Ligand source activities (1 row/activity)



Get vendors


<
Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page 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
44263999 205089 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL 558 15 5 6 3.3 COc1ccc(NC(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2ccccc2)C(=O)O)cc1 10.1021/jm950908d
CHEMBL7753 205089 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL 558 15 5 6 3.3 COc1ccc(NC(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2ccccc2)C(=O)O)cc1 10.1021/jm950908d
CHEMBL267388 210716 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL None None None CSCC[C@H](NC(=O)Nc1ccc(Cl)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
1022 1667 None 55 Human Functional pEC50 = 8 8.0 4897 3
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL None None None None 10.1021/jm900592h
443295 1667 None 55 Human Functional pEC50 = 8 8.0 4897 3
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL None None None None 10.1021/jm900592h
CHEMBL267179 1667 None 55 Human Functional pEC50 = 8 8.0 4897 3
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL None None None None 10.1021/jm900592h
145952664 162431 None 0 Human Functional pEC50 = 5.0 5.0 -1 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 500 9 3 4 4.6 COc1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)NCC2(c3ccc(C)c(F)c3)CC2)cc1 10.1016/j.ejmech.2017.09.023
CHEMBL4166385 162431 None 0 Human Functional pEC50 = 5.0 5.0 -1 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 500 9 3 4 4.6 COc1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)NCC2(c3ccc(C)c(F)c3)CC2)cc1 10.1016/j.ejmech.2017.09.023
71698968 90675 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 445 5 1 4 4.2 Cc1cc(Cc2cccc(Cl)c2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391281 90675 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 445 5 1 4 4.2 Cc1cc(Cc2cccc(Cl)c2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
44232677 196344 None 0 Human Functional pEC50 = 5.0 5.0 1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 408 7 1 7 2.7 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc([N+](=O)[O-])cc3)c2=O)c1 10.1021/jm900592h
CHEMBL562456 196344 None 0 Human Functional pEC50 = 5.0 5.0 1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 408 7 1 7 2.7 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc([N+](=O)[O-])cc3)c2=O)c1 10.1021/jm900592h
71698530 90670 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 509 7 1 5 5.3 COc1cccc(Cc2cc(C3CCCCC3)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
CHEMBL2391257 90670 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 509 7 1 5 5.3 COc1cccc(Cc2cc(C3CCCCC3)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
44233646 196421 None 0 Human Functional pEC50 = 6.0 6.0 1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 393 7 1 6 2.8 COc1ccc(NC(=O)Cn2nc(C)cc(Cc3cccc(OC)c3)c2=O)cc1 10.1021/jm900592h
CHEMBL562910 196421 None 0 Human Functional pEC50 = 6.0 6.0 1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 393 7 1 6 2.8 COc1ccc(NC(=O)Cn2nc(C)cc(Cc3cccc(OC)c3)c2=O)cc1 10.1021/jm900592h
44233646 196421 None 0 Human Functional pEC50 = 6.0 6.0 1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 393 7 1 6 2.8 COc1ccc(NC(=O)Cn2nc(C)cc(Cc3cccc(OC)c3)c2=O)cc1 10.1021/jm900592h
CHEMBL562910 196421 None 0 Human Functional pEC50 = 6.0 6.0 1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 393 7 1 6 2.8 COc1ccc(NC(=O)Cn2nc(C)cc(Cc3cccc(OC)c3)c2=O)cc1 10.1021/jm900592h
164916035 192348 None 3 Human Functional pEC50 = 6.0 6.0 -16 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.2 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5207056 192348 None 3 Human Functional pEC50 = 6.0 6.0 -16 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.2 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc32)cc1 10.1021/acs.jmedchem.1c02203
71698446 90707 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 427 5 1 5 3.6 COc1ccc(-c2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 10.1016/j.ejmech.2013.03.066
CHEMBL2391452 90707 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 427 5 1 5 3.6 COc1ccc(-c2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 10.1016/j.ejmech.2013.03.066
44232924 195321 None 0 Human Functional pEC50 = 5.0 5.0 -1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 455 7 1 5 3.9 COc1cccc(Cc2cc(C)nn(CCC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL551590 195321 None 0 Human Functional pEC50 = 5.0 5.0 -1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 455 7 1 5 3.9 COc1cccc(Cc2cc(C)nn(CCC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
44232924 195321 None 0 Human Functional pEC50 = 5.0 5.0 -1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 455 7 1 5 3.9 COc1cccc(Cc2cc(C)nn(CCC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL551590 195321 None 0 Human Functional pEC50 = 5.0 5.0 -1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 455 7 1 5 3.9 COc1cccc(Cc2cc(C)nn(CCC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
122487974 170412 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 497 9 1 5 5.3 CCCCC(C(=O)Nc1ccc(Br)cc1)n1nc(C)cc(Cc2cccc(OC)c2)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL4448213 170412 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 497 9 1 5 5.3 CCCCC(C(=O)Nc1ccc(Br)cc1)n1nc(C)cc(Cc2cccc(OC)c2)c1=O 10.1021/acs.jmedchem.8b01912
168279295 191044 None 0 Human Functional pEC50 = 5.9 5.9 -91 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.4 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5187135 191044 None 0 Human Functional pEC50 = 5.9 5.9 -91 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.4 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
71699142 90704 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 442 6 2 6 3.7 COc1ccc(Nc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 10.1016/j.ejmech.2013.03.066
CHEMBL2391449 90704 None 0 Human Functional pEC50 = 4.9 4.9 -1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 442 6 2 6 3.7 COc1ccc(Nc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 10.1016/j.ejmech.2013.03.066
