Ligand source activities (1 row/activity)
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Assay information | Chemical information | ||||||||||||||||||
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Sel. page | Common name
| GPCRdb ID
| #Vendors | Reference ligand
| Fold selectivity | # Tested GPCRs | Species
| p-value (-log) | Activity Type
| Activity Relation
| Activity Value
| AssayType
| Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
|
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Assay information
| Chemical information
| ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| #Vendors | Reference ligand
| Fold selectivity | # Tested GPCRs | Species
| p-value (-log) | Activity Type
| Activity Relation
| Activity Value
| AssayType
| Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
|
53322111 | 57366 | 0 | None | 125 | 2 | Human | 9.0 | pEC50 | = | 9 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 482 | 7 | 4 | 8 | 3.4 | C#CCNC(=O)CNc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 | 10.1021/ml100229v | |
CHEMBL1651721 | 57366 | 0 | None | 125 | 2 | Human | 9.0 | pEC50 | = | 9 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 482 | 7 | 4 | 8 | 3.4 | C#CCNC(=O)CNc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 | 10.1021/ml100229v | |
53320793 | 57368 | 0 | None | - | 1 | Human | 8.0 | pEC50 | = | 8 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1136 | 18 | 5 | 17 | 10.1 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
CHEMBL1651723 | 57368 | 0 | None | - | 1 | Human | 8.0 | pEC50 | = | 8 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1136 | 18 | 5 | 17 | 10.1 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
11618319 | 79779 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation |
ChEMBL | 403 | 4 | 1 | 8 | 4.6 | COc1cccc(-c2nc(SC)nc3sc(C(=O)OC(C)(C)C)c(N)c23)c1 | 10.1021/jm060247s | |
CHEMBL211871 | 79779 | 0 | None | - | 1 | Human | 6.0 | pEC50 | = | 6.0 | Functional | Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation |
ChEMBL | 403 | 4 | 1 | 8 | 4.6 | COc1cccc(-c2nc(SC)nc3sc(C(=O)OC(C)(C)C)c(N)c23)c1 | 10.1021/jm060247s | |
11509369 | 80008 | 0 | None | - | 1 | Human | 5.9 | pEC50 | = | 5.9 | Functional | Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation |
ChEMBL | 390 | 3 | 2 | 6 | 4.3 | CSc1nc(-c2cccc(F)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/jm060247s | |
CHEMBL212815 | 80008 | 0 | None | - | 1 | Human | 5.9 | pEC50 | = | 5.9 | Functional | Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation |
ChEMBL | 390 | 3 | 2 | 6 | 4.3 | CSc1nc(-c2cccc(F)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/jm060247s | |
44440750 | 97327 | 0 | None | - | 1 | Human | 4.9 | pEC50 | = | 4.9 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 610 | 13 | 3 | 7 | 6.2 | CC(C)(C)Oc1ccc(C[C@H](NC(=O)CCCCNc2cc(-c3cccnc3)nn2-c2ccc(C(C)(C)C)cc2)C(N)=O)cc1 | 10.1016/j.bmcl.2006.12.062 | |
CHEMBL269261 | 97327 | 0 | None | - | 1 | Human | 4.9 | pEC50 | = | 4.9 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 610 | 13 | 3 | 7 | 6.2 | CC(C)(C)Oc1ccc(C[C@H](NC(=O)CCCCNc2cc(-c3cccnc3)nn2-c2ccc(C(C)(C)C)cc2)C(N)=O)cc1 | 10.1016/j.bmcl.2006.12.062 | |
44440752 | 169027 | 0 | None | - | 1 | Human | 6.8 | pEC50 | = | 6.8 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 568 | 13 | 4 | 7 | 5.1 | CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@@H](Cc2cccc(O)c2)C(N)=O)cc1 | 10.1016/j.bmcl.2006.12.062 | |
CHEMBL439392 | 169027 | 0 | None | - | 1 | Human | 6.8 | pEC50 | = | 6.8 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 568 | 13 | 4 | 7 | 5.1 | CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@@H](Cc2cccc(O)c2)C(N)=O)cc1 | 10.1016/j.bmcl.2006.12.062 | |
11502667 | 78416 | 0 | None | - | 1 | Human | 5.8 | pEC50 | = | 5.8 | Functional | Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation |
ChEMBL | 420 | 4 | 2 | 7 | 4.3 | COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1F | 10.1021/jm060247s | |
