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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 | |
[Ac-His1]PACAP-27 | 257 | None | 0 | Human | Binding | IC50 | = | 13.00 | 7.89 | - | 4 | Displacement of [125I]PACAP27 from human VPAC2 receptor expressed in CHO cells | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/jm0609059 | |
[Ala11,22,28]VIP | 328 | None | 0 | Human | Binding | pKi | = | - | 5.60 | -316 | 3 | inhibition of [125I]-VIP binding to membranes from CHO cells stably expressing the recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10801840 | |
[Arg16]chicken secretin | 468 | None | 0 | Human | Binding | pIC50 | = | - | 5.30 | - | 7 | Inhibition of [125I]VIP binding in membranes from CHO cells expressing recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9437714 | |
[Arg16]chicken secretin | 468 | None | 0 | Rat | Binding | pIC50 | = | - | 5.00 | - | 7 | Inhibition of [125I]VIP binding in membranes from CHO cells expressing recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9437714 | |
[Lys15,Arg16,Leu27]VIP-(1-7)/GRF-(8-27)-NH2 | 2436 | None | 0 | Human | Binding | pIC50 | > | - | 6.00 | - | 5 | inhibition of [125I]-VIP binding to membranes from CHO cells stably expressing the recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11931347 | |
[Lys15,Arg16,Leu27]VIP-(1-7)/GRF-(8-27)-NH2 | 2436 | None | 0 | Human | Binding | pIC50 | > | - | 4.50 | - | 5 | Inhibition of [125I]VIP binding in membranes from CHO cells expressing recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9437714 | |
[Lys15,Arg16,Leu27]VIP-(1-7)/GRF-(8-27)-NH2 | 2436 | None | 0 | Rat | Binding | pIC50 | = | - | 4.50 | - | 5 | Inhibition of [125I]VIP binding in membranes from CHO cells expressing recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9437714 | |
BAY 55-9837 | 583 | None | 0 | Human | Binding | pIC50 | = | - | 7.20 | - | 3 | inhibition of [125I]-PACAP-27 binding to membranes from CHO cells stably expressing the recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11978642 | |
BAY 55-9837 | 583 | None | 0 | Human | Binding | pKd | = | - | 9.20 | - | 3 | binding to membranes from CHO cells stably expressing the recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11978642 | |
CHEMBL3736134 | 136572 | None | 0 | Human | Binding | IC50 | = | 36.31 | 7.44 | - | 3 | Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis | ChEMBL | 3263.7 | 105 | 48 | 45 | -10.62 | CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(C#Cc2ccc(F)cc2)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)C(C)C)[C@@H](C)O | https://dx.doi.org/10.1016/j.ejmech.2015.09.017 | |
CHEMBL3736134 | 136572 | None | 0 | Human | Binding | IC50 | = | 36.00 | 7.44 | - | 3 | Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis | ChEMBL | 3263.7 | 105 | 48 | 45 | -10.62 | CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(C#Cc2ccc(F)cc2)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)C(C)C)[C@@H](C)O | https://dx.doi.org/10.1016/j.ejmech.2015.09.017 | |
CHEMBL3736230 | 136590 | None | 0 | Human | Binding | IC50 | = | 53.70 | 7.27 | - | 3 | Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis | ChEMBL | 3245.7 | 105 | 48 | 45 | -10.76 | CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(C#Cc2ccccc2)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)C(C)C)[C@@H](C)O | https://dx.doi.org/10.1016/j.ejmech.2015.09.017 | |
CHEMBL3736230 | 136590 | None | 0 | Human | Binding | IC50 | = | 53.00 | 7.28 | - | 3 | Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis | ChEMBL | 3245.7 | 105 | 48 | 45 | -10.76 | CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(C#Cc2ccccc2)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)C(C)C)[C@@H](C)O | https://dx.doi.org/10.1016/j.ejmech.2015.09.017 | |
