Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
136036237 195418 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 632 7 3 6 5.9 CCC(C)[C@H]1C(=O)Nc2ccc(N3CCC(NC(C)=O)C3)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 10.1016/j.bmcl.2009.01.085
CHEMBL503202 195418 0 None -3 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 632 7 3 6 5.9 CCC(C)[C@H]1C(=O)Nc2ccc(N3CCC(NC(C)=O)C3)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 10.1016/j.bmcl.2009.01.085
136036259 195442 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 550 6 2 6 5.6 CC(C)[C@H]1C(=O)Nc2ccc(NCc3ccccc3)cc2-c2nc3cc(C(=O)N(C)C4CCN(C)CC4)ccc3n21 10.1016/j.bmcl.2009.01.085
CHEMBL503688 195442 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 550 6 2 6 5.6 CC(C)[C@H]1C(=O)Nc2ccc(NCc3ccccc3)cc2-c2nc3cc(C(=O)N(C)C4CCN(C)CC4)ccc3n21 10.1016/j.bmcl.2009.01.085
136036261 195531 0 None -10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 632 9 3 6 7.1 CCC(C)[C@H]1C(=O)Nc2ccc(NCCN3CCCCC3)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 10.1016/j.bmcl.2009.01.085
CHEMBL505263 195531 0 None -10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 632 9 3 6 7.1 CCC(C)[C@H]1C(=O)Nc2ccc(NCCN3CCCCC3)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 10.1016/j.bmcl.2009.01.085
135407952 7846 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 542 4 2 6 5.8 CN1CCCN(CC1)C(=O)c1ccc2c(c1)nc1n2[C@@H](C(C)C)C(=O)Nc2c1cc(cc2)NC1CCCCCC1 10.1016/j.bmcl.2009.01.085
5530 7846 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 542 4 2 6 5.8 CN1CCCN(CC1)C(=O)c1ccc2c(c1)nc1n2[C@@H](C(C)C)C(=O)Nc2c1cc(cc2)NC1CCCCCC1 10.1016/j.bmcl.2009.01.085
CHEMBL463274 7846 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 542 4 2 6 5.8 CN1CCCN(CC1)C(=O)c1ccc2c(c1)nc1n2[C@@H](C(C)C)C(=O)Nc2c1cc(cc2)NC1CCCCCC1 10.1016/j.bmcl.2009.01.085
135869412 195222 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 619 6 1 7 5.3 CC(C)[C@H]1C(=O)Nc2ccc(N3CCN(Cc4ccccc4)CC3)cc2-c2nc3cc(C(=O)N(C)C4CCN(C)CC4)ccc3n21 10.1016/j.bmcl.2009.01.085
CHEMBL502480 195222 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 619 6 1 7 5.3 CC(C)[C@H]1C(=O)Nc2ccc(N3CCN(Cc4ccccc4)CC3)cc2-c2nc3cc(C(=O)N(C)C4CCN(C)CC4)ccc3n21 10.1016/j.bmcl.2009.01.085
CHEMBL2448526 217279 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@@H]2CCCN2)CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1016/j.bmcl.2009.01.085
135407930 195199 0 None -10 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 606 10 3 6 6.6 CCC(C)[C@H]1C(=O)Nc2ccc(NCCCN(C)C)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 10.1016/j.bmcl.2009.01.085
CHEMBL502132 195199 0 None -10 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human MrgX2 receptorAgonist activity at human MrgX2 receptor
ChEMBL 606 10 3 6 6.6 CCC(C)[C@H]1C(=O)Nc2ccc(NCCCN(C)C)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 10.1016/j.bmcl.2009.01.085
164734529 197618 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MRGPRX2 expressed in HEK293 cells co-expressing mouse Galpha15 assessed as inhibition of Cortistatin-14 induced Ca2+ mobilization preincubated for 30 mins followed by Cortistatin-14 addition by FLIPRtetra-calcium mobilization assayAntagonist activity at human MRGPRX2 expressed in HEK293 cells co-expressing mouse Galpha15 assessed as inhibition of Cortistatin-14 induced Ca2+ mobilization preincubated for 30 mins followed by Cortistatin-14 addition by FLIPRtetra-calcium mobilization assay
ChEMBL 491 6 1 6 3.6 C[C@@H](C(=O)Nc1cnc(Oc2ccc(F)cc2F)cn1)N1CCC(F)(F)[C@@H](c2cc[n+]([O-])cc2)C1 10.1021/acsmedchemlett.2c00262