CHEMBL211129 | 78416 | 0 | None | - | 1 | Human | 5.8 | pEC50 | = | 5.8 | Functional | Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation |
ChEMBL | 420 | 4 | 2 | 7 | 4.3 | COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1F | 10.1021/jm060247s | |
44572264 | 179438 | 19 | None | - | 1 | Human | 5.8 | pEC50 | = | 5.8 | Functional | Agonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase productionAgonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase production |
ChEMBL | 357 | 4 | 1 | 2 | 6.1 | O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 | 10.1021/jm801561h | |
CHEMBL474041 | 179438 | 19 | None | - | 1 | Human | 5.8 | pEC50 | = | 5.8 | Functional | Agonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase productionAgonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase production |
ChEMBL | 357 | 4 | 1 | 2 | 6.1 | O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 | 10.1021/jm801561h | |
44440751 | 93828 | 0 | None | - | 1 | Human | 6.8 | pEC50 | = | 6.8 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 554 | 12 | 4 | 7 | 5.3 | CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@H](C(N)=O)c2ccc(O)cc2)cc1 | 10.1016/j.bmcl.2006.12.062 | |
CHEMBL247700 | 93828 | 0 | None | - | 1 | Human | 6.8 | pEC50 | = | 6.8 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 554 | 12 | 4 | 7 | 5.3 | CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@H](C(N)=O)c2ccc(O)cc2)cc1 | 10.1016/j.bmcl.2006.12.062 | |
44440753 | 148521 | 0 | None | - | 1 | Human | 6.7 | pEC50 | = | 6.7 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 537 | 12 | 2 | 5 | 5.5 | CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@H](CC(N)=O)Cc2ccccc2)cc1 | 10.1016/j.bmcl.2006.12.062 | |
CHEMBL393847 | 148521 | 0 | None | - | 1 | Human | 6.7 | pEC50 | = | 6.7 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 537 | 12 | 2 | 5 | 5.5 | CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@H](CC(N)=O)Cc2ccccc2)cc1 | 10.1016/j.bmcl.2006.12.062 | |
11531195 | 138798 | 0 | None | - | 1 | Human | 5.7 | pEC50 | = | 5.7 | Functional | Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation |
ChEMBL | 388 | 3 | 3 | 7 | 3.9 | CSc1nc(-c2cccc(O)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/jm060247s | |
CHEMBL378091 | 138798 | 0 | None | - | 1 | Human | 5.7 | pEC50 | = | 5.7 | Functional | Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation |
ChEMBL | 388 | 3 | 3 | 7 | 3.9 | CSc1nc(-c2cccc(O)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/jm060247s | |
9915237 | 93523 | 1 | None | - | 1 | Human | 7.7 | pEC50 | = | 7.7 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 539 | 11 | 3 | 6 | 4.9 | CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 | 10.1016/j.bmcl.2006.12.062 | |
CHEMBL246321 | 93523 | 1 | None | - | 1 | Human | 7.7 | pEC50 | = | 7.7 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 539 | 11 | 3 | 6 | 4.9 | CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 | 10.1016/j.bmcl.2006.12.062 | |
44440784 | 93378 | 0 | None | - | 1 | Human | 5.6 | pEC50 | = | 5.6 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 539 | 11 | 3 | 6 | 4.9 | CC(C)(C)c1ccc(-n2nc(CCCCC(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)cc2-c2ccncc2)cc1 | 10.1016/j.bmcl.2006.12.062 | |
CHEMBL245663 | 93378 | 0 | None | - | 1 | Human | 5.6 | pEC50 | = | 5.6 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 539 | 11 | 3 | 6 | 4.9 | CC(C)(C)c1ccc(-n2nc(CCCCC(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)cc2-c2ccncc2)cc1 | 10.1016/j.bmcl.2006.12.062 | |
53320759 | 57385 | 0 | None | - | 1 | Human | 7.6 | pEC50 | = | 7.6 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1136 | 18 | 5 | 17 | 10.1 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
CHEMBL1651829 | 57385 | 0 | None | - | 1 | Human | 7.6 | pEC50 | = | 7.6 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1136 | 18 | 5 | 17 | 10.1 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
