Initializing potency table...
Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
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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 | |
CHEMBL2216803 | 84371 | None | 0 | Human | Binding | EC50 | = | 1.00 | 9.00 | - | 1 | Allosteric activation of human FSH receptor | ChEMBL | 653.2 | 10 | 2 | 6 | 5.75 | COc1ccc(CCNC(=O)C[C@H]2S[C@@H](c3ccc(C#Cc4ccccc4)cc3)N(c3ccc(C(N)=O)c(Cl)c3)C2=O)cc1OC | https://dx.doi.org/10.1016/j.bmc.2012.03.069 | |
CHEMBL3263667 | 111198 | None | 0 | Human | Binding | EC50 | = | 100.00 | 7.00 | - | 1 | Positive allosteric modulation of human FSHR expressed in rat granulocytes assessed as FSH-induced estradiol production after 72 hrs by radioimmunossay | ChEMBL | 570.3 | 10 | 2 | 7 | 4.18 | Cc1ccccc1N1CCN(c2ccc(C(=O)NCCCN3CCCC3=O)cc2NC(=O)c2coc(C3CC3)n2)CC1 | https://dx.doi.org/10.1021/acsmedchemlett.6b00082 | |
CHEMBL3263691 | 111203 | None | 0 | Human | Binding | EC50 | = | 100.00 | 7.00 | - | 1 | Positive allosteric modulation of human FSHR expressed in rat granulocytes assessed as FSH-induced estradiol production after 72 hrs by radioimmunossay | ChEMBL | 555.3 | 10 | 3 | 9 | 3.31 | Cc1ccccc1N1CCN(c2ccc(C(=O)NCCCc3nn[nH]n3)cc2NC(=O)c2coc(C3CC3)n2)CC1 | https://dx.doi.org/10.1021/acsmedchemlett.6b00082 | |
CHEMBL3809148 | 140518 | None | 0 | Human | Binding | EC50 | = | 100.00 | 7.00 | - | 1 | Positive allosteric modulation of human FSHR expressed in rat granulocytes assessed as FSH-induced estradiol production after 72 hrs by radioimmunossay | ChEMBL | 557.3 | 9 | 2 | 5 | 4.46 | Cc1ccccc1N1CCN(c2ccc(C(=O)NCCCN3CCCC3=O)cc2NC(=O)c2ccc(F)cc2)CC1 | https://dx.doi.org/10.1021/acsmedchemlett.6b00082 | |
CHEMBL4780505 | 182103 | None | 0 | Human | Binding | IC50 | = | 8030.00 | 5.09 | - | 2 | Antagonist activity at human FSHR expressed in CHO-K1 cells by PathHunter beta-arrestin assay | ChEMBL | 565.2 | 4 | 2 | 6 | 5.09 | COC(=O)[C@H]1[C@@H](O)CC[C@H]2CN(C#N)CCc3c([nH]c4ccccc34)[C@H](OCc3ccc(Br)cc3)C[C@@H]21 | https://dx.doi.org/10.1016/j.bmc.2020.115546 | |
CHEMBL5267037 | 193615 | None | 0 | Human | Binding | IC50 | = | 1440.00 | 5.84 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 439.2 | 4 | 1 | 3 | 5.65 | CC(=O)N1c2ncc(NC(=O)CCc3cccc(Cl)c3)cc2C2(CCCCC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5267043 | 193617 | None | 0 | Human | Binding | IC50 | = | 156.00 | 6.81 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 476.2 | 3 | 1 | 5 | 4.96 | CC(=O)N1c2cnc(NC(=O)OCC3(C(F)(F)F)CC3)nc2C2(CCC(F)(F)CC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5267166 | 193619 | None | 0 | Human | Binding | IC50 | = | 6000.00 | 5.22 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 440.2 | 3 | 1 | 3 | 6.44 | CC(=O)N1c2ccc(NC(=O)OCc3cccc(Cl)c3)cc2C2(CCCCC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5268512 | 193677 | None | 0 | Human | Binding | IC50 | = | 5670.00 | 5.25 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 387.3 | 2 | 1 | 4 | 5.02 | CC(=O)N1c2ncc(NC(=O)OCC(C)(C)C)cc2C2(CCCCC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5268829 | 193688 | None | 0 | Human | Binding | IC50 | = | 10000.00 | 5.00 