CHEMBL5184300 197618 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human MRGPRX2 expressed in HEK293 cells co-expressing mouse Galpha15 assessed as inhibition of Cortistatin-14 induced Ca2+ mobilization preincubated for 30 mins followed by Cortistatin-14 addition by FLIPRtetra-calcium mobilization assayAntagonist activity at human MRGPRX2 expressed in HEK293 cells co-expressing mouse Galpha15 assessed as inhibition of Cortistatin-14 induced Ca2+ mobilization preincubated for 30 mins followed by Cortistatin-14 addition by FLIPRtetra-calcium mobilization assay
ChEMBL 491 6 1 6 3.6 C[C@@H](C(=O)Nc1cnc(Oc2ccc(F)cc2F)cn1)N1CCC(F)(F)[C@@H](c2cc[n+]([O-])cc2)C1 10.1021/acsmedchemlett.2c00262
9567 10522 9 None -1819 3 Human 5.7 pEC50 = 5.7 Functional
Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).
Guide to Pharmacology 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 11765135
9567 10522 9 None -1819 3 Human 5.7 pEC50 = 5.7 Functional
Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).
Guide to Pharmacology 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 23396314
9567 10522 9 None -1819 3 Human 5.7 pEC50 = 5.7 Functional
Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).
Guide to Pharmacology 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 28288109
9950038 10522 9 None -1819 3 Human 5.7 pEC50 = 5.7 Functional
Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).
Guide to Pharmacology 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 11765135
9950038 10522 9 None -1819 3 Human 5.7 pEC50 = 5.7 Functional
Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).
Guide to Pharmacology 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 23396314
9950038 10522 9 None -1819 3 Human 5.7 pEC50 = 5.7 Functional
Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).
Guide to Pharmacology 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 28288109
CHEMBL327745 10522 9 None -1819 3 Human 5.7 pEC50 = 5.7 Functional
Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).
Guide to Pharmacology 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 11765135
CHEMBL327745 10522 9 None -1819 3 Human 5.7 pEC50 = 5.7 Functional
Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).
Guide to Pharmacology 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 23396314
CHEMBL327745 10522 9 None -1819 3 Human 5.7 pEC50 = 5.7 Functional
Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).Assayed using racemic TAN-67, the more active stereoisomer is the (4aS,12aR).
Guide to Pharmacology 344 1 1 3 3.9 CN1CC[C@]2([C@H](C1)Cc1c(C2)nc2c(c1)cccc2)c1cccc(c1)O 28288109
10567 8618 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Determined in a FLIPR calcium imaging assay using HEK cells heterologously expressing hMRGPRX2Determined in a FLIPR calcium imaging assay using HEK cells heterologously expressing hMRGPRX2
Guide to Pharmacology None None None None 35704588
145996510 8618 0 None -1 3 Human 5.7 pEC50 = 5.7 Functional
Determined in a FLIPR calcium imaging assay using HEK cells heterologously expressing hMRGPRX2Determined in a FLIPR calcium imaging assay using HEK cells heterologously expressing hMRGPRX2
Guide to Pharmacology None None None None 35704588
2098 10466 36 None -2089 11 Human 6.0 pEC50 = 6.0 Functional
In a calcium mobilisation asay.In a calcium mobilisation asay.
Guide to Pharmacology None None None None 25517090
2098 10466 36 None -2089 11 Human 6.0 pEC50 = 6.0 Functional
In a calcium mobilisation asay.In a calcium mobilisation asay.
Guide to Pharmacology None None None None 28288109
36511 10466 36 None -2089 11 Human 6.0 pEC50 = 6.0 Functional
In a calcium mobilisation asay.In a calcium mobilisation asay.