44440746 | 152727 | 0 | None | - | 1 | Human | 6.6 | pEC50 | = | 6.6 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 539 | 11 | 3 | 6 | 4.9 | CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 | 10.1016/j.bmcl.2006.12.062 | |
CHEMBL397316 | 152727 | 0 | None | - | 1 | Human | 6.6 | pEC50 | = | 6.6 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 539 | 11 | 3 | 6 | 4.9 | CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 | 10.1016/j.bmcl.2006.12.062 | |
53323417 | 57379 | 0 | None | - | 1 | Human | 7.6 | pEC50 | = | 7.6 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1180 | 21 | 5 | 18 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
CHEMBL1651823 | 57379 | 0 | None | - | 1 | Human | 7.6 | pEC50 | = | 7.6 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1180 | 21 | 5 | 18 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
9887381 | 79531 | 24 | None | 27 | 2 | Human | 6.5 | pEC50 | = | 6.5 | Functional | Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation |
ChEMBL | 402 | 4 | 2 | 7 | 4.2 | COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 | 10.1021/jm060247s | |
CHEMBL211405 | 79531 | 24 | None | 27 | 2 | Human | 6.5 | pEC50 | = | 6.5 | Functional | Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation |
ChEMBL | 402 | 4 | 2 | 7 | 4.2 | COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 | 10.1021/jm060247s | |
53324744 | 57388 | 0 | None | - | 1 | Human | 7.4 | pEC50 | = | 7.4 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1313 | 30 | 5 | 21 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
CHEMBL1651831 | 57388 | 0 | None | - | 1 | Human | 7.4 | pEC50 | = | 7.4 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1313 | 30 | 5 | 21 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
53320758 | 57380 | 0 | None | 21 | 2 | Human | 7.4 | pEC50 | = | 7.4 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1225 | 24 | 5 | 19 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
CHEMBL1651824 | 57380 | 0 | None | 21 | 2 | Human | 7.4 | pEC50 | = | 7.4 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1225 | 24 | 5 | 19 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
44255904 | 57384 | 0 | None | 79 | 2 | Human | 8.3 | pEC50 | = | 8.3 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 682 | 17 | 4 | 14 | 3.9 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCN=[N+]=[N-])nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
CHEMBL1651828 | 57384 | 0 | None | 79 | 2 | Human | 8.3 | pEC50 | = | 8.3 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 682 | 17 | 4 | 14 | 3.9 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCN=[N+]=[N-])nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
44440748 | 93868 | 0 | None | - | 1 | Human | 6.3 | pEC50 | = | 6.3 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 609 | 8 | 3 | 6 | 6.6 | CC(C)(C)c1ccc(-n2nc(-c3cc4ccccc4cn3)cc2-c2cccc(C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)c2)cc1 | 10.1016/j.bmcl.2006.12.062 | |
CHEMBL247945 | 93868 | 0 | None | - | 1 | Human | 6.3 | pEC50 | = | 6.3 | Functional | Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA |
ChEMBL | 609 | 8 | 3 | 6 | 6.6 | CC(C)(C)c1ccc(-n2nc(-c3cc4ccccc4cn3)cc2-c2cccc(C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)c2)cc1 | 10.1016/j.bmcl.2006.12.062 | |
53324743 | 57382 | 0 | None | 18 | 2 | Human | 7.3 | pEC50 | = | 7.3 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1313 | 30 | 5 | 21 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
CHEMBL1651826 | 57382 | 0 | None | 18 | 2 | Human | 7.3 | pEC50 | = | 7.3 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1313 | 30 | 5 | 21 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
53318121 | 57378 | 0 | None | - | 1 | Human | 7.2 | pEC50 | = | 7.2 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1269 | 27 | 5 | 20 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
CHEMBL1651822 | 57378 | 0 | None | - | 1 | Human | 7.2 | pEC50 | = | 7.2 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1269 | 27 | 5 | 20 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