71698365 90702 None 0 Human Functional pEC50 = 4.9 4.9 -7 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 484 7 2 7 3.9 COc1ccc(Nc2c(C(C)=O)c(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 10.1016/j.ejmech.2013.03.066
CHEMBL2391447 90702 None 0 Human Functional pEC50 = 4.9 4.9 -7 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 484 7 2 7 3.9 COc1ccc(Nc2c(C(C)=O)c(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 10.1016/j.ejmech.2013.03.066
71699061 90695 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 461 5 1 4 4.7 Cc1cc(Cc2cccc3ccccc23)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391438 90695 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 461 5 1 4 4.7 Cc1cc(Cc2cccc3ccccc23)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
146597625 191260 None 1 Human Functional pEC50 = 5.9 5.9 -47 2
Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
ChEMBL 420 5 2 6 3.4 COc1cc(F)c([C@@H]2CNC(=O)[C@H]2Nc2nnc(-c3ccc(Cl)cc3)o2)c(F)c1 10.1021/acsmedchemlett.2c00079
CHEMBL5190385 191260 None 1 Human Functional pEC50 = 5.9 5.9 -47 2
Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
ChEMBL 420 5 2 6 3.4 COc1cc(F)c([C@@H]2CNC(=O)[C@H]2Nc2nnc(-c3ccc(Cl)cc3)o2)c(F)c1 10.1021/acsmedchemlett.2c00079
168286767 191680 None 0 Human Functional pEC50 = 5.9 5.9 -53 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5196551 191680 None 0 Human Functional pEC50 = 5.9 5.9 -53 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
145949892 162818 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 459 9 3 5 3.6 O=C(Nc1ccc([N+](=O)[O-])cc1)N[C@H](Cc1cccnc1)C(=O)NCC1(c2ccccc2)CC1 10.1016/j.ejmech.2017.09.023
CHEMBL4172556 162818 None 0 Human Functional pEC50 = 5.8 5.8 -2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 459 9 3 5 3.6 O=C(Nc1ccc([N+](=O)[O-])cc1)N[C@H](Cc1cccnc1)C(=O)NCC1(c2ccccc2)CC1 10.1016/j.ejmech.2017.09.023
168279956 191081 None 0 Human Functional pEC50 = 5.8 5.8 -4 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 460 5 2 3 4.2 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc3C2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5187563 191081 None 0 Human Functional pEC50 = 5.8 5.8 -4 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 460 5 2 3 4.2 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc3C2)cc1 10.1021/acs.jmedchem.1c02203
168283359 190810 None 0 Human Functional pEC50 = 4.8 4.8 -5 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 5 2 3 3.1 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCC2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5183856 190810 None 0 Human Functional pEC50 = 4.8 4.8 -5 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 5 2 3 3.1 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCC2)cc1 10.1021/acs.jmedchem.1c02203
155519369 170376 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 441 7 1 6 4.0 COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Cl)cc3)c2=O)c1OC 10.1021/acs.jmedchem.8b01912
CHEMBL4447830 170376 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 441 7 1 6 4.0 COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Cl)cc3)c2=O)c1OC 10.1021/acs.jmedchem.8b01912
44233647 195533 None 0 Human Functional pEC50 = 4.8 4.8 -1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 423 8 1 7 2.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(OC)c(OC)c3)c2=O)c1 10.1021/jm900592h
CHEMBL554291 195533 None 0 Human Functional pEC50 = 4.8 4.8 -1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 423 8 1 7 2.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(OC)c(OC)c3)c2=O)c1 10.1021/jm900592h
54580795 61474 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assayAgonist activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 424 8 2 6 4.6 CCOc1ccc2oc(C(=O)NC(CCSC)c3nc4cnccc4[nH]3)c(C)c2c1 10.1016/j.bmcl.2011.03.049
CHEMBL1770476 61474 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assayAgonist activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay
ChEMBL 424 8 2 6 4.6 CCOc1ccc2oc(C(=O)NC(CCSC)c3nc4cnccc4[nH]3)c(C)c2c1 10.1016/j.bmcl.2011.03.049
44236330 194828 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 377 6 1 5 3.1 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL539401 194828 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 377 6 1 5 3.1 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C)cc3)c2=O)c1 10.1021/jm900592h
44236330 194828 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 377 6 1 5 3.1 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL539401 194828 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 377 6 1 5 3.1 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C)cc3)c2=O)c1 10.1021/jm900592h
168292800 192060 None 0 Human Functional pEC50 = 4.8 4.8 -3 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5202577 192060 None 0 Human Functional pEC50 = 4.8 4.8 -3 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
155516247 170027 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 411 6 1 5 4.0 COc1ccccc1Cc1cc(C)nn(C(C)C(=O)Nc2ccc(Cl)cc2)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL4442702 170027 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 411 6 1 5 4.0 COc1ccccc1Cc1cc(C)nn(C(C)C(=O)Nc2ccc(Cl)cc2)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL5076914 214467 None 4 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at human FPR1 expressed in HEK293-A cells assessed as ERK phosphorylation level incubated for 5 mins by ELISA assayAgonist activity at human FPR1 expressed in HEK293-A cells assessed as ERK phosphorylation level incubated for 5 mins by ELISA assay
ChEMBL None None None O=C(Nc1ccc(Br)cc1)NC1CCN(c2ccccc2)C1=O 10.1016/j.ejmech.2021.113805
168282160 190848 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.2 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3cc(F)ccc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5184490 190848 None 0 Human Functional pEC50 = 5.8 5.8 -1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.2 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3cc(F)ccc32)cc1 10.1021/acs.jmedchem.1c02203
