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 115209 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 115209 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 208802 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 106649 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 106649 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 99643 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 99643 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 114584 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 114584 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 115533 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 115533 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 208503 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 212658 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 99674 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 99674 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 99247 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 99247 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 24028 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 24028 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 211592 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 102714 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 102714 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 117224 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 117224 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 211585 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 99878 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 99878 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 208697 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 99751 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 99751 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 208711 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 208701 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 114785 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 114785 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 167827 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 167827 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 22698 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 22698 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 115209 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 115209 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 208685 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 208802 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 100103 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 100103 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 210462 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 106699 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 106699 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 99988 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 99988 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 116866 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 116866 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 208725 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 211400 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 211566 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 99677 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 99677 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 210571 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 116871 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 116871 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 114424 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 114424 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 211597 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 100089 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 100089 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 208722 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 116729 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 116729 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 106670 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 106670 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 211401 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 211400 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 167851 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 167851 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 208690 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 98776 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 98776 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 119703 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 119703 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 24283 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 24283 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 211401 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 117174 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 117174 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 213659 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 210610 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 211147 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 24028 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 24028 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 106698 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 106698 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 99957 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 99957 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 208723 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 210567 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 116545 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 116545 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 100020 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 100020 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 117220 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 117220 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 119292 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 119292 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 209917 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 211596 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 115433 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 115433 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 99951 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 99951 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 115119 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 115119 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 112657 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 112657 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 102946 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 102946 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 211146 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 106667 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 106667 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 208719 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 208684 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 209965 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 102915 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 102915 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 116979 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 116979 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 116520 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 116520 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 211599 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 99405 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 99405 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 210738 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 112348 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 112348 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 211142 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 118562 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 118562 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 148624 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 148624 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 171182 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 171182 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 203100 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 203100 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 203653 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 203653 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 75653 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 75653 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 75653 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 161922 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 161922 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 102252 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 102252 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 202908 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 202908 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 104154 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 104154 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 75653 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 75653 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 75653 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 158648 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 158648 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 165035 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 165035 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 165096 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 165096 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 102772 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 102772 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 159476 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 159476 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 177097 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 177097 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 104776 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 104776 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 203823 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 203823 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 211154 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 102712 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 102712 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 109634 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 109634 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 106700 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 106700 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 109692 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 109692 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 5845 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 5845 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 156662 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 156662 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 9422 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 9422 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 111199 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 111199 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 175520 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 175520 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 5845 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 5845 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 8224 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 8224 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 9146 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 9146 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 102602 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 102602 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 96837 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 96837 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 203345 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 203345 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 208093 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 208093 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 109755 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 109755 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 214993 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 214511 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 173918 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 173918 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 9350 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 9350 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 109634 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 109634 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 167916 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 167916 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 156014 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 156014 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 158728 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 158728 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 96837 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 96837 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 157966 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 157966 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 168909 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 168909 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 7499 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 7499 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 211153 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 211166 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 159352 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 159352 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 211175 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 211171 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 214588 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 173918 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 173918 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 177520 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 177520 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 166728 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 166728 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 211164 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 204949 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 204949 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 204949 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 211144 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 102732 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 102732 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 156865 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 156865 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 5551 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 5551 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 32428 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 32428 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 169770 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 169770 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 214914 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 204949 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 204949 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 204949 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 204949 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 204949 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 204949 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 205493 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 205493 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 205531 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 205531 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 211155 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 102711 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 102711 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 202908 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 202908 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 9305 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 9305 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 106659 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 106659 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 102129 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 102129 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 103108 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 103108 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 105126 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 105126 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 156902 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 156902 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 205076 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 205076 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 211165 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 203345 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 203345 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 158677 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 158677 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 111381 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 111381 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 106660 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 106660 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 169770 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 169770 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 109490 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 109490 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 9146 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 9146 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 202862 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 202862 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 157863 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 157863 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 97337 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 97337 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 102252 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 102252 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 106645 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 106645 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 6893 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 6893 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 106639 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 106639 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 106651 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 106651 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 211169 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 167916 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 167916 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 9347 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 9347 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 97337 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 97337 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 211178 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 215469 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 152236 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 152236 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 211141 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 205437 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 205437 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 165080 