Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
13,14-dihydro-16-m-chlorophenoxy-w-tetranor-PGF1α | 16 | None | 0 | Human | Binding | IC50 | = | 1.00 | 9.00 | - | 5 | Displacement of [3H]PGF2-alpha from human FP-receptor expressed in CHO-KI cells | ChEMBL | 428.2 | 13 | 4 | 5 | 3.64 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)COc1cccc(Cl)c1 | https://dx.doi.org/10.1016/s0960-894x(00)00273-0 | |
13,14-dihydro-16-m-chlorophenoxy-w-tetranor-PGF1α | 16 | None | 0 | Human | Binding | IC50 | = | 2.60 | 8.59 | - | 5 | Affinity for human Prostanoid FP receptor expressed in COS-7 cells | ChEMBL | 428.2 | 13 | 4 | 5 | 3.64 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)COc1cccc(Cl)c1 | https://dx.doi.org/10.1021/jm990542v | |
AH-23848 | 218901 | 3H-PGF2Alpha | 0 | Human | Binding | pKi | = | 10000.00 | 5.00 | -10 | 6 | - | PDSP KiDatabase | 477.3 | 11 | 1 | 5 | 5.08 | O=C1CCC(CCC(=CCC(C(=O)O)N2CCOCC2)OCc2ccc(-c3ccccc3)cc2)C1 | - | |
AH-23848 | 218901 | 3H-PGF2Alpha | 0 | Human | Binding | pKi | = | 10000.00 | 5.00 | -10 | 6 | - | PDSP KiDatabase | 477.3 | 11 | 1 | 5 | 5.08 | O=C1CCC(CCC(=CCC(C(=O)O)N2CCOCC2)OCc2ccc(-c3ccccc3)cc2)C1 | - | |
AH6809 | 320 | 3H-PGF2Alpha | 49 | Human | Binding | pKi | = | 10000.00 | 5.00 | -30 | 10 | - | PDSP KiDatabase | 298.1 | 3 | 1 | 4 | 3.43 | CC(C)Oc1ccc2c(=O)c3cc(C(=O)O)ccc3oc2c1 | - | |
AS604872 | 486 | None | 0 | Human | Binding | pKi | = | - | 7.50 | - | 1 | Unclassified | Guide to Pharmacology | 515.1 | 7 | 1 | 5 | 4.72 | O=C(N[C@H](c1ccccc1)c1ccccn1)[C@@H]1SCCN1S(=O)(=O)c1ccc(-c2ccccc2)cc1 | https://pubmed.ncbi.nlm.nih.gov/17618756 | |
BAY-403 | 216506 | None | 0 | Human | Binding | IC50 | = | 1200.00 | 5.92 | - | 2 | Bayer inhouse assay (human) | ChEMBL | - | - | - | - | - | Cc1c(N2CCNCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.6019/CHEMBL4630901 | |
BAY-6672 | 586 | None | 11 | Human | Binding | pIC50 | = | - | 7.66 | - | 4 | Receptor binding determined in a proprietary hFP-R binding assay. | Guide to Pharmacology | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://pubmed.ncbi.nlm.nih.gov/32969660 | |
BAY-6672 | 586 | None | 11 | Human | Binding | IC50 | = | 18.00 | 7.75 | - | 4 | Functional cellular assay: MCP-1 inhibition | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.6019/CHEMBL4630901 | |
BAY-6672 | 586 | None | 11 | Human | Binding | IC50 | = | 12.00 | 7.92 | - | 4 | Functional cellular assay: cytokine-induced neutrophil-attracting chemokine (KC) inhibition | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.6019/CHEMBL4630901 | |
BAY-6672 | 586 | None | 11 | Human | Binding | IC50 | = | 52.00 | 7.28 | - | 4 | Wistar rat tissue assay of PGF2alpha-induced contraction of (nonpregnant) uterus at Panlabs | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.6019/CHEMBL4630901 | |
BAY-6672 | 586 | None | 11 | Human | Binding | IC50 | = | 11.00 | 7.96 | - | 4 | Bayer inhouse assay (rat) | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.6019/CHEMBL4630901 | |
BAY-6672 | 586 | None | 11 | Human | Binding | IC50 | = | 11.00 | 7.96 | - | 4 | Bayer inhouse assay (human) | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.6019/CHEMBL4630901 | |
BAY-6672 | 586 | None | 11 | Human | Binding | IC50 | = | 22.00 | 7.66 | - | 4 | Panlabs binding assay | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.6019/CHEMBL4630901 | |
BAY-6672 | 586 | None | 11 | Human | Binding | Ki | = | 14.80 | 7.83 | - | 4 | Prostanoid FP Eurofins-Panlabs radioligand binding assay | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.6019/CHEMBL4630901 | |
BAY-6672 | 586 | None | 11 | Human | Binding | IC50 | = | 21.00 | 7.68 | - | 4 | Prostanoid FP Eurofins-Panlabs radioligand binding assay | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.6019/CHEMBL4630901 | |
BAY-6672 | 586 | None | 11 | Human | Binding | Ki | = | 16.00 | 7.80 | - | 4 | Displacement of [3H]PGF2alpha from full-length recombinant human FP receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.1021/acs.jmedchem.0c00834 | |