168278342 191149 None 0 Human Functional pEC50 = 4.7 4.7 1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 394 5 2 3 3.4 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCCC2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5188537 191149 None 0 Human Functional pEC50 = 4.7 4.7 1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 394 5 2 3 3.4 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCCC2)cc1 10.1021/acs.jmedchem.1c02203
145953127 162437 None 0 Human Functional pEC50 = 4.7 4.7 -9 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 470 8 4 2 4.9 O=C(Nc1ccc(F)cc1)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC1(c2ccccc2)CC1 10.1016/j.ejmech.2017.09.023
CHEMBL4166447 162437 None 0 Human Functional pEC50 = 4.7 4.7 -9 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 470 8 4 2 4.9 O=C(Nc1ccc(F)cc1)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC1(c2ccccc2)CC1 10.1016/j.ejmech.2017.09.023
CHEMBL266802 210698 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL None None None CSCC[C@H](NC(=O)Nc1ccc(C)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
1022 1667 None 55 Human Functional pEC50 = 7.7 7.7 4897 3
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL None None None None 10.1021/jm950908d
443295 1667 None 55 Human Functional pEC50 = 7.7 7.7 4897 3
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL None None None None 10.1021/jm950908d
CHEMBL267179 1667 None 55 Human Functional pEC50 = 7.7 7.7 4897 3
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL None None None None 10.1021/jm950908d
44233648 195065 None 0 Human Functional pEC50 = 4.7 4.7 -2 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 431 6 1 5 3.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C(F)(F)F)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL549570 195065 None 0 Human Functional pEC50 = 4.7 4.7 -2 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 431 6 1 5 3.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C(F)(F)F)cc3)c2=O)c1 10.1021/jm900592h
44233648 195065 None 0 Human Functional pEC50 = 4.7 4.7 -2 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 431 6 1 5 3.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C(F)(F)F)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL549570 195065 None 0 Human Functional pEC50 = 4.7 4.7 -2 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 431 6 1 5 3.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C(F)(F)F)cc3)c2=O)c1 10.1021/jm900592h
168280238 190952 None 0 Human Functional pEC50 = 5.7 5.7 -6 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2Cc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5185921 190952 None 0 Human Functional pEC50 = 5.7 5.7 -6 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2Cc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
155519289 170363 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 427 7 1 6 3.5 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1OC 10.1021/acs.jmedchem.8b01912
CHEMBL4447632 170363 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 427 7 1 6 3.5 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1OC 10.1021/acs.jmedchem.8b01912
44232675 195661 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 407 6 1 7 2.5 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc4c(c3)OCO4)c2=O)c1 10.1021/jm900592h
CHEMBL556485 195661 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 407 6 1 7 2.5 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc4c(c3)OCO4)c2=O)c1 10.1021/jm900592h
145978177 163059 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 452 8 4 2 4.7 O=C(Nc1ccccc1)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC1(c2ccccc2)CC1 10.1016/j.ejmech.2017.09.023
CHEMBL4176353 163059 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 452 8 4 2 4.7 O=C(Nc1ccccc1)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC1(c2ccccc2)CC1 10.1016/j.ejmech.2017.09.023
168283038 190925 None 0 Human Functional pEC50 = 5.6 5.6 -16 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 429 5 2 4 3.4 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3cccnc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5185462 190925 None 0 Human Functional pEC50 = 5.6 5.6 -16 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 429 5 2 4 3.4 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3cccnc32)cc1 10.1021/acs.jmedchem.1c02203
122487986 175972 None 0 Human Functional pEC50 = 4.6 4.6 -1 2
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 411 6 1 5 4.0 COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Cl)cc3)c2=O)c1 10.1021/acs.jmedchem.8b01912
CHEMBL4588649 175972 None 0 Human Functional pEC50 = 4.6 4.6 -1 2
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 411 6 1 5 4.0 COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Cl)cc3)c2=O)c1 10.1021/acs.jmedchem.8b01912
122181231 121705 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilizationAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization
ChEMBL 555 10 4 5 5.3 COc1ccc(NC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC2(c3ccc(OC)cn3)CCCCC2)cc1 10.1016/j.ejmech.2017.09.023
CHEMBL3588871 121705 None 0 Human Functional pEC50 = 6.6 6.6 -3 3
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilizationAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization
ChEMBL 555 10 4 5 5.3 COc1ccc(NC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC2(c3ccc(OC)cn3)CCCCC2)cc1 10.1016/j.ejmech.2017.09.023
44236328 195674 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 397 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL556625 195674 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 397 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1 10.1021/jm900592h
44236326 195320 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 441 6 1 5 3.6 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL551589 195320 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 441 6 1 5 3.6 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
44236326 195320 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 441 6 1 5 3.6 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL551589 195320 None 0 Human Functional pEC50 = 5.6 5.6 -1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 441 6 1 5 3.6 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