53324742 | 57381 | 0 | None | 26 | 2 | Human | 7.2 | pEC50 | = | 7.2 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1269 | 27 | 5 | 20 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
CHEMBL1651825 | 57381 | 0 | None | 26 | 2 | Human | 7.2 | pEC50 | = | 7.2 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1269 | 27 | 5 | 20 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
53324741 | 57377 | 0 | None | - | 1 | Human | 7.1 | pEC50 | = | 7.1 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1225 | 24 | 5 | 19 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v | |
CHEMBL1651821 | 57377 | 0 | None | - | 1 | Human | 7.1 | pEC50 | = | 7.1 | Functional | Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay |
ChEMBL | 1225 | 24 | 5 | 19 | 10.2 | CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 | 10.1021/ml100229v |
Showing 1 to 50 of 179 entries
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Assay information | Chemical information | |||||||||||||||||||
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Sel. page | Similar- ity
| Common name
| GPCRdb ID | #Vendors
| Reference ligand | Fold selectivity | # Tested GPCRs
| Species | p-value (-log)
| Activity Type
| Activity Relation
| Activity Value
| Assay Type
| Assay Description
| Source | Mol weight | Rot Bonds | H don | H acc | LogP
| Smiles
| DOI |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Assay information
| Chemical information
| |||||||||||||||||||
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Sel. page | Similar- ity
| Common name
| GPCRdb ID | #Vendors
| Reference ligand | Fold selectivity | # Tested GPCRs
| Species | p-value (-log)
| Activity Type
| Activity Relation
| Activity Value
| Assay Type
| Assay Description
| Source | Mol weight | Rot Bonds | H don | H acc | LogP
| Smiles
| DOI |
9887381 | 79531 | 24 | None | - | 0 | Human | 6.7 | pEC50 | = | 6.7 | Binding | Agonist activity at LHCGR (unknown origin)Agonist activity at LHCGR (unknown origin) |
ChEMBL | 402 | 4 | 2 | 7 | 4.2 | COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 | 10.1039/c1md00145k | ||
CHEMBL211405 | 79531 | 24 | None | - | 0 | Human | 6.7 | pEC50 | = | 6.7 | Binding | Agonist activity at LHCGR (unknown origin)Agonist activity at LHCGR (unknown origin) |
ChEMBL | 402 | 4 | 2 | 7 | 4.2 | COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 | 10.1039/c1md00145k | ||
139600337 | 173793 | 12 | None | - | 0 | Human | 5.9 | pIC50 | = | 5.9 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
CHEMBL4537998 | 173793 | 12 | None | - | 0 | Human | 5.9 | pIC50 | = | 5.9 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
139600337 | 173793 | 12 | None | - | 0 | Human | 5.8 | pIC50 | = | 5.8 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
CHEMBL4537998 | 173793 | 12 | None | - | 0 | Human | 5.8 | pIC50 | = | 5.8 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
139600337 | 173793 | 12 | None | - | 0 | Human | 5.8 | pIC50 | = | 5.8 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
CHEMBL4537998 | 173793 | 12 | None | - | 0 | Human | 5.8 | pIC50 | = | 5.8 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
139600337 | 173793 | 12 | None | - | 0 | Human | 5.8 | pIC50 | = | 5.8 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
CHEMBL4537998 | 173793 | 12 | None | - | 0 | Human | 5.8 | pIC50 | = | 5.8 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
139600336 | 171137 | 14 | None | - | 1 | Human | 6.7 | pIC50 | = | 6.7 | Binding | Affinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGRAffinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGR |
ChEMBL | 459 | 4 | 1 | 5 | 5.1 | O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 | 10.6019/CHEMBL5210121 | ||
CHEMBL4458424 | 171137 | 14 | None | - | 1 | Human | 6.7 | pIC50 | = | 6.7 | Binding | Affinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGRAffinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGR |
ChEMBL | 459 | 4 | 1 | 5 | 5.1 | O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 | 10.6019/CHEMBL5210121 | ||