BAY-6672 | 586 | None | 11 | Human | Binding | IC50 | = | 22.00 | 7.66 | - | 4 | Displacement of [3H]PGF2alpha from full-length recombinant human FP receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.1021/acs.jmedchem.0c00834 | |
BAY-6672 | 586 | None | 11 | Rat | Binding | IC50 | = | 52.00 | 7.28 | - | 4 | Antagonist activity at FPR in Wistar rat assessed as inhibition of PGF2alpha-induced uterus contraction | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.1021/acs.jmedchem.0c00834 | |
BAY-6672 | 586 | None | 11 | Rat | Binding | IC50 | = | 11.00 | 7.96 | - | 4 | Antagonist activity at rat FPR stably expressed in CHO cells assessed as inhibition of PGF2alpha-induced calcium flux preincubated for 10 mins followed by PGF2alpha stimulation and measured for 120 secs by fluo-8 AM dye based fluorescence assay | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.1021/acs.jmedchem.0c00834 |
Showing 1 to 20 of 251 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
13,14-dihydro-16-m-chlorophenoxy-w-tetranor-PGF1α | 16 | None | 0 | Human | Functional | pIC50 | None | - | 8.80 | 1258 | 5 | Unclassified | Guide to Pharmacology | 428.2 | 13 | 4 | 5 | 3.64 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)COc1cccc(Cl)c1 | https://pubmed.ncbi.nlm.nih.gov/10715159 | |
13,14-dihydro-16-m-chlorophenoxy-w-tetranor-PGF1α | 16 | None | 0 | Human | Functional | EC50 | = | 9.00 | 8.05 | 1258 | 5 | Functional activity in RAT-1cells, transiently-transfected with human FP-receptor (% of control ligand, fluprostenol=100%) | ChEMBL | 428.2 | 13 | 4 | 5 | 3.64 | O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)COc1cccc(Cl)c1 | https://dx.doi.org/10.1016/s0960-894x(00)00273-0 | |
AL-8810 | 325 | None | 0 | Rat | Functional | pEC50 | None | - | 6.70 | 1 | 2 | Unclassified | Guide to Pharmacology | 402.2 | 9 | 3 | 3 | 3.85 | O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H](F)[C@@H]1/C=C/[C@H](O)C1Cc2ccccc2C1 | https://pubmed.ncbi.nlm.nih.gov/10454504 | |
AL-8810 | 325 | None | 0 | Mouse | Functional | pEC50 | None | - | 6.70 | -1 | 2 | Unclassified | Guide to Pharmacology | 402.2 | 9 | 3 | 3 | 3.85 | O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H](F)[C@@H]1/C=C/[C@H](O)C1Cc2ccccc2C1 | https://pubmed.ncbi.nlm.nih.gov/10454504 | |
AL12180 | 323 | None | 0 | Human | Functional | pEC50 | = | - | 7.80 | - | 1 | Unclassified | Guide to Pharmacology | 410.1 | 11 | 3 | 5 | 3.21 | O=C(O)CC/C=C\CC[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@@H](O)COc1cccc(Cl)c1 | https://pubmed.ncbi.nlm.nih.gov/17076623 | |
BAY-6672 | 586 | None | 11 | Human | Functional | IC50 | = | 11.00 | 7.96 | -1 | 4 | Antagonist activity at human FPR expressed in human Chem-1 cells assessed as inhibition of PGF2alpha-induced calcium flux preincubated for 10 mins followed by PGF2alpha stimulation and measured for 120 secs by fluo-8 AM dye based fluorescence assay | ChEMBL | 543.1 | 8 | 2 | 4 | 5.94 | Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl | https://dx.doi.org/10.1021/acs.jmedchem.0c00834 | |
bimatoprost | 658 | None | 0 | Human | Functional | pIC50 | = | - | 5.30 | - | 1 | Unclassified | Guide to Pharmacology | 415.3 | 12 | 4 | 4 | 3.15 | CCNC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCc1ccccc1 | https://pubmed.ncbi.nlm.nih.gov/12606640 | |
bimatoprost (free acid form) | 659 | None | 34 | Human | Functional | pIC50 | = | - | 8.70 | 1737 | 2 | Unclassified | Guide to Pharmacology | 388.2 | 11 | 4 | 4 | 3.10 | O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCc1ccccc1 | https://pubmed.ncbi.nlm.nih.gov/10952685 | |
bimatoprost (free acid form) | 659 | None | 34 | Human | Functional | EC50 | = | 12.00 | 7.92 | 1737 | 2 | Agonist activity at human prostaglandin FP receptor expressed in CHO cells assessed as increase in intracellular calcium level by Fura 2-AM dye based fluorescence assay | ChEMBL | 388.2 | 11 | 4 | 4 | 3.10 | O=C(O)CCC/C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)CCc1ccccc1 | https://dx.doi.org/10.1021/acsmedchemlett.6b00415 | |