168281748 190883 None 0 Human Functional pEC50 = 5.6 5.6 -6 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 460 5 2 3 4.2 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc3C2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5184913 190883 None 0 Human Functional pEC50 = 5.6 5.6 -6 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 460 5 2 3 4.2 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc3C2)cc1 10.1021/acs.jmedchem.1c02203
168283383 190842 None 0 Human Functional pEC50 = 4.6 4.6 -3 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 5 2 3 3.1 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCC2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5184396 190842 None 0 Human Functional pEC50 = 4.6 4.6 -3 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 5 2 3 3.1 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCC2)cc1 10.1021/acs.jmedchem.1c02203
44233644 196088 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 489 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(I)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL560780 196088 None 0 Human Functional pEC50 = 5.6 5.6 1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 489 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(I)cc3)c2=O)c1 10.1021/jm900592h
145952485 162851 None 0 Human Functional pEC50 = 5.6 5.6 -2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 483 9 3 5 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc([N+](=O)[O-])cc2)C(=O)NCC2(c3ccccc3)CC2)cc1 10.1016/j.ejmech.2017.09.023
CHEMBL4172968 162851 None 0 Human Functional pEC50 = 5.6 5.6 -2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 483 9 3 5 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc([N+](=O)[O-])cc2)C(=O)NCC2(c3ccccc3)CC2)cc1 10.1016/j.ejmech.2017.09.023
155538591 172403 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 427 7 1 6 3.5 COc1cccc(OC)c1Cc1cc(C)nn(CC(=O)Nc2ccc(Cl)cc2)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL4476616 172403 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 427 7 1 6 3.5 COc1cccc(OC)c1Cc1cc(C)nn(CC(=O)Nc2ccc(Cl)cc2)c1=O 10.1021/acs.jmedchem.8b01912
168282231 190960 None 0 Human Functional pEC50 = 5.5 5.5 -16 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.2 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5185982 190960 None 0 Human Functional pEC50 = 5.5 5.5 -16 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.2 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc32)cc1 10.1021/acs.jmedchem.1c02203
168291793 191929 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 429 5 2 4 3.4 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3cccnc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5200365 191929 None 0 Human Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 429 5 2 4 3.4 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3cccnc32)cc1 10.1021/acs.jmedchem.1c02203
71699063 90698 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 454 6 2 5 2.6 Cc1cc(Cc2ccc(C(N)=O)cc2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391440 90698 None 0 Human Functional pEC50 = 4.5 4.5 -1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 454 6 2 5 2.6 Cc1cc(Cc2ccc(C(N)=O)cc2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL265408 210645 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL None None None CCCCNC(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
71698362 90701 None 0 Human Functional pEC50 = 5.5 5.5 -3 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 455 6 1 6 3.2 COc1cccc(C(=O)c2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
CHEMBL2391446 90701 None 0 Human Functional pEC50 = 5.5 5.5 -3 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 455 6 1 6 3.2 COc1cccc(C(=O)c2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
CHEMBL7306 215870 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL None None None CSCC[C@H](NC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
24776341 3237 None 39 Human Functional pEC50 = 7.5 7.5 -20 4
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 4 4.6 O=C(Nc1c(C(C)C)n(n(c1=O)c1ccccc1)C)Nc1ccc(cc1)Cl 10.1021/acs.jmedchem.8b01912
5831 3237 None 39 Human Functional pEC50 = 7.5 7.5 -20 4
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 4 4.6 O=C(Nc1c(C(C)C)n(n(c1=O)c1ccccc1)C)Nc1ccc(cc1)Cl 10.1021/acs.jmedchem.8b01912
CHEMBL379761 3237 None 39 Human Functional pEC50 = 7.5 7.5 -20 4
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 384 4 2 4 4.6 O=C(Nc1c(C(C)C)n(n(c1=O)c1ccccc1)C)Nc1ccc(cc1)Cl 10.1021/acs.jmedchem.8b01912
164916036 191585 None 0 Human Functional pEC50 = 6.5 6.5 -147 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5195186 191585 None 0 Human Functional pEC50 = 6.5 6.5 -147 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
44232925 196647 None 2 Human Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 455 6 1 5 4.1 COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL564392 196647 None 2 Human Functional pEC50 = 5.5 5.5 -2 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 455 6 1 5 4.1 COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
44233644 196088 None 0 Human Functional pEC50 = 5.5 5.5 1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 489 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(I)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL560780 196088 None 0 Human Functional pEC50 = 5.5 5.5 1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 489 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(I)cc3)c2=O)c1 10.1021/jm900592h
44233645 196183 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 363 6 1 5 2.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccccc3)c2=O)c1 10.1021/jm900592h
CHEMBL561375 196183 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 363 6 1 5 2.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccccc3)c2=O)c1 10.1021/jm900592h
44233644 196088 None 0 Human Functional pEC50 = 5.5 5.5 1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 489 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(I)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL560780 196088 None 0 Human Functional pEC50 = 5.5 5.5 1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 489 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(I)cc3)c2=O)c1 10.1021/jm900592h