139600337 | 173793 | 12 | None | - | 0 | Human | 6.7 | pIC50 | = | 6.7 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
CHEMBL4537998 | 173793 | 12 | None | - | 0 | Human | 6.7 | pIC50 | = | 6.7 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
139600337 | 173793 | 12 | None | - | 0 | Human | 5.7 | pIC50 | = | 5.7 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
CHEMBL4537998 | 173793 | 12 | None | - | 0 | Human | 5.7 | pIC50 | = | 5.7 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
139600337 | 173793 | 12 | None | - | 0 | Human | 5.7 | pIC50 | = | 5.7 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
CHEMBL4537998 | 173793 | 12 | None | - | 0 | Human | 5.7 | pIC50 | = | 5.7 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
44572264 | 179438 | 19 | None | - | 0 | Human | 5.6 | pIC50 | = | 5.6 | Binding | Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cellsDisplacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells |
ChEMBL | 357 | 4 | 1 | 2 | 6.1 | O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 | 10.1021/jm801561h | ||
CHEMBL474041 | 179438 | 19 | None | - | 0 | Human | 5.6 | pIC50 | = | 5.6 | Binding | Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cellsDisplacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells |
ChEMBL | 357 | 4 | 1 | 2 | 6.1 | O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 | 10.1021/jm801561h | ||
139600337 | 173793 | 12 | None | - | 0 | Human | 5.6 | pIC50 | = | 5.6 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
CHEMBL4537998 | 173793 | 12 | None | - | 0 | Human | 5.6 | pIC50 | = | 5.6 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
139600337 | 173793 | 12 | None | - | 0 | Human | 6.2 | pIC50 | = | 6.2 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
CHEMBL4537998 | 173793 | 12 | None | - | 0 | Human | 6.2 | pIC50 | = | 6.2 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
139600337 | 173793 | 12 | None | - | 0 | Human | 7.0 | pIC50 | = | 7.0 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
CHEMBL4537998 | 173793 | 12 | None | - | 0 | Human | 7.0 | pIC50 | = | 7.0 | Binding | Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control |
ChEMBL | 473 | 4 | 1 | 3 | 6.8 | O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 | 10.1021/acs.jmedchem.9b01382 | ||
44267887 | 98481 | 0 | None | 41 | 2 | Rat | 9.9 | pKd | = | 9.9 | Binding | In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells |
ChEMBL | 967 | 10 | 1 | 14 | 7.8 | CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C | 10.1021/jm030418i | ||
CHEMBL275935 | 98481 | 0 | None | 41 | 2 | Rat | 9.9 | pKd | = | 9.9 | Binding | In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells |
ChEMBL | 967 | 10 | 1 | 14 | 7.8 | CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C | 10.1021/jm030418i | ||
44267907 | 16331 | 0 | None | -1 | 2 | Rat | 9.3 | pKd | = | 9.3 | Binding | In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells |
ChEMBL | 937 | 11 | 1 | 14 | 6.8 | CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C | 10.1021/jm030418i | ||
CHEMBL12282 | 16331 | 0 | None | -1 | 2 | Rat | 9.3 | pKd | = | 9.3 | Binding | In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells |
ChEMBL | 937 | 11 | 1 | 14 | 6.8 | CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C | 10.1021/jm030418i | ||
9854500 | 102272 | 0 | None | 1 | 2 | Rat | 8.8 | pKd | = | 8.8 | Binding | In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells |
ChEMBL | 953 | 11 | 1 | 14 | 7.3 | CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C | 10.1021/jm030418i | ||
CHEMBL303274 | 102272 | 0 | None | 1 | 2 | Rat | 8.8 | pKd | = | 8.8 | Binding | In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells |
ChEMBL | 953 | 11 | 1 | 14 | 7.3 | CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C | 10.1021/jm030418i | ||
44267812 | 98103 | 0 | None | 8 | 2 | Rat | 8.8 | pKd | = | 8.8 | Binding | In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells |
ChEMBL | 941 | 10 | 1 | 14 | 7.3 | CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C | 10.1021/jm030418i | ||
CHEMBL273440 | 98103 | 0 | None | 8 | 2 | Rat | 8.8 | pKd | = | 8.8 | Binding | In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells |
ChEMBL | 941 | 10 | 1 | 14 | 7.3 | CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C | 10.1021/jm030418i | ||
CHEMBL412984 | 213038 | 0 | None | - | 1 | Rat | 10.7 | pKi | = | 10.7 | Binding | In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant |
ChEMBL | None | None | None | CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C)C(N)=O | 10.1021/jm00130a019 | ||||
44350635 | 157213 | 0 | None | - | 1 | Rat | 10.6 | pKi | = | 10.6 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | 1292 | 32 | 15 | 13 | 0.5 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
CHEMBL407606 | 157213 | 0 | None | - | 1 | Rat | 10.6 | pKi | = | 10.6 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | 1292 | 32 | 15 | 13 | 0.5 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
CHEMBL407123 | 212641 | 0 | None | - | 1 | Rat | 10.4 | pKi | = | 10.4 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)O | 10.1021/jm00099a017 | ||||
44350493 | 155753 | 0 | None | - | 1 | Rat | 10.1 | pKi | = | 10.1 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | 1296 | 32 | 15 | 14 | -0.4 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
CHEMBL405737 | 155753 | 0 | None | - | 1 | Rat | 10.1 | pKi | = | 10.1 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | 1296 | 32 | 15 | 14 | -0.4 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
44350501 | 141596 | 0 | None | - | 1 | Rat | 10.0 | pKi | = | 10.0 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | 1220 | 32 | 14 | 14 | -0.8 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
CHEMBL385042 | 141596 | 0 | None | - | 1 | Rat | 10.0 | pKi | = | 10.0 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | 1220 | 32 | 14 | 14 | -0.8 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
44350636 | 161947 | 0 | None | - | 1 | Rat | 9.8 | pKi | = | 9.8 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | 1200 | 33 | 14 | 15 | -1.9 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(OC)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
CHEMBL415571 | 161947 | 0 | None | - | 1 | Rat | 9.8 | pKi | = | 9.8 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | 1200 | 33 | 14 | 15 | -1.9 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(OC)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
44350565 | 141673 | 0 | None | - | 1 | Rat | 9.7 | pKi | = | 9.7 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay |
ChEMBL | 1209 | 32 | 15 | 14 | -1.4 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
CHEMBL385468 | 141673 | 0 | None | - | 1 | Rat | 9.7 | pKi | = | 9.7 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay |
ChEMBL | 1209 | 32 | 15 | 14 | -1.4 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
44350487 | 167239 | 0 | None | - | 1 | Rat | 9.7 | pKi | = | 9.7 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | 1306 | 32 | 14 | 13 | 0.9 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)N(C)C(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
CHEMBL429240 | 167239 | 0 | None | - | 1 | Rat | 9.7 | pKi | = | 9.7 | Binding | Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay |
ChEMBL | 1306 | 32 | 14 | 13 | 0.9 | CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)N(C)C(=O)[C@@H]1CCC(=O)N1 | 10.1021/jm00099a017 | ||
44314940 | 82115 | 0 | None | - | 1 | Rat | 9.6 | pKi | = | 9.6 | Binding | In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant |
ChEMBL | 1041 | 26 | 10 | 10 | 2.8 | CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 | 10.1021/jm00130a019 | ||
CHEMBL216617 | 82115 | 0 | None | - | 1 | Rat | 9.6 | pKi | = | 9.6 | Binding | In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant |
ChEMBL | 1041 | 26 | 10 | 10 | 2.8 | CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 | 10.1021/jm00130a019 |
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