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 165080 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 106658 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 106658 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 158935 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 158935 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 109160 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 109160 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 214973 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 215298 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 147346 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 147346 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 172105 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 172105 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 178756 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 178756 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 106635 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 106635 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 102732 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 102732 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 204913 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 204913 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 205498 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 205498 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 156655 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 156655 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 106662 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 106662 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 202862 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 202862 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 205465 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 205465 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 517 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 517 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 517 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 517 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 165056 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 165056 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 168208 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 168208 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 96702 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 96702 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 208037 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 208037 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 165080 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 165080 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 170663 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 170663 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 75654 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 75654 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 23324 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 23324 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 23324 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 23324 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 165056 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 165056 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 170663 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 170663 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 108842 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 108842 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 9350 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 9350 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 156378 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 156378 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 106640 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 106640 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 9323 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 9323 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 517 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 517 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 517 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 517 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 23324 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 23324 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 163301 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 163301 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 211162 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 168909 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 168909 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 98294 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 98294 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 5551 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 5551 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 106668 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 106668 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 173918 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 173918 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 7292 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 7292 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 102160 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 102160 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 172848 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 172848 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 110999 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 110999 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 170416 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 170416 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 106666 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 106666 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 102195 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 102195 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 106637 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 106637 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 106657 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 106657 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 170416 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 170416 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 176211 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 176211 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 214218 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 148749 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 148749 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 169668 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 169668 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 106646 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 106646 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 106647 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 106647 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 9306 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 9306 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 102772 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 102772 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 203602 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 203602 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 205432 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 205432 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 205448 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 205448 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 106654 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 106654 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 205532 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 205532 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 102259 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 102259 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 211149 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 176211 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 176211 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 111199 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 111199 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 214045 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 9443 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 9443 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 106636 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 106636 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 203036 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 203036 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 9135 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 9135 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 102711 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 102711 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 106656 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 106656 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 9306 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 9306 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 4007 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 4007 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 4007 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 4007 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 4007 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 211156 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 106671 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 106671 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 102691 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 102691 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 102259 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 102259 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 168208 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 168208 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 204949 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 204949 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 204949 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 214492 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 211158 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 6893 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 6893 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 109778 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 109778 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 110332 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 110332 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 211160 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 102604 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 102604 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 8685 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 8685 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 109122 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 109122 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 211172 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 205055 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 205055 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 172848 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 172848 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 5848 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 5848 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 211143 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 106642 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 106642 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 177067 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 177067 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 158211 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 158211 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 166728 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 166728 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 32428 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 32428 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 214767 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 106650 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 106650 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 5923 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 5923 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 100910 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 100910 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 203547 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 203547 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 203653 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 203653 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 168079 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 168079 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 177134 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 177134 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 102602 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 102602 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 203547 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 203547 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 4007 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 4007 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 4007 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 4007 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 4007 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 203036 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 203036 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 102160 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 102160 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 106644 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 106644 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 9416 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 9416 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 105297 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 105297 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 106669 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 106669 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 106664 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 106664 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 211182 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 214741 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 215157 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 215516 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 111381 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 111381 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 102691 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 102691 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 203100 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 203100 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 100330 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 100330 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 157350 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 157350 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 204987 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 204987 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 205538 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 205538 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 106663 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 106663 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 177512 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 177512 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 211151 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 102129 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 102129 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 32428 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 32428 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 215435 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 215483 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 106641 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 106641 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 103034 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 103034 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 204857 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 204857 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 204994 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 204994 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 211159 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 204866 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 204866 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 158556 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 158556 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 165096 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 165096 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 9328 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 9328 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 211150 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 106638 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 106638 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 32428 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 32428 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 100910 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 100910 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 106643 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 106643 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 156348 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 156348 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 211170 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 157120 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 157120 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 211163 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 106661 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 106661 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 9326 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 9326 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 5848 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 5848 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 9326 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 9326 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 211143 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 205279 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 205279 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 102712 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 102712 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 203823 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 203823 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 102604 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 102604 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 204913 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 204913 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 9450 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 9450 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 82384 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 82384 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 106652 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 106652 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 9347 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 9347 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 159452 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 159452 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 165035 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 165035 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 106655 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 106655 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 211150 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 156344 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 156344 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 171182 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 171182 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 75653 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 75653 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 75653 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 158963 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 158963 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 203602 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 203602 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 106665 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 106665 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 98323 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 98323 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 1616 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 1616 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 1616 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 6137 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 6137 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 6334 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 6334 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 6165 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 6165 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 7478 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 7478 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 6301 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 6301 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 3790 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9315351