Guide to Pharmacology None None None None 25517090
36511 10466 36 None -2089 11 Human 6.0 pEC50 = 6.0 Functional
In a calcium mobilisation asay.In a calcium mobilisation asay.
Guide to Pharmacology None None None None 28288109
3805 10466 36 None -2089 11 Human 6.0 pEC50 = 6.0 Functional
In a calcium mobilisation asay.In a calcium mobilisation asay.
Guide to Pharmacology None None None None 25517090
3805 10466 36 None -2089 11 Human 6.0 pEC50 = 6.0 Functional
In a calcium mobilisation asay.In a calcium mobilisation asay.
Guide to Pharmacology None None None None 28288109
3835 10466 36 None -2089 11 Human 6.0 pEC50 = 6.0 Functional
In a calcium mobilisation asay.In a calcium mobilisation asay.
Guide to Pharmacology None None None None 25517090
3835 10466 36 None -2089 11 Human 6.0 pEC50 = 6.0 Functional
In a calcium mobilisation asay.In a calcium mobilisation asay.
Guide to Pharmacology None None None None 28288109
CHEMBL235363 10466 36 None -2089 11 Human 6.0 pEC50 = 6.0 Functional
In a calcium mobilisation asay.In a calcium mobilisation asay.
Guide to Pharmacology None None None None 25517090
CHEMBL235363 10466 36 None -2089 11 Human 6.0 pEC50 = 6.0 Functional
In a calcium mobilisation asay.In a calcium mobilisation asay.
Guide to Pharmacology None None None None 28288109
16133849 10448 12 None -66069 4 Human 5.4 pEC50 = 5.4 Functional
In a calcium mobilisation assay.In a calcium mobilisation assay.
Guide to Pharmacology None None None None 23396314
2020 10448 12 None -66069 4 Human 5.4 pEC50 = 5.4 Functional
In a calcium mobilisation assay.In a calcium mobilisation assay.
Guide to Pharmacology None None None None 23396314
91935900 10448 12 None -66069 4 Human 5.4 pEC50 = 5.4 Functional
In a calcium mobilisation assay.In a calcium mobilisation assay.
Guide to Pharmacology None None None None 23396314
CHEMBL501796 10448 12 None -66069 4 Human 5.4 pEC50 = 5.4 Functional
In a calcium mobilisation assay.In a calcium mobilisation assay.
Guide to Pharmacology None None None None 23396314
12988 8361 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 673 5 2 9 6.2 NC1=C(C#N)C2=C(C=CC(F)=C2S1)C3=C(F)C4=NC(OC[C@@]56CCCN5C[C@H](F)C6)=NC(N7CC8CCC(C7)N8)=C4C=C3C(F)(F)F 37321326
164904685 8361 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 673 5 2 9 6.2 NC1=C(C#N)C2=C(C=CC(F)=C2S1)C3=C(F)C4=NC(OC[C@@]56CCCN5C[C@H](F)C6)=NC(N7CC8CCC(C7)N8)=C4C=C3C(F)(F)F 37321326
2855 7889 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 519 16 3 6 4.2 CNCCc1cc(Cc2cc(CCNC)ccc2OC)c(c(c1)Cc1cc(CCNC)ccc1OC)OC 28288109
5531 7889 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 519 16 3 6 4.2 CNCCc1cc(Cc2cc(CCNC)ccc2OC)c(c(c1)Cc1cc(CCNC)ccc1OC)OC 28288109
9566 10199 14 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 28288109
95882507 10199 14 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 28288109
CHEMBL4520293 10199 14 None - 1 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 28288109
135407952 7846 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 542 4 2 6 5.8 CN1CCCN(CC1)C(=O)c1ccc2c(c1)nc1n2[C@@H](C(C)C)C(=O)Nc2c1cc(cc2)NC1CCCCCC1 19230660
5530 7846 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 542 4 2 6 5.8 CN1CCCN(CC1)C(=O)c1ccc2c(c1)nc1n2[C@@H](C(C)C)C(=O)Nc2c1cc(cc2)NC1CCCCCC1 19230660
CHEMBL463274 7846 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 542 4 2 6 5.8 CN1CCCN(CC1)C(=O)c1ccc2c(c1)nc1n2[C@@H](C(C)C)C(=O)Nc2c1cc(cc2)NC1CCCCCC1 19230660