44233645 196183 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 363 6 1 5 2.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccccc3)c2=O)c1 10.1021/jm900592h
CHEMBL561375 196183 None 0 Human Functional pEC50 = 5.5 5.5 -5 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 363 6 1 5 2.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccccc3)c2=O)c1 10.1021/jm900592h
168283929 191098 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.1 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2Cc3ccc(F)cc3C2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5187763 191098 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.1 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2Cc3ccc(F)cc3C2)cc1 10.1021/acs.jmedchem.1c02203
44236326 195320 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 441 6 1 5 3.6 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL551589 195320 None 0 Human Functional pEC50 = 5.5 5.5 -1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 441 6 1 5 3.6 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
44233647 195533 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 423 8 1 7 2.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(OC)c(OC)c3)c2=O)c1 10.1021/jm900592h
CHEMBL554291 195533 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 423 8 1 7 2.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(OC)c(OC)c3)c2=O)c1 10.1021/jm900592h
44232675 195661 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 407 6 1 7 2.5 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc4c(c3)OCO4)c2=O)c1 10.1021/jm900592h
CHEMBL556485 195661 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 407 6 1 7 2.5 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc4c(c3)OCO4)c2=O)c1 10.1021/jm900592h
44233647 195533 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 423 8 1 7 2.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(OC)c(OC)c3)c2=O)c1 10.1021/jm900592h
CHEMBL554291 195533 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 423 8 1 7 2.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(OC)c(OC)c3)c2=O)c1 10.1021/jm900592h
44232675 195661 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 407 6 1 7 2.5 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc4c(c3)OCO4)c2=O)c1 10.1021/jm900592h
CHEMBL556485 195661 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 407 6 1 7 2.5 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc4c(c3)OCO4)c2=O)c1 10.1021/jm900592h
44236329 195445 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 381 6 1 5 2.9 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(F)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL552396 195445 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 381 6 1 5 2.9 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(F)cc3)c2=O)c1 10.1021/jm900592h
44236329 195445 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 381 6 1 5 2.9 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(F)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL552396 195445 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 381 6 1 5 2.9 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(F)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL7520 215873 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL None None None CSCC[C@H](NC(=O)Nc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
11024 687 None 19 Human Functional pEC50 = 6.4 6.4 -177 4
Agonist activity at human FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 361 4 3 3 2.4 COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 10.1021/acs.jmedchem.9b02101
122583088 687 None 19 Human Functional pEC50 = 6.4 6.4 -177 4
Agonist activity at human FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 361 4 3 3 2.4 COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 10.1021/acs.jmedchem.9b02101
CHEMBL4784510 687 None 19 Human Functional pEC50 = 6.4 6.4 -177 4
Agonist activity at human FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 361 4 3 3 2.4 COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 10.1021/acs.jmedchem.9b02101
11024 687 None 19 Human Functional pEC50 = 6.4 6.4 -177 4
Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
ChEMBL 361 4 3 3 2.4 COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 10.1021/acsmedchemlett.2c00079
122583088 687 None 19 Human Functional pEC50 = 6.4 6.4 -177 4
Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
ChEMBL 361 4 3 3 2.4 COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 10.1021/acsmedchemlett.2c00079
CHEMBL4784510 687 None 19 Human Functional pEC50 = 6.4 6.4 -177 4
Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
ChEMBL 361 4 3 3 2.4 COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 10.1021/acsmedchemlett.2c00079
168296342 192445 None 0 Human Functional pEC50 = 4.4 4.4 -2 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2Cc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5208434 192445 None 0 Human Functional pEC50 = 4.4 4.4 -2 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2Cc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
71698528 90668 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 503 7 1 5 3.6 CCc1cc(Cc2cccc(OC)c2)c(=O)n(CC(=O)Nc2ccc(I)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391255 90668 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 503 7 1 5 3.6 CCc1cc(Cc2cccc(OC)c2)c(=O)n(CC(=O)Nc2ccc(I)cc2)n1 10.1016/j.ejmech.2013.03.066
168274924 190267 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 456 5 2 3 4.8 CC1(C)CN(C(=O)[C@H](Cc2ccc(C#N)cc2)NC(=O)Nc2ccc(F)cc2)c2ccccc21 10.1021/acs.jmedchem.1c02203
CHEMBL5175543 190267 None 0 Human Functional pEC50 = 5.4 5.4 -1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 456 5 2 3 4.8 CC1(C)CN(C(=O)[C@H](Cc2ccc(C#N)cc2)NC(=O)Nc2ccc(F)cc2)c2ccccc21 10.1021/acs.jmedchem.1c02203
168273654 190324 None 0 Human Functional pEC50 = 5.4 5.4 -6 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 437 6 4 4 2.2 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)NC2CCCCNC2=O)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5176452 190324 None 0 Human Functional pEC50 = 5.4 5.4 -6 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 437 6 4 4 2.2 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)NC2CCCCNC2=O)cc1 10.1021/acs.jmedchem.1c02203