3742 3790 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9315351
CHEMBL4065100 3790 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9315351
19323337 1616 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 1616 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 1616 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 3421 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 3421 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 3421 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 3558 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 3558 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 3558 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 517 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 517 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 517 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 517 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

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 DOI
CHEMBL2370701 209917 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 215139 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 214727 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 215131 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 150533 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 150533 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 160432 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 160432 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 148950 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 148950 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 4007 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 4007 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 4007 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 4007 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 4007 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 147652 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 147652 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 151938 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 151938 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 160432 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 160432 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 160710 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 160710 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 160858 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 160858 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 103869 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 103869 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 143302 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 143302 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 159873 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 159873 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 4007 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 4007 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 4007 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 4007 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 4007 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 147841 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 147841 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 148424 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 148424 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 152169 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 152169 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 160695 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 160695 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 160321 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 160321 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 214045 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 140820 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 140820 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 87028 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 87028 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 87972 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 87972 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 97285 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 97285 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 72565 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 72565 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 146832 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 146832 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 148710 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 148710 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 144423 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 144423 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 150289 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 150289 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 140853 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 140853 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 103882 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 103882 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 75407 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 75407 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 76032 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 76032 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 72022 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 72022 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 100599 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 100599 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 162573 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 162573 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 211148 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 207097 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 207097 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 75015 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 75015 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 202908 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 202908 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 134423 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 134423 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 2574 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 2574 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 2574 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 125143 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 125143 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 178561 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 178561 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 99763 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 99763 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 99915 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 99915 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 100282 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 100282 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 167827 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 167827 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 93196 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 93196 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 9328 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 9328 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 106667 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 106667 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 133282 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 133282 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 127271 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 127271 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 127278 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 127278 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 133563 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 133563 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 83289 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 83289 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 133563 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 133563 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 159472 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 159472 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 86694 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 86694 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 133563 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 133563 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 133451 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 133451 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 133563 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 133563 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 127284 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 127284 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 127533 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 127533 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 106658 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 106658 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 211149 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 133277 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 133277 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 207003 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 207003 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 103872 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 103872 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 102602 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 102602 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 132822 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 132822 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 60001 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 60001 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 142614 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 142614 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 211175 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 75655 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 75655 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 102772 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 102772 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 133301 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 133301 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 92953 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 92953 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 125142 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 125142 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 146663 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 146663 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 9347 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 9347 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 211152 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 133292 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 133292 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 211160 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 136560 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 136560 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 87559 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 87559 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 88147 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 88147 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 103218 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 103218 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 4007 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 4007 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 4007 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 4007 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 4007 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 206873 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 206873 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 145704 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 145704 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 103865 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 103865 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 206868 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 206868 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 9306 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 9306 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 116520 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 116520 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 144918 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 144918 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 203441 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 203441 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 138493 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 138493 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 76540 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 76540 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 72103 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 72103 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 203018 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 203018 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 133291 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 133291 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 106657 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 106657 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 75796 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 75796 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 86689 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 86689 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 93112 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 93112 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 73250 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 73250 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 72070 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 72070 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 204275 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 204275 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 140812 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 140812 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 106652 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 106652 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 106665 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 106665 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 87032 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 87032 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 100910 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 100910 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 102711 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 102711 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 204913 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 204913 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 99677 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 99677 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 118078 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 118078 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 125140 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 125140 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 86696 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 86696 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 207960 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 207960 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 125139 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 125139 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 86943 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 86943 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 83428 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 83428 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 168624 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 168624 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 145461 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 145461 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 154717 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 154717 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 127530 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 127530 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 103878 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 103878 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 133283 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 133283 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 133300 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 133300 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 125147 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 125147 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 99247 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 99247 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 115119 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 115119 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 75896 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 75896 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 70378 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 70378 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 146243 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 146243 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 83353 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 83353 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 133293 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 133293 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 76710 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 76710 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 76710 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 76710 