N4CC[C@@H](O)C4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109576 111579 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 568 4 1 5 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)N4CC[C@@H](O)C4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
16214871 25090 3 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270738 25090 3 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccccn2)cn1 10.1016/j.bmcl.2010.09.009
59016155 111581 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 508 5 2 6 4.7 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@]1(O)C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109578 111581 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 508 5 2 6 4.7 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@]1(O)C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
10345602 211666 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 493 7 2 4 4.1 CNc1ccc(C#CC[C@H](NS(=O)(=O)c2ccc3c(c2)CCCC3)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
CHEMBL7587 211666 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 493 7 2 4 4.1 CNc1ccc(C#CC[C@H](NS(=O)(=O)c2ccc3c(c2)CCCC3)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
9804049 140341 2 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against Protease-activated receptor 1Inhibitory constant against Protease-activated receptor 1
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
CHEMBL371069 140341 2 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against Protease-activated receptor 1Inhibitory constant against Protease-activated receptor 1
ChEMBL 455 3 0 3 6.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3CCCC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/jm0502236
59016136 111583 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 434 4 1 4 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CN)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109580 111583 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 434 4 1 4 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CN)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
24878828 194962 5 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 420 3 1 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](N)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
CHEMBL498785 194962 5 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 420 3 1 4 4.8 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](N)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
90644636 118751 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288435 118751 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
90644643 118761 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 459 3 1 6 4.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccn5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288444 118761 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 459 3 1 6 4.2 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccn5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
76310287 111578 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 575 5 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)Nc4cccnc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109575 111578 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 575 5 1 5 7.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)Nc4cccnc4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
76310289 111589 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 531 6 2 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNC(=O)[C@@H]4CCCN4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109586 111589 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 531 6 2 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CNC(=O)[C@@H]4CCCN4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
52942074 25105 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccnc2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270840 25105 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccnc2)cn1 10.1016/j.bmcl.2010.09.009
76310290 111594 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 512 4 1 4 5.8 CNC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
CHEMBL3109591 111594 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 512 4 1 4 5.8 CNC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
90644642 118760 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5F)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288443 118760 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5F)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
52946929 25119 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccncc2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1270942 25119 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 475 5 1 6 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccncc2)cn1 10.1016/j.bmcl.2010.09.009
90644639 118755 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288439 118755 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
90644638 118754 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C#N)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288438 118754 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C#N)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
90644640 118757 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288440 118757 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 476 3 1 5 5.0 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(F)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
127053945 151285 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 417 3 1 4 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
CHEMBL3906979 151285 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 417 3 1 4 4.5 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(O)CC1(F)F nan
127053948 153617 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 488 6 2 5 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NCCO)CC1(F)F nan
CHEMBL3925032 153617 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 488 6 2 5 3.8 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2[C@@H](C)OC(=O)[C@]2(C(=O)NCCO)CC1(F)F nan
127053939 160980 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 401 3 0 3 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
CHEMBL3985900 160980 0 None - 1 Human 8.5 pKi = 8.5 Binding
High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).High Throughput Thrombin Receptor Radioligand Binding Assay: Thrombin receptor antagonists were screened using a modification of the thrombin receptor radioligand binding assay of Ahn et al. (Ahn et al., Mol. Pharmacol., 51:350-356 (1997)). The assay was performed in 96 well Nunc plates (Cat. No. 269620) at a final assay volume of 200 μl. Platelet membranes and [3H]haTRAP were diluted to 0.4 mg/ml and 22.2 nM, respectively, in binding buffer (50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.1% BSA). Stock solutions (10 mM in 100% DMSO) of test compounds were further diluted in 100% DMSO. Unless otherwise indicated, 10 μl of diluted compound solutions and 90 μL of radioligand (a final concentration of 10 nM in 5% DMSO) were added to each well, and the reaction was started by the addition of 100 μl of membranes (40 μg protein/well).