122181231 121705 None 0 Human Functional pEC50 = 6.4 6.4 -3 3
Agonist activity at human FPR1 transfected in human HL60 cells assessed as stimulation of Ca2+ influx measured every 5 secs for 240 secs by FLIPR assayAgonist activity at human FPR1 transfected in human HL60 cells assessed as stimulation of Ca2+ influx measured every 5 secs for 240 secs by FLIPR assay
ChEMBL 555 10 4 5 5.3 COc1ccc(NC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC2(c3ccc(OC)cn3)CCCCC2)cc1 10.1016/j.bmc.2014.12.007
CHEMBL3588871 121705 None 0 Human Functional pEC50 = 6.4 6.4 -3 3
Agonist activity at human FPR1 transfected in human HL60 cells assessed as stimulation of Ca2+ influx measured every 5 secs for 240 secs by FLIPR assayAgonist activity at human FPR1 transfected in human HL60 cells assessed as stimulation of Ca2+ influx measured every 5 secs for 240 secs by FLIPR assay
ChEMBL 555 10 4 5 5.3 COc1ccc(NC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC2(c3ccc(OC)cn3)CCCCC2)cc1 10.1016/j.bmc.2014.12.007
44233905 196331 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 441 6 1 5 3.6 COc1ccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 10.1021/jm900592h
CHEMBL562380 196331 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 441 6 1 5 3.6 COc1ccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 10.1021/jm900592h
44233905 196331 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 441 6 1 5 3.6 COc1ccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 10.1021/jm900592h
CHEMBL562380 196331 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 441 6 1 5 3.6 COc1ccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 10.1021/jm900592h
168281597 191268 None 0 Human Functional pEC50 = 6.4 6.4 -50 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.4 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5190571 191268 None 0 Human Functional pEC50 = 6.4 6.4 -50 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.4 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
145956361 162009 None 0 Human Functional pEC50 = 6.4 6.4 2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 520 9 3 4 4.9 COc1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)NCC2(c3ccc(F)c(Cl)c3)CC2)cc1 10.1016/j.ejmech.2017.09.023
CHEMBL4159569 162009 None 0 Human Functional pEC50 = 6.4 6.4 2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 520 9 3 4 4.9 COc1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)NCC2(c3ccc(F)c(Cl)c3)CC2)cc1 10.1016/j.ejmech.2017.09.023
71698529 90669 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 469 7 1 5 4.4 COc1cccc(Cc2cc(C(C)C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
CHEMBL2391256 90669 None 0 Human Functional pEC50 = 5.4 5.4 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 469 7 1 5 4.4 COc1cccc(Cc2cc(C(C)C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
71699059 90677 None 0 Human Functional pEC50 = 5.4 5.4 3 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 417 5 1 5 3.6 Cc1cc(Cc2ccsc2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391286 90677 None 0 Human Functional pEC50 = 5.4 5.4 3 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 417 5 1 5 3.6 Cc1cc(Cc2ccsc2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
146597621 191335 None 0 Human Functional pEC50 = 6.3 6.3 -33 2
Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
ChEMBL 419 5 2 5 4.0 COc1cc(F)c([C@@H]2CNC(=O)[C@H]2Nc2cc(-c3ccc(Cl)cc3)on2)c(F)c1 10.1021/acsmedchemlett.2c00079
CHEMBL5191583 191335 None 0 Human Functional pEC50 = 6.3 6.3 -33 2
Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
ChEMBL 419 5 2 5 4.0 COc1cc(F)c([C@@H]2CNC(=O)[C@H]2Nc2cc(-c3ccc(Cl)cc3)on2)c(F)c1 10.1021/acsmedchemlett.2c00079
145956762 162166 None 0 Human Functional pEC50 = 5.3 5.3 -1 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 483 9 3 5 4.0 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc([N+](=O)[O-])cc2)C(=O)NCC2(c3ccccc3)CC2)cc1 10.1016/j.ejmech.2017.09.023
CHEMBL4162303 162166 None 0 Human Functional pEC50 = 5.3 5.3 -1 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 483 9 3 5 4.0 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc([N+](=O)[O-])cc2)C(=O)NCC2(c3ccccc3)CC2)cc1 10.1016/j.ejmech.2017.09.023
163322252 191878 None 5 Human Functional pEC50 = 5.3 5.3 -26 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.2 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3cc(F)ccc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5199629 191878 None 5 Human Functional pEC50 = 5.3 5.3 -26 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.2 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3cc(F)ccc32)cc1 10.1021/acs.jmedchem.1c02203
457933 215721 None 28 Human Functional pEC50 = 6.3 6.3 -501 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](CCSC)C(N)=O)C(C)C 10.1021/jm900592h
CHEMBL552527 215721 None 28 Human Functional pEC50 = 6.3 6.3 -501 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](CCSC)C(N)=O)C(C)C 10.1021/jm900592h
11024 687 None 19 Mouse Functional pEC50 = 6.3 6.3 -12 4
Agonist activity at mouse FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at mouse FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 361 4 3 3 2.4 COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 10.1021/acs.jmedchem.9b02101
122583088 687 None 19 Mouse Functional pEC50 = 6.3 6.3 -12 4
Agonist activity at mouse FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at mouse FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 361 4 3 3 2.4 COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 10.1021/acs.jmedchem.9b02101
CHEMBL4784510 687 None 19 Mouse Functional pEC50 = 6.3 6.3 -12 4
Agonist activity at mouse FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at mouse FPR1 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 361 4 3 3 2.4 COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 10.1021/acs.jmedchem.9b02101
145958736 162214 None 0 Human Functional pEC50 = 5.3 5.3 -6 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 508 8 3 3 5.1 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)NCC2(c3ccc(F)c(Cl)c3)CC2)cc1 10.1016/j.ejmech.2017.09.023