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 83401 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 83401 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 93133 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 93133 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 73244 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 73244 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 127531 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 127531 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 86961 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 86961 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 92956 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 92956 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 144479 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 144479 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 127285 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 127285 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 80003 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 80003 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 81099 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 81099 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 5848 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 5848 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 74430 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 74430 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 81099 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 81099 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 71779 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 71779 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 72041 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 72041 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 82467 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 82467 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 71426 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 71426 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 140700 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 140700 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 207636 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 207636 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 100089 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 100089 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 125138 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 125138 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 93192 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 93192 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 106669 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 106669 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 133297 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 133297 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 140248 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 140248 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 87560 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 87560 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 136970 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 136970 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 149414 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 149414 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 106647 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 106647 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 103573 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 103573 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 106654 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 106654 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 159476 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 159476 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 101156 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 101156 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 99951 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 99951 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 116866 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 116866 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 99138 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 99138 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 99643 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 99643 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 116548 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 116548 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 106666 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 106666 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 127280 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 127280 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 23324 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 23324 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 211144 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 154524 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 154524 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 154524 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 83288 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 83288 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 144157 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 144157 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 146839 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 146839 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 127528 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 127528 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 127276 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 127276 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 211170 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 140784 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 140784 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 125146 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 125146 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 100020 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 100020 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 133295 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 133295 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 203002 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 203002 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 165853 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 165853 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 73258 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 73258 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 127282 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 127282 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 152918 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 152918 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 18318 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 18318 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 102129 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 102129 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 75651 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 75651 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 111469 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 111469 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 133289 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 133289 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 106659 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 106659 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 211158 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 211182 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 92951 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 92951 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 72104 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 72104 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 134717 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 134717 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 127274 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 127274 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 102915 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 102915 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 143401 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 143401 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 147496 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 147496 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 103869 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 103869 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 160321 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 160321 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 160388 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 160388 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 147129 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 147129 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 147824 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 147824 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 160246 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 160246 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 154132 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 154132 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 160710 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 160710 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 103882 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 103882 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 144581 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 144581 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 147493 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 147493 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 151362 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 151362 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 153622 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 153622 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 145695 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 145695 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 103882 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 103882 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 144692 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 144692 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 211143 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 73247 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 73247 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 73256 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 73256 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 72106 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 72106 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 154637 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 154637 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 141712 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 141712 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 143881 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 143881 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 204059 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 204059 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 81199 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 81199 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 103877 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 103877 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 114584 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 114584 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 116871 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 116871 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 117224 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 117224 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 119703 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 119703 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 14897 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 14897 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 14897 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 72244 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 72244 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 133294 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 133294 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 147310 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 147310 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 154524 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 154524 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 154524 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 211169 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 93113 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 93113 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 73249 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 73249 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 127535 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 127535 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 86795 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 86795 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 106638 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 106638 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 103870 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 103870 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 103880 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 103880 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 133568 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 133568 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 125145 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 125145 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 206526 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 206526 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 103861 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 103861 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 135266 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 135266 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 6893 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 6893 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 86739 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 86739 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 141280 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 141280 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 80416 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 80416 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 133296 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 133296 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 76602 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 76602 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 93111 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 93111 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 73243 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 73243 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 86737 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 86737 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 86738 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 86738 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 72347 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 72347 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 106671 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 106671 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 103862 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 103862 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 97337 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 97337 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 75800 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 75800 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 100103 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 100103 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 96552 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 96552 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 109490 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 109490 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 93191 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 93191 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 145313 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 145313 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 154834 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 154834 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 73240 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 73240 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 75892 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 75892 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 106661 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 106661 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 211141 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 211143 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 136759 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 136759 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 203811 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 203811 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 103876 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 103876 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 103879 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 103879 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 102252 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 102252 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 99405 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 99405 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 112348 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 112348 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 106662 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 106662 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 133299 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 133299 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 127277 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 127277 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 106648 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 106648 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 106699 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 106699 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 211171 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 211177 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 73241 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 73241 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 133563 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 133563 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 102732 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 102732 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 102714 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 102714 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 117220 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 117220 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 133279 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 133279 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 173542 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 173542 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 173545 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 173545 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 211172 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 127281 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 127281 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 