ChEMBL 401 3 0 3 5.4 C[C@H]1[C@H](/C=C/c2ccc(-c3cccc(F)c3)cn2)C2C(CC1(F)F)C(=O)O[C@@H]2C nan
24878982 180353 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 556 5 0 5 6.9 CCOC(=O)N(C)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm800180e
CHEMBL453277 180353 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 556 5 0 5 6.9 CCOC(=O)N(C)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(C(F)(F)F)c3)cn2)C1 10.1021/jm800180e
24878829 179225 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 512 4 1 4 5.9 CC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/jm800180e
CHEMBL447913 179225 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 512 4 1 4 5.9 CC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/jm800180e
76317512 111575 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 540 5 1 4 6.5 CC(C)NC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
CHEMBL3109572 111575 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 540 5 1 4 6.5 CC(C)NC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
90644644 118762 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)CNC(=O)O4 10.1021/ml500008w
CHEMBL3288445 118762 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)CNC(=O)O4 10.1021/ml500008w
76332096 111588 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 505 6 2 5 4.6 C[C@H](N)C(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109585 111588 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 505 6 2 5 4.6 C[C@H](N)C(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
52940897 25152 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 476 5 1 7 4.3 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cncnc2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1271252 25152 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 476 5 1 7 4.3 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cncnc2)cn1 10.1016/j.bmcl.2010.09.009
58187662 111574 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 526 5 1 4 6.1 CCNC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
CHEMBL3109571 111574 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 526 5 1 4 6.1 CCNC(=O)[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(F)(F)F)c2)cn1 10.1021/ml400452v
24879035 183560 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 517 6 2 6 4.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(N)=O)c2)cn1 10.1021/jm800180e
CHEMBL460583 183560 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 517 6 2 6 4.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(C(N)=O)c2)cn1 10.1021/jm800180e
76317513 111580 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 568 4 1 5 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)N4CC[C@H](O)C4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109577 111580 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 568 4 1 5 5.6 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)N4CC[C@H](O)C4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
90644645 118763 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)CNC(=O)O4 10.1021/ml500008w
CHEMBL3288446 118763 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 526 3 1 5 5.9 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C(F)(F)F)c5)cn3)[C@H]12)CNC(=O)O4 10.1021/ml500008w
24878930 195090 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 5 0 5 6.0 CCOC(=O)N(C)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm800180e
CHEMBL500551 195090 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 506 5 0 5 6.0 CCOC(=O)N(C)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm800180e
44428104 151201 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
CHEMBL390630 151201 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human platelet membraneDisplacement of [3H]haTRAP from PAR1 in human platelet membrane
ChEMBL 478 4 0 5 5.2 CCOC(=O)N1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm070704k
24878874 194178 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 477 4 2 4 4.8 CNC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL493633 194178 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 477 4 2 4 4.8 CNC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
24878875 200043 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 491 5 2 4 5.2 CCNC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL523854 200043 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 491 5 2 4 5.2 CCNC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
52942093 25129 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 489 5 1 6 5.2 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cc(C)ccn2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1271045 25129 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 489 5 1 6 5.2 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cc(C)ccn2)cn1 10.1016/j.bmcl.2010.09.009
90644641 118759 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C#N)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288442 118759 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5cccc(C#N)c5)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
24878929 181084 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 527 4 1 6 6.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NC(=O)OC(C)(C)C)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@H]12 10.1021/jm800180e
CHEMBL455020 181084 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 527 4 1 6 6.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NC(=O)OC(C)(C)C)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C#N)c4)cn3)[C@H]12 10.1021/jm800180e
52946957 25161 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 505 6 1 7 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccc(OC)cn2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1271353 25161 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 505 6 1 7 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccc(OC)cn2)cn1 10.1016/j.bmcl.2010.09.009
76285459 111584 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.5 COC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
CHEMBL3109581 111584 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.5 COC(=O)NC[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/ml400452v
86302495 118753 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5C#N)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288437 118753 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5C#N)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
24878983 178245 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 504 6 1 6 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(OC)c2)cn1 10.1021/jm800180e
CHEMBL446344 178245 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 504 6 1 6 5.5 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(OC)c2)cn1 10.1021/jm800180e