CHEMBL4162930 162214 None 0 Human Functional pEC50 = 5.3 5.3 -6 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 508 8 3 3 5.1 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)NCC2(c3ccc(F)c(Cl)c3)CC2)cc1 10.1016/j.ejmech.2017.09.023
155555898 174365 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 453 9 1 5 5.2 CCCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2cccc(OC)c2)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL4551649 174365 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 453 9 1 5 5.2 CCCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2cccc(OC)c2)c1=O 10.1021/acs.jmedchem.8b01912
146035589 173727 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 483 10 1 6 5.2 CCCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2cccc(OC)c2OC)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL4536334 173727 None 0 Human Functional pEC50 = 7.3 7.3 -1 2
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 483 10 1 6 5.2 CCCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2cccc(OC)c2OC)c1=O 10.1021/acs.jmedchem.8b01912
145951856 162889 None 0 Human Functional pEC50 = 5.3 5.3 -8 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 508 8 3 3 5.1 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)NCC2(c3ccc(F)c(Cl)c3)CC2)cc1 10.1016/j.ejmech.2017.09.023
CHEMBL4173645 162889 None 0 Human Functional pEC50 = 5.3 5.3 -8 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 508 8 3 3 5.1 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)NCC2(c3ccc(F)c(Cl)c3)CC2)cc1 10.1016/j.ejmech.2017.09.023
71698880 90672 None 0 Human Functional pEC50 = 5.3 5.3 2 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 411 5 1 4 3.5 Cc1cc(Cc2ccccc2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391277 90672 None 0 Human Functional pEC50 = 5.3 5.3 2 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 411 5 1 4 3.5 Cc1cc(Cc2ccccc2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
162425412 191066 None 0 Human Functional pEC50 = 5.3 5.3 -21 2
Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
ChEMBL 386 5 2 6 2.7 COc1cc(F)c([C@@H]2CNC(=O)[C@H]2Nc2nnc(-c3ccccc3)o2)c(F)c1 10.1021/acsmedchemlett.2c00079
CHEMBL5187399 191066 None 0 Human Functional pEC50 = 5.3 5.3 -21 2
Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
ChEMBL 386 5 2 6 2.7 COc1cc(F)c([C@@H]2CNC(=O)[C@H]2Nc2nnc(-c3ccccc3)o2)c(F)c1 10.1021/acsmedchemlett.2c00079
168278240 191099 None 0 Human Functional pEC50 = 5.3 5.3 1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.1 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2Cc3ccc(F)cc3C2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5187767 191099 None 0 Human Functional pEC50 = 5.3 5.3 1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 446 5 2 3 4.1 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2Cc3ccc(F)cc3C2)cc1 10.1021/acs.jmedchem.1c02203
44233648 195065 None 0 Human Functional pEC50 = 5.2 5.2 -2 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 431 6 1 5 3.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C(F)(F)F)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL549570 195065 None 0 Human Functional pEC50 = 5.2 5.2 -2 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 431 6 1 5 3.8 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C(F)(F)F)cc3)c2=O)c1 10.1021/jm900592h
71698972 90676 None 0 Human Functional pEC50 = 5.2 5.2 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 401 5 1 5 3.1 Cc1cc(Cc2ccoc2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391285 90676 None 0 Human Functional pEC50 = 5.2 5.2 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 401 5 1 5 3.1 Cc1cc(Cc2ccoc2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
145955803 162644 None 0 Human Functional pEC50 = 5.2 5.2 -2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 488 8 3 3 4.7 Cc1ccc(C2(CNC(=O)[C@H](Cc3ccc(C#N)cc3)NC(=O)Nc3ccc(F)cc3)CC2)cc1F 10.1016/j.ejmech.2017.09.023
CHEMBL4169807 162644 None 0 Human Functional pEC50 = 5.2 5.2 -2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 488 8 3 3 4.7 Cc1ccc(C2(CNC(=O)[C@H](Cc3ccc(C#N)cc3)NC(=O)Nc3ccc(F)cc3)CC2)cc1F 10.1016/j.ejmech.2017.09.023
154706263 173567 None 2 Human Functional pEC50 = 8.2 8.2 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 527 10 1 6 5.3 CCCCC(C(=O)Nc1ccc(Br)cc1)n1nc(C)cc(Cc2cccc(OC)c2OC)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL4532583 173567 None 2 Human Functional pEC50 = 8.2 8.2 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 527 10 1 6 5.3 CCCCC(C(=O)Nc1ccc(Br)cc1)n1nc(C)cc(Cc2cccc(OC)c2OC)c1=O 10.1021/acs.jmedchem.8b01912
146035588 170894 None 2 Human Functional pEC50 = 6.2 6.2 -5 2
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 453 9 1 5 5.2 CCCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2ccccc2OC)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL4454594 170894 None 2 Human Functional pEC50 = 6.2 6.2 -5 2
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 453 9 1 5 5.2 CCCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2ccccc2OC)c1=O 10.1021/acs.jmedchem.8b01912
71698527 90667 None 0 Human Functional pEC50 = 5.2 5.2 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 427 6 1 5 3.2 COc1cccc(Cc2ccnn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
CHEMBL2391254 90667 None 0 Human Functional pEC50 = 5.2 5.2 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 427 6 1 5 3.2 COc1cccc(Cc2ccnn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
145956276 162674 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 520 9 3 4 4.9 COc1ccc(NC(=O)N[C@H](Cc2ccc(C#N)cc2)C(=O)NCC2(c3ccc(F)c(Cl)c3)CC2)cc1 10.1016/j.ejmech.2017.09.023
CHEMBL4170201 162674 None 0 Human Functional pEC50 = 6.2 6.2 1 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 520 9 3 4 4.9 COc1ccc(NC(=O)N[C@H](Cc2ccc(C#N)cc2)C(=O)NCC2(c3ccc(F)c(Cl)c3)CC2)cc1 10.1016/j.ejmech.2017.09.023
122488043 174264 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 427 7 1 6 3.5 COc1ccc(OC)c(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1 10.1021/acs.jmedchem.8b01912
CHEMBL4549250 174264 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 427 7 1 6 3.5 COc1ccc(OC)c(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1 10.1021/acs.jmedchem.8b01912