103157 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 103157 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 106649 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 106649 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 106650 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 106650 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 127534 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 127534 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 141198 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 141198 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 142021 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 142021 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 152927 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 152927 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 73245 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 73245 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 72315 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 72315 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 169066 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 169066 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 8224 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 8224 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 133604 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 133604 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 133285 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 133285 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 102259 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 102259 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 202862 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 202862 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 99776 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 99776 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 133288 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 133288 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 106698 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 106698 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 517 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 517 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 517 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 517 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 92860 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 92860 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 92950 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 92950 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 103883 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 103883 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 145667 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 145667 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 140895 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 140895 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 106640 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 106640 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 9146 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 9146 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 32428 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 32428 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 203036 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 203036 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 203345 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 203345 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 100077 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 100077 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 100635 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 100635 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 86736 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 86736 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 75652 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 75652 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 73252 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 73252 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 71298 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 71298 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 71298 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 71298 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 211142 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 101308 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 101308 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 178496 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 178496 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 100104 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 100104 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 140671 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 140671 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 124479 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 124479 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 154563 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 154563 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 154563 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 211154 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 211159 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 75404 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 75404 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 82672 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 82672 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 83421 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 83421 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 136931 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 136931 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 73246 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 73246 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 140571 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 140571 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 103863 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 103863 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 87194 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 87194 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 208159 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 208159 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 106634 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 106634 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 127270 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 127270 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 154439 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 154439 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 154439 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 87029 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 87029 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 140695 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 140695 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 87386 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 87386 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 9350 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 9350 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 77636 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 77636 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 75654 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 75654 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 99922 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 99922 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 106656 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 106656 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 168751 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 168751 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 143395 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 143395 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 144982 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 144982 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 154214 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 154214 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 160707 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 160707 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 144503 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 144503 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 149441 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 149441 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 160858 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 160858 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 144828 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 144828 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 152494 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 152494 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 160800 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 160800 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 153284 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 153284 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 153601 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 153601 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 142723 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 142723 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 159939 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 159939 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 160897 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 160897 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 140778 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 140778 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 140808 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 140808 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 154563 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 154563 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 154563 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 75911 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 75911 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 100640 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 100640 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 71779 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 71779 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 140551 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 140551 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 141326 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 141326 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 203100 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 203100 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 71779 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 71779 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 100640 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 100640 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 75894 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 75894 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 99878 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 99878 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 115433 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 115433 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 100483 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 100483 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 4007 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 4007 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 4007 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 4007 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 4007 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 86991 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 86991 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 204315 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 204315 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 106663 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 106663 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 203823 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 203823 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 115533 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 115533 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 167851 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 167851 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 102946 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 102946 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 75893 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 75893 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 88146 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 88146 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 211153 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 102712 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 102712 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 102237 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 102237 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 69678 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 69678 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 70393 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 70393 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 145977 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 145977 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 103881 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 103881 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 73254 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 73254 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 112602 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 112602 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 143874 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 143874 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 93114 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 93114 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 127529 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 127529 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 103158 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 103158 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 86697 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 86697 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 154863 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 154863 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 203602 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 203602 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 211150 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 211157 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 211173 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 75653 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 75653 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 75653 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 211161 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 150602 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 150602 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 204309 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 204309 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 211151 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 73255 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 73255 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 72143 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 72143 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 106664 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 106664 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 88238 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 88238 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 138413 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 138413 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 102195 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 102195 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 141124 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 141124 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 127275 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 127275 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 208116 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 208116 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 145980 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 145980 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 103875 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 103875 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 88237 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 88237 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 133287 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 133287 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 212911 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 70581 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 70581 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 136775 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 136775 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 143454 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 143454 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 106643 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 106643 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 211146 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 93190 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 93190 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 80579 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 80579 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 137883 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 137883 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 160556 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 160556 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 167916 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 167916 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 75891 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 75891 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 211164 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 75415 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 75415 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 75889 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 75889 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 103878 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 103878 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 63191 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 63191 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 106646 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 106646 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 152556 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 152556 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 150284 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 150284 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 150701 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 150701 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 153595 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 153595 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 152265 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 152265 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 73261 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 73261 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 151825 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 151825 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 160132 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 160132 