CHEMBL3889643 | 142476 | None | 0 | Human | Binding | IC50 | = | 5000.00 | 5.30 | - | 1 | Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay | ChEMBL | 550.2 | 12 | 3 | 6 | 3.21 | CO[C@@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H](Cc1ccccc1)C[C@H](O)CNS(=O)(=O)c1ccc(C(C)=O)cc1 | - | |
CHEMBL3890096 | 142529 | None | 0 | Human | Binding | IC50 | = | 6000.00 | 5.22 | - | 1 | Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay | ChEMBL | 566.2 | 11 | 3 | 7 | 2.77 | CO[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H](Cc1ccccc1)C[C@H](O)CNS(=O)(=O)c1ccc2c(c1)OCCO2 | - | |
CHEMBL3905363 | 144404 | None | 0 | Human | Binding | IC50 | = | 10000.00 | 5.00 | - | 1 | Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay | ChEMBL | 534.2 | 10 | 4 | 5 | 2.84 | O=C(N[C@H]1c2ccccc2C[C@H]1O)[C@H](Cc1ccccc1)C[C@H](O)CNS(=O)(=O)c1ccc2c(c1)CCC2 | - | |
CHEMBL3908152 | 144736 | None | 0 | Human | Binding | IC50 | = | 40600.00 | 4.39 | - | 1 | Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay | ChEMBL | 538.2 | 11 | 5 | 6 | 2.40 | CC(O)c1ccc(S(=O)(=O)NC[C@@H](O)C[C@@H](Cc2ccccc2)C(=O)N[C@H]2c3ccccc3C[C@H]2O)cc1 | - | |
CHEMBL3927475 | 147204 | None | 0 | Human | Binding | IC50 | = | 206.00 | 6.69 | - | 1 | Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay | ChEMBL | 552.2 | 10 | 4 | 7 | 2.12 | O=C(N[C@H]1c2ccccc2C[C@H]1O)[C@H](Cc1ccccc1)C[C@H](O)CNS(=O)(=O)c1ccc2c(c1)OCCO2 | - | |
CHEMBL3927669 | 147225 | None | 0 | Human | Binding | IC50 | = | 4000.00 | 5.40 | - | 1 | Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay | ChEMBL | 542.2 | 11 | 3 | 5 | 3.66 | CO[C@@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H](Cc1ccccc1)C[C@H](O)CNS(=O)(=O)c1ccc(Cl)cc1 | - | |
CHEMBL3938565 | 148618 | None | 0 | Human | Binding | IC50 | = | 1130.00 | 5.95 | - | 1 | Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay | ChEMBL | 522.2 | 11 | 4 | 5 | 2.91 | CCc1ccc(S(=O)(=O)NC[C@@H](O)C[C@@H](Cc2ccccc2)C(=O)N[C@H]2c3ccccc3C[C@H]2O)cc1 | - |
Showing 1 to 20 of 80 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 | |
[Ac-His1]PACAP-27 | 257 | None | 0 | Human | Functional | EC50 | = | 0.09 | 10.06 | -1 | 4 | Activity at human VPAC2 receptor in CHO cells by measuring cAMP accumulation | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/jm0609059 | |
[Ala11,22,28]VIP | 328 | None | 0 | Human | Functional | pEC50 | > | - | 5.00 | -4168 | 3 | cyclic AMP formation in CHO cells stably expressing recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/16930633 | |
[Ala11,22,28]VIP | 328 | None | 0 | Human | Functional | pEC50 | = | - | 5.90 | -4168 | 3 | stimulation of cyclic AMP formation in CHO cells stably expressing the recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10801840 | |
[Ala11,22,28]VIP | 328 | None | 0 | Human | Functional | pEC50 | > | - | 5.00 | -4168 | 3 | calcium influx in CHO cells stably expressing recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/16930633 | |
[Lys15,Arg16,Leu27]VIP-(1-7)/GRF-(8-27)-NH2 | 2436 | None | 0 | Human | Functional | pEC50 | > | - | 6.00 | -1584 | 5 | stimulation of cyclic AMP formation in CHO cells stably expressing the recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11931347 | |
BAY 55-9837 | 583 | None | 0 | Human | Functional | pEC50 | = | - | 9.40 | 177 | 3 | cyclic AMP formation in CHO cells stably expressing recombinant receptor | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11978642 | |
CHEMBL1893324 | 211519 | None | 20 | Human | Functional | EC50 | = | 0.08 | 10.10 | -1 | 3 | Agonist activity at VPAC2 in human SH-SY5Y cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay | ChEMBL | - | - | - | - | - | CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)C(C)C)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(N)=O | https://dx.doi.org/10.1021/acs.jmedchem.0c01396 | |