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 410.2 | 1 | 1 | 5 | 4.42 | CC(=O)N1c2cnc(NC(=O)OC(C)(C)C)nc2C2(CCC(F)(F)CC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5270266 | 193735 | None | 0 | Human | Binding | IC50 | = | 214.00 | 6.67 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 408.2 | 3 | 1 | 5 | 4.57 | CC(=O)N1c2cnc(NC(=O)OCc3ccccc3)nc2C2(CCCCC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5270771 | 193758 | None | 0 | Human | Binding | IC50 | = | 1750.00 | 5.76 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 478.2 | 3 | 1 | 5 | 5.47 | CC(=O)N1c2cnc(NC(=O)OCc3cccc(Cl)c3)nc2C2(CCC(F)(F)CC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5271120 | 193778 | None | 0 | Human | Binding | IC50 | = | 2550.00 | 5.59 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 386.3 | 2 | 1 | 3 | 5.63 | CC(=O)N1c2ccc(NC(=O)OCC(C)(C)C)cc2C2(CCCCC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5273361 | 193867 | None | 0 | Human | Binding | IC50 | = | 322.00 | 6.49 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 424.2 | 4 | 1 | 2 | 5.87 | CC(=O)N1c2ccc(NC(=O)CCc3cccc(Cl)c3)cc2C2(CCCCC2)C1C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5275140 | 193949 | None | 0 | Human | Binding | IC50 | = | 606.00 | 6.22 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 438.2 | 3 | 1 | 5 | 5.05 | CC(=O)N1c2cnc(NC(=O)OC(C)(C)C(C)C)nc2C2(CCC(F)(F)CC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5275472 | 193965 | None | 0 | Human | Binding | IC50 | = | 912.00 | 6.04 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 424.2 | 2 | 1 | 5 | 4.66 | CC(=O)N1c2cnc(NC(=O)OCC(C)(C)C)nc2C2(CCC(F)(F)CC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5275619 | 193975 | None | 0 | Human | Binding | IC50 | = | 432.00 | 6.37 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 388.2 | 2 | 1 | 5 | 4.42 | CC(=O)N1c2cnc(NC(=O)OCC(C)(C)C)nc2C2(CCCCC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5279687 | 194145 | None | 0 | Human | Binding | IC50 | = | 466.00 | 6.33 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 440.2 | 4 | 1 | 4 | 5.05 | CC(=O)N1c2cnc(NC(=O)CCc3cccc(Cl)c3)nc2C2(CCCCC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5280508 | 194181 | None | 0 | Human | Binding | IC50 | = | 458.00 | 6.34 | - | 3 | Antagonist activity at human FSHR expressed in HEK293 cells assessed as reduction in cAMP production incubated for 2 hrs by Eu-cAMP tracer based TR-FRET assay | ChEMBL | 438.2 | 4 | 1 | 2 | 6.26 | CC(=O)N1c2ccc(NC(=O)CCc3cccc(Cl)c3)cc2C2(CCCCC2)C1(C)C | https://dx.doi.org/10.1016/j.bmc.2023.117258 | |
CHEMBL5281228 | 194216 | None | 0 | Human | Binding | IC50 | = | 17.00 | 7.77 | - | 2 | Allosteric antagonist activity at human FSHR expressed in CHO cells assessed as inhibition of FSH-induced activity incubated for 4 hrs by CRE-luciferase assay | ChEMBL | 480.2 | 5 | 1 | 2 | 6.34 | CC(=O)N1CCC(C)(c2ccccc2)c2cc(NC(=O)CCc3cccc(C(F)(F)F)c3)ccc21 | https://dx.doi.org/10.1016/j.bmc.2023.117258 |
Showing 1 to 20 of 30 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
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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 | |