24879038 182503 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 510 5 1 5 5.8 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cc(F)cc(F)c2)cn1 10.1021/jm800180e
CHEMBL458264 182503 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 510 5 1 5 5.8 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cc(F)cc(F)c2)cn1 10.1021/jm800180e
24830595 194240 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 478 4 1 5 5.2 COC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL493983 194240 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 478 4 1 5 5.2 COC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
24878873 194177 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 462 4 1 4 5.0 CC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL493632 194177 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 462 4 1 4 5.0 CC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
24878871 194208 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 476 5 1 4 5.4 CCC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
CHEMBL493792 194208 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 476 5 1 4 5.4 CCC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1 10.1021/jm800180e
24878872 194353 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 488 5 1 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NC(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
CHEMBL494618 194353 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 488 5 1 4 5.4 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](NC(=O)C4CC4)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/jm800180e
52949425 25168 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 464 5 1 6 5.1 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccoc2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1271461 25168 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 464 5 1 6 5.1 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2ccoc2)cn1 10.1016/j.bmcl.2010.09.009
10390481 202267 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 481 9 2 4 4.2 CCCc1ccc(S(=O)(=O)N[C@@H](CC#Cc2ccc(NC)cc2)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
CHEMBL553108 202267 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibitory activity against factor XaInhibitory activity against factor Xa
ChEMBL 481 9 2 4 4.2 CCCc1ccc(S(=O)(=O)N[C@@H](CC#Cc2ccc(NC)cc2)C(=O)N(C)C2CCCC2)cc1 10.1016/s0960-894x(99)00125-0
52948306 24954 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 481 5 1 7 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2nccs2)cn1 10.1016/j.bmcl.2010.09.009
CHEMBL1269815 24954 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 481 5 1 7 4.9 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2nccs2)cn1 10.1016/j.bmcl.2010.09.009
59016133 111582 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 435 4 1 4 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CO)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109579 111582 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 435 4 1 4 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](CO)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(F)c4)cn3)[C@H]12 10.1021/ml400452v
10077130 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2010.09.009
4047 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2010.09.009
4870 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2010.09.009
CHEMBL493982 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2010.09.009
DB09030 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of high affinity TRAP form human platelet PAR1Displacement of high affinity TRAP form human platelet PAR1
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1016/j.bmcl.2010.09.009
10077130 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4047 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
4870 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
CHEMBL493982 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
DB09030 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/jm800180e
10077130 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400452v
4047 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400452v
4870 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400452v
CHEMBL493982 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400452v
DB09030 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 10.1021/ml400452v
86302515 118758 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5C#N)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
CHEMBL3288441 118758 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 receptor in human platelet membranes after 1 hr by scintillation counting analysis
ChEMBL 483 3 1 6 4.7 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@]4(CC[C@H]3[C@H](/C=C/c3ccc(-c5ccccc5C#N)cn3)[C@H]12)COC(=O)N4 10.1021/ml500008w
24878981 195634 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 534 7 0 5 6.8 CCCN(C(=O)OCC)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm800180e
CHEMBL506808 195634 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]haTRAP from PAR1 in human plateletsDisplacement of [3H]haTRAP from PAR1 in human platelets
ChEMBL 534 7 0 5 6.8 CCCN(C(=O)OCC)[C@@H]1CC[C@@H]2[C@H](C[C@H]3C(=O)O[C@H](C)[C@H]3[C@H]2/C=C/c2ccc(-c3cccc(F)c3)cn2)C1 10.1021/jm800180e
76332095 111576 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 542 6 2 5 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)NCCO)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
CHEMBL3109573 111576 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysisDisplacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis
ChEMBL 542 6 2 5 5.1 C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](C(=O)NCCO)CC[C@H]3[C@H](/C=C/c3ccc(-c4cccc(C(F)(F)F)c4)cn3)[C@H]12 10.1021/ml400452v
10077130 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C None
4047 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C None
4870 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C None
CHEMBL493982 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C None
DB09030 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
antagonistantagonist
Drug Central 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C None
10077130 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 18447380
4047 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 18447380
4870 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 18447380
CHEMBL493982 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 18447380
DB09030 10779 53 None - 1 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 492 5 1 5 5.6 CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@@H]1[C@H]([C@H]2/C=C/c2ccc(cn2)c2cccc(c2)F)[C@H](OC1=O)C 18447380