Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 44354055 | 115273 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 115273 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 211261 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | 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 | 106705 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 106705 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | 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 | 99697 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 99697 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 114648 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 114648 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 115597 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 115597 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 210962 | None | 22 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | 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 | 215118 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | 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 | 99728 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | 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 | 99728 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | 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 | 99301 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | 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 | 99301 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | 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 | 24036 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | 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 | 24036 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | 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 | 214051 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | 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 | 102769 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | 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 | 102769 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | 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 | 117288 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | 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 | 117288 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | 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 | 214044 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | 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 | 99932 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | 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 | 99932 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | 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 | 211156 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | 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 | 99805 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | 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 | 99805 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | 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 | 211170 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | 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 | 211160 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | 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 | 114849 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | 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 | 114849 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | 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 | 167930 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | 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 | 167930 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | 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 | 22706 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | 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 | 22706 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | 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 | 115273 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | 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 | 115273 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | 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 | 211144 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | 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 | 211261 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | 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 | 100157 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | 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 | 100157 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | 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 | 212921 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 44 | 2 | 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 | 106755 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | 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 | 106755 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | 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 | 100042 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | 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 | 100042 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | 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 | 116930 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | 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 | ||
Showing 1 to 50 of 740 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
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Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| CHEMBL2370701 | 212376 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | 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 | 217629 | None | 0 | Human | Binding | pEC50 | = | 4.3 | 4.3 | - | 0 | 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 | 217215 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | 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 | 217621 | None | 0 | Human | Binding | pEC50 | = | 4 | 4.0 | - | 0 | 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 | 150621 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 150621 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160526 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160526 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 149038 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 149038 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 1 | 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 | ||
| 10077130.0 | 4007 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 1 | 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 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 1 | 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 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 1 | 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 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 1 | 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 | None | 47 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 1 | 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 | 147740 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 147740 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 152027 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 152027 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160526 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160526 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160804 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160804 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160952 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160952 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 103924 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | 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 | 103924 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | 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 | 143389 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 143389 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 159967 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 159967 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | None | 47 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 1 | 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 | ||
| 10077130.0 | 4007 | None | 47 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 1 | 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 | None | 47 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 1 | 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 | None | 47 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 1 | 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 | None | 47 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 1 | 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 | None | 47 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 1 | 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 | 147929 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 147929 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 148512 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 148512 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 152258 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 152258 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160789 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160789 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160415 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | 160415 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (prepared in water) at a concentration equal to the effective concentration that achieves 80% activation of signaling on the day of the experiment.FLIPR Assay: HEK 293 Cells were grown in media containing DMEM, 10% FBS pen/strep/L-Glutamine and non-essential amino acids. The cells were plated in 384-well PDL coated plates at 12000 cells/well and incubated overnight at 37° C./5% CO2. Media was then removed from the cells, which were then incubated with buffer (Hank's containing HEPES and Chaps) containing FLIPR calcium-5 dye, made with buffer containing probenecid, for 60 minutes at 37° C. Varying concentrations of compound in a final concentration of 5% DMSO were then added to the cells and incubated at 25° C. for 30 minutes. The plates were then added to the FLIPR Tetra and the device added a concentration of a PAR1 selective receptor-activating peptide with the sequence Ala-parafluoroPhe-Arg-Cha-Cit-Try-Nh2 (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 | ||
| CHEMBL4630644 | 216501 | None | 4 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | 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@H](c2ccc(OC(F)(F)F)cc2)C[C@H](c2nc(C3CC3)no2)C1 | 10.6019/CHEMBL5210121 | ||||
| 127050657 | 140907 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | 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 | ||
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