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 151242 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 151242 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 140828 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 140828 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 106637 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 106637 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 144089 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 144089 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 71409 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 71409 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 71766 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 71766 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 112657 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 112657 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 99674 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 99674 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 119292 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 119292 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 517 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 517 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 517 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 517 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 106641 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 106641 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 83249 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 83249 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 103883 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 103883 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 103883 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 103883 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 169754 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 169754 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 133298 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 133298 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 106700 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 106700 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 211162 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 116979 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 116979 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 141516 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 141516 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 211150 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 103871 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 103871 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 145701 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 145701 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 103130 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 103130 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 106660 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 106660 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 106639 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 106639 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 133563 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 133563 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 141349 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 141349 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 3421 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 3421 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 3421 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 86743 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 86743 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 168909 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 168909 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 98776 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 98776 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 114785 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 114785 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 154525 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 154525 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 154525 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 73248 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 73248 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 203391 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 203391 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 73259 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 73259 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 106636 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 106636 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 135547 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 135547 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 86944 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 86944 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 100062 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 100062 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 72531 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 72531 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 86695 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 86695 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 211147 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 9326 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 9326 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 103860 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 103860 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 211176 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 203956 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 203956 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 75888 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 75888 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 83052 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 83052 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 127272 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 127272 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 133302 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 133302 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 73260 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 73260 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 102099 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 102099 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 154201 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 154201 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 142759 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 142759 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 159876 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 159876 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 103880 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 103880 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 152259 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 152259 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 152536 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 152536 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 140770 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 140770 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 140834 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 140834 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 75429 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 75429 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 77148 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 77148 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 103878 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 103878 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 204255 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 204255 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 106642 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 106642 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 76490 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 76490 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 168991 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 168991 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 203653 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 203653 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 80552 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 80552 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 166400 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 166400 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 173294 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 173294 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 99842 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 99842 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 73251 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 73251 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 203395 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 203395 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 203395 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 203395 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 5845 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 5845 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 59586 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 59586 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 75797 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 75797 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 102838 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 102838 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 82791 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 82791 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 103868 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 103868 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 127532 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 127532 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 102691 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 102691 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 164899 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 164899 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 178997 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 178997 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 99957 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 99957 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 92954 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 92954 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 72337 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 72337 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 211400 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 116729 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 116729 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 214045 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 3558 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 3558 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 3558 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 3558 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 3558 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 3558 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 106668 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 106668 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 102160 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 102160 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 178928 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 178928 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 115269 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 115269 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 154525 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 154525 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 154525 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 100274 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 100274 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 86684 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 86684 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 103864 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 103864 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 152557 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 152557 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 140576 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 140576 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 160768 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 160768 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 103864 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 103864 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 73253 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 73253 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 149441 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 149441 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 160198 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 160198 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 160157 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 160157 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 211156 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 167887 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 167887 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 140733 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 140733 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 140841 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 140841 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 75407 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 75407 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 75407 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 75407 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 5551 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 5551 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 93193 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 93193 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 142913 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 142913 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 75890 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 75890 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 118562 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 118562 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 101245 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 101245 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 125141 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 125141 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 211166 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 211178 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 81356 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 81356 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 76710 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 76710 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 101451 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 101451 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 138640 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 138640 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 127536 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 127536 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 86741 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 86741 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 211167 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 133278 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 133278 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 73263 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 73263 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 203547 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 203547 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 114424 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 114424 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 86794 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 86794 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 208255 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 208255 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 159476 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 159476 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 206899 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 206899 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 103873 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 103873 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 103874 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 103874 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 101538 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 101538 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 140694 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 140694 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 106655 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 106655 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 203029 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 203029 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 145010 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 145010 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 143809 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 143809 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 127283 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 127283 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 148763 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 148763 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 103870 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 103870 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 143428 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 143428 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 211165 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 88016 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 88016 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 151711 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 151711 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 178756 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 178756 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 87245 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 87245 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 211155 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 102158 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 102158 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 169210 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 169210 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 140836 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 140836 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 83236 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 83236 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 72106 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 72106 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 106155 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 106155 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 141378 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 141378 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 81085 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 81085 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 166009 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 166009 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 116796 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 116796 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 117174 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 