CHEMBL166351 | 57560 | None | 0 | Human | Functional | Ki | = | 41000.00 | 4.39 | - | 8 | Antagonistic activity at Prostanoid FP receptor in human was determined | ChEMBL | 306.0 | 4 | 1 | 1 | 4.68 | O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)c(Cl)c1 | https://dx.doi.org/10.1016/s0960-894x(01)00056-7 | |
CHEMBL182117 | 64881 | None | 0 | Human | Functional | EC50 | = | 293.00 | 6.53 | - | 2 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells | ChEMBL | 390.2 | 12 | 3 | 5 | 2.95 | O=C(O)CCCC/C=C\C[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@@H](O)COc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2004.06.037 | |
CHEMBL183193 | 65601 | None | 0 | Human | Functional | EC50 | = | 23.00 | 7.64 | - | 2 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells | ChEMBL | 424.2 | 12 | 3 | 5 | 3.60 | O=C(O)CC/C=C\CCC[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@@H](O)COc1cccc(Cl)c1 | https://dx.doi.org/10.1016/j.bmcl.2004.06.037 | |
CHEMBL184249 | 66181 | None | 0 | Human | Functional | EC50 | = | 57.00 | 7.24 | - | 2 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells | ChEMBL | 390.2 | 12 | 3 | 5 | 2.95 | O=C(O)CC/C=C\CCC[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@@H](O)COc1ccccc1 | https://dx.doi.org/10.1016/j.bmcl.2004.06.037 | |
CHEMBL184264 | 66185 | None | 0 | Human | Functional | EC50 | = | 194.00 | 6.71 | - | 2 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells | ChEMBL | 424.2 | 12 | 3 | 5 | 3.60 | O=C(O)CCCC/C=C\C[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@H](O)COc1cccc(Cl)c1 | https://dx.doi.org/10.1016/j.bmcl.2004.06.037 | |
CHEMBL185466 | 66709 | None | 0 | Human | Functional | EC50 | = | 899.00 | 6.05 | - | 1 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells | ChEMBL | 458.2 | 12 | 3 | 5 | 3.97 | O=C(O)CCCC/C=C\C[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@H](O)COc1cccc(C(F)(F)F)c1 | https://dx.doi.org/10.1016/j.bmcl.2004.06.037 | |
CHEMBL185484 | 66712 | None | 0 | Human | Functional | EC50 | = | 2.70 | 8.57 | - | 2 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells | ChEMBL | 500.2 | 12 | 3 | 6 | 4.43 | CC(C)OC(=O)CCC/C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1/C=C/C(O)COc1cccc(C(F)(F)F)c1 | https://dx.doi.org/10.1016/j.bmcl.2004.06.037 | |
CHEMBL185559 | 66728 | None | 0 | Human | Functional | EC50 | = | 67.00 | 7.17 | - | 2 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells | ChEMBL | 458.2 | 12 | 3 | 5 | 3.97 | O=C(O)CC/C=C\CCC[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@@H](O)COc1cccc(C(F)(F)F)c1 | https://dx.doi.org/10.1016/j.bmcl.2004.06.037 | |
CHEMBL186192 | 66868 | None | 0 | Human | Functional | EC50 | = | 187.00 | 6.73 | - | 2 | Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells | ChEMBL | 458.2 | 12 | 3 | 5 | 3.97 | O=C(O)CCCC/C=C\C[C@H]1[C@@H](O)CO[C@@H]1/C=C/[C@@H](O)COc1cccc(C(F)(F)F)c1 | https://dx.doi.org/10.1016/j.bmcl.2004.06.037 | |
CHEMBL1910324 | 211537 | None | 7 | Mouse | Functional | IC50 | = | 13.00 | 7.89 | 1 | 3 | Antagonist activity at FP receptor in mouse myometrial strip assessed as inhibition of PGF-2alpha-induced contractions | ChEMBL | - | - | - | - | - | CC[C@@H](C)[C@@H](N)C(=O)N[C@H](CC(C)C)C(=O)NCC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCCN)C(=O)O | https://dx.doi.org/10.1021/jm200608k | |
CHEMBL1910324 | 211537 | None | 7 | Bovine | Functional | IC50 | = | 13.00 | 7.89 | -1 | 3 | Antagonist activity at FP receptor in bovine myometrial strip assessed as inhibition of PGF-2alpha-induced contractions | ChEMBL | - | - | - | - | - | CC[C@@H](C)[C@@H](N)C(=O)N[C@H](CC(C)C)C(=O)NCC(=O)N[C@H](Cc1cnc[nH]1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCCN)C(=O)O | https://dx.doi.org/10.1021/jm200608k |
Showing 1 to 20 of 128 entries