CHEMBL2159347 | 81431 | None | 0 | Human | Functional | IC50 | = | 2600.00 | 5.58 | -281 | 4 | Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter | ChEMBL | 587.1 | 9 | 2 | 5 | 7.50 | COc1ccc2cc(-c3cc(-c4cc(Cl)ccc4Cl)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 | https://dx.doi.org/10.1021/jm300579z | |
CHEMBL2159348 | 81432 | None | 0 | Human | Functional | IC50 | = | 1700.00 | 5.77 | -186 | 3 | Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter | ChEMBL | 587.1 | 9 | 2 | 5 | 7.50 | COc1ccc2cc(-c3cc(-c4ccc(Cl)c(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 | https://dx.doi.org/10.1021/jm300579z | |
CHEMBL2159349 | 81433 | None | 0 | Human | Functional | IC50 | = | 2600.00 | 5.58 | -794 | 4 | Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter | ChEMBL | 621.2 | 9 | 2 | 5 | 7.87 | COc1ccc2cc(-c3cc(-c4cc(Cl)cc(C(F)(F)F)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 | https://dx.doi.org/10.1021/jm300579z | |
CHEMBL3102919 | 213486 | None | 0 | Human | Functional | EC50 | = | 0.14 | 9.85 | - | 1 | Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/ml400257h | |
CHEMBL3102920 | 213487 | None | 0 | Human | Functional | EC50 | = | 6.60 | 8.18 | - | 1 | Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/ml400257h | |
CHEMBL3102921 | 213488 | None | 0 | Human | Functional | EC50 | = | 0.38 | 9.42 | - | 1 | Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/ml400257h | |
CHEMBL3102922 | 213489 | None | 0 | Human | Functional | EC50 | = | 0.21 | 9.68 | - | 1 | Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/ml400257h | |
CHEMBL3102923 | 213490 | None | 0 | Human | Functional | EC50 | = | 1.16 | 8.94 | - | 1 | Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ChEMBL | - | - | - | - | - | CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)C(C)C)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N1)C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)O | https://dx.doi.org/10.1021/ml400257h | |
CHEMBL3102924 | 213491 | None | 0 | Human | Functional | EC50 | = | 0.10 | 10.00 | - | 1 | Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ChEMBL | - | - | - | - | - | CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)C(C)C)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)O | https://dx.doi.org/10.1021/ml400257h | |
CHEMBL3102925 | 213492 | None | 0 | Human | Functional | EC50 | = | 0.11 | 9.96 | - | 1 | Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ChEMBL | - | - | - | - | - | CC[C@H](C)[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(C)C)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)O)[C@@H](C)CC)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O)C(C)C | https://dx.doi.org/10.1021/ml400257h | |
CHEMBL3102926 | 213493 | None | 0 | Human | Functional | EC50 | = | 1.37 | 8.86 | - | 1 | Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ChEMBL | - | - | - | - | - | C=CCCC[C@](C)(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@](C)(CCCC=C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(C)C)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)O)[C@@H](C)CC)C(C)C | https://dx.doi.org/10.1021/ml400257h | |
CHEMBL3102927 | 213494 | None | 0 | Human | Functional | EC50 | = | 1.49 | 8.83 | - | 1 | Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ChEMBL | - | - | - | - | - | C=CCCC[C@](C)(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(C)C)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@](C)(CCCC=C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)O)[C@@H](C)CC)C(C)C | https://dx.doi.org/10.1021/ml400257h | |
CHEMBL3102928 | 213495 | None | 0 | Human | Functional | EC50 | = | 3.80 | 8.42 | - | 1 | Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ChEMBL | - | - | - | - | - | C=CCCC[C@](C)(NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(C)C)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@](C)(CCCC=C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)O)[C@@H](C)CC | https://dx.doi.org/10.1021/ml400257h |
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