117174 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 75798 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 75798 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 83426 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 83426 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 72279 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 72279 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 74429 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 74429 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 168208 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 168208 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 211400 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 112797 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 112797 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 141994 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 141994 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 211174 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 99201 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 99201 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 143449 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 143449 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 109634 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 109634 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 59649 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 59649 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 106644 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 106644 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 103867 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 103867 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 127527 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 127527 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 92952 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 92952 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 93115 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 93115 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 149541 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 149541 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 73257 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 73257 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 144507 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 144507 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 103870 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 103870 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 73262 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 73262 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 73242 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 73242 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 140793 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 140793 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 93190 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 93190 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 141582 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 141582 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 74645 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 74645 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 141080 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 141080 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 96837 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 96837 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 166454 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 166454 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 101371 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 101371 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 4007 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 4007 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 4007 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 4007 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 4007 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 127535 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 127535 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 166728 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 166728 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 178515 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 178515 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 133286 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 133286 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 83427 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 83427 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 154439 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 154439 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 154439 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 125148 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 125148 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 138157 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 138157 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 125144 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 125144 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 72106 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 72106 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 72106 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 72106 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 87285 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 87285 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 71895 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 71895 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 99988 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 99988 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 116545 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 116545 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 211145 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 102797 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 102797 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 143671 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 143671 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 86782 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 86782 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 109692 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 109692 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 103880 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 103880 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 211168 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 106651 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 106651 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 160934 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 160934 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 204544 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 204544 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 88039 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 88039 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 71934 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 71934 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 208074 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 208074 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 115273 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 115273 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 145310 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 145310 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 102604 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 102604 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 211163 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 99751 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 99751 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 101208 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 101208 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 106653 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 106653 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 133280 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 133280 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 101027 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 101027 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 207670 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 207670 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 103869 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 103869 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 83194 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 83194 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 59874 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 59874 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 133284 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 133284 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 207716 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 207716 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 127273 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 127273 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 103866 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 103866 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 212906 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 106645 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 106645 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 111199 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 111199 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 97054 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 97054 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 204949 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 204949 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 204949 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 98484 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 98484 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 166728 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 166728 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 204913 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 204913 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 204929 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 204929 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 97337 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 97337 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 97191 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 97191 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 169440 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 169440 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 172453 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 172453 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 83288 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 83288 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 187458 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 187458 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 187732 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 187732 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 188908 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 188908 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 192604 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 192604 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 104809 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 104809 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 18303 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 18303 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 72106 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 72106 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 104810 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 104810 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 104816 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 104816 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 172632 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 172632 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 104813 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 104813 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 104808 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 104808 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 104815 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 104815 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 104800 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 104800 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 205093 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 205093 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 18368 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 18368 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 104814 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 104814 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 18291 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 18291 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 111975 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 111975 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 187615 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 187615 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 104802 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 104802 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 18318 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 18318 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 104804 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 104804 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 204887 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 204887 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 133563 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 133563 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 104806 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 104806 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 188183 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 188183 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 111974 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 111974 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 111984 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 111984 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 104801 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 104801 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 104812 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 104812 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 18333 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 18333 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 104817 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 104817 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 111983 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 111983 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 18347 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 18347 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 111978 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 111978 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 111977 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 111977 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 111980 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 111980 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 144507 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 144507 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 146839 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 146839 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 154201 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 154201 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 173574 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 173574 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 172446 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 172446 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 104798 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 104798 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 111985 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 111985 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 104811 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 104811 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 18380 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 18380 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 104797 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 104797 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 176781 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 176781 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 104803 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 104803 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 111986 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 111986 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 188311 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 188311 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 144423 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 144423 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 187399 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 187399 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 193264 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 193264 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 18357 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 18357 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 111982 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 111982 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 174305 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 174305 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 18389 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 18389 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 104807 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 104807 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 111976 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 111976 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 171466 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 171466 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 175724 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 175724 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 187461 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 187461 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 187398 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 187398 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 187429 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 187429 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 187574 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 187574 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 18396 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 18396 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 195488 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 195488 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 18182 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 18182 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 104805 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 104805 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 111981 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 111981 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 188855 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 188855 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 104799 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 104799 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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 4007 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