2007 7953 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12915402
2007 7953 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15823563
2007 7953 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 23396314
2007 7953 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 28288109
4056 9772 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15823563




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
9566 10199 14 None - 2 Human 6.0 pEC50 = 6 Binding
Selectivity interaction (FLIPR assay) EUB0000353a MRGPRX2Selectivity interaction (FLIPR assay) EUB0000353a MRGPRX2
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5212743
95882507 10199 14 None - 2 Human 6.0 pEC50 = 6 Binding
Selectivity interaction (FLIPR assay) EUB0000353a MRGPRX2Selectivity interaction (FLIPR assay) EUB0000353a MRGPRX2
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5212743
CHEMBL4520293 10199 14 None - 2 Human 6.0 pEC50 = 6 Binding
Selectivity interaction (FLIPR assay) EUB0000353a MRGPRX2Selectivity interaction (FLIPR assay) EUB0000353a MRGPRX2
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5212743
12074028 197665 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonistic activity at MRGPRX2 (unknown origin)Agonistic activity at MRGPRX2 (unknown origin)
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2(c3cccc(O)c3)Cc3nc4ccccc4cc3C[C@@H]2C1 10.1016/j.bmcl.2021.128485
CHEMBL5184932 197665 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonistic activity at MRGPRX2 (unknown origin)Agonistic activity at MRGPRX2 (unknown origin)
ChEMBL 344 1 1 3 3.9 CN1CC[C@]2(c3cccc(O)c3)Cc3nc4ccccc4cc3C[C@@H]2C1 10.1016/j.bmcl.2021.128485
9566 10199 14 None - 2 Human 6.1 pEC50 = 6.1 Binding
Affinity On-target Cellular interaction (PRESTO-Tango concentration response assay (by the NIMH-PDSP)) EUB0000353a MRGPRX2Affinity On-target Cellular interaction (PRESTO-Tango concentration response assay (by the NIMH-PDSP)) EUB0000353a MRGPRX2
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5210121
95882507 10199 14 None - 2 Human 6.1 pEC50 = 6.1 Binding
Affinity On-target Cellular interaction (PRESTO-Tango concentration response assay (by the NIMH-PDSP)) EUB0000353a MRGPRX2Affinity On-target Cellular interaction (PRESTO-Tango concentration response assay (by the NIMH-PDSP)) EUB0000353a MRGPRX2
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5210121
CHEMBL4520293 10199 14 None - 2 Human 6.1 pEC50 = 6.1 Binding
Affinity On-target Cellular interaction (PRESTO-Tango concentration response assay (by the NIMH-PDSP)) EUB0000353a MRGPRX2Affinity On-target Cellular interaction (PRESTO-Tango concentration response assay (by the NIMH-PDSP)) EUB0000353a MRGPRX2
ChEMBL 307 3 0 5 2.5 CN([C@@H]1CCN(C1)c1cc(nc2n1ncc2)c1ccccc1)C 10.6019/CHEMBL5210121
129072557 183985 6 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at MRGPX2 (unknown origin)Agonist activity at MRGPX2 (unknown origin)
ChEMBL 763 9 5 10 3.1 Cc1cc(C[C@@H](NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)C(=O)N[C@@H](CC2CCNCC2)C(=O)N2CCN(c3ccncc3)CC2)cc2cn[nH]c12 10.1021/acs.jmedchem.0c01003
CHEMBL4635331 183985 6 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at MRGPX2 (unknown origin)Agonist activity at MRGPX2 (unknown origin)
ChEMBL 763 9 5 10 3.1 Cc1cc(C[C@@H](NC(=O)N2CCC3(CC2)OC(=O)Nc2ncccc23)C(=O)N[C@@H](CC2CCNCC2)C(=O)N2CCN(c3ccncc3)CC2)cc2cn[nH]c12 10.1021/acs.jmedchem.0c01003