71698967 90674 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 429 5 1 4 3.7 Cc1cc(Cc2cccc(F)c2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391280 90674 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 429 5 1 4 3.7 Cc1cc(Cc2cccc(F)c2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
44236328 195674 None 0 Human Functional pEC50 = 5.2 5.2 -1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 397 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL556625 195674 None 0 Human Functional pEC50 = 5.2 5.2 -1 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 397 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1 10.1021/jm900592h
44236328 195674 None 0 Human Functional pEC50 = 5.2 5.2 -1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 397 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL556625 195674 None 0 Human Functional pEC50 = 5.2 5.2 -1 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 397 6 1 5 3.4 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1 10.1021/jm900592h
168269851 189964 None 0 Human Functional pEC50 = 5.2 5.2 -3 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.0 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5170711 189964 None 0 Human Functional pEC50 = 5.2 5.2 -3 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.0 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
168278228 191078 None 0 Human Functional pEC50 = 5.2 5.2 -3 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 394 5 2 3 3.4 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCCC2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5187530 191078 None 0 Human Functional pEC50 = 5.2 5.2 -3 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 394 5 2 3 3.4 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCCC2)cc1 10.1021/acs.jmedchem.1c02203
71698966 90673 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 377 5 1 6 2.5 Cc1cc(Cc2ccccc2)c(=O)n(CC(=O)Nc2ccc3c(c2)OCO3)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391279 90673 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 377 5 1 6 2.5 Cc1cc(Cc2ccccc2)c(=O)n(CC(=O)Nc2ccc3c(c2)OCO3)n1 10.1016/j.ejmech.2013.03.066
168284664 191511 None 0 Human Functional pEC50 = 5.2 5.2 -7 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 488 5 2 3 4.9 CC1(C)CN(C(=O)[C@H](Cc2ccc(C#N)cc2)NC(=O)Nc2ccc(F)cc2)Cc2cc(F)ccc21 10.1021/acs.jmedchem.1c02203
CHEMBL5193947 191511 None 0 Human Functional pEC50 = 5.2 5.2 -7 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 488 5 2 3 4.9 CC1(C)CN(C(=O)[C@H](Cc2ccc(C#N)cc2)NC(=O)Nc2ccc(F)cc2)Cc2cc(F)ccc21 10.1021/acs.jmedchem.1c02203
44236330 194828 None 0 Human Functional pEC50 = 5.1 5.1 -1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 377 6 1 5 3.1 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL539401 194828 None 0 Human Functional pEC50 = 5.1 5.1 -1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 377 6 1 5 3.1 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(C)cc3)c2=O)c1 10.1021/jm900592h
71699065 90699 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 519 7 1 6 3.4 COc1cc(Cc2cc(C)nn(CC(=O)Nc3ccc(I)cc3)c2=O)cc(OC)c1 10.1016/j.ejmech.2013.03.066
CHEMBL2391442 90699 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 519 7 1 6 3.4 COc1cc(Cc2cc(C)nn(CC(=O)Nc3ccc(I)cc3)c2=O)cc(OC)c1 10.1016/j.ejmech.2013.03.066
44236329 195445 None 0 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 381 6 1 5 2.9 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(F)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL552396 195445 None 0 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 381 6 1 5 2.9 COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(F)cc3)c2=O)c1 10.1021/jm900592h
44233646 196421 None 0 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 393 7 1 6 2.8 COc1ccc(NC(=O)Cn2nc(C)cc(Cc3cccc(OC)c3)c2=O)cc1 10.1021/jm900592h
CHEMBL562910 196421 None 0 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 393 7 1 6 2.8 COc1ccc(NC(=O)Cn2nc(C)cc(Cc3cccc(OC)c3)c2=O)cc1 10.1021/jm900592h
164916034 191688 None 0 Human Functional pEC50 = 6.1 6.1 -6 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 437 6 4 4 2.2 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)NC2CCCCNC2=O)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5196771 191688 None 0 Human Functional pEC50 = 6.1 6.1 -6 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 437 6 4 4 2.2 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)NC2CCCCNC2=O)cc1 10.1021/acs.jmedchem.1c02203
44232925 196647 None 2 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 455 6 1 5 4.1 COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL564392 196647 None 2 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 455 6 1 5 4.1 COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
44232925 196647 None 2 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 455 6 1 5 4.1 COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL564392 196647 None 2 Human Functional pEC50 = 6.1 6.1 -2 2
Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay
ChEMBL 455 6 1 5 4.1 COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
71699060 90694 None 0 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 417 5 1 5 3.6 Cc1cc(Cc2cccs2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391437 90694 None 0 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 417 5 1 5 3.6 Cc1cc(Cc2cccs2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
71698442 90703 None 0 Human Functional pEC50 = 5.1 5.1 3 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 336 3 2 5 1.5 Cc1cc(N)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391448 90703 None 0 Human Functional pEC50 = 5.1 5.1 3 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 336 3 2 5 1.5 Cc1cc(N)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
145963525 162321 None 0 Human Functional pEC50 = 6.1 6.1 2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 459 9 3 5 3.6 O=C(Nc1ccc([N+](=O)[O-])cc1)N[C@@H](Cc1cccnc1)C(=O)NCC1(c2ccccc2)CC1 10.1016/j.ejmech.2017.09.023
CHEMBL4164673 162321 None 0 Human Functional pEC50 = 6.1 6.1 2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 459 9 3 5 3.6 O=C(Nc1ccc([N+](=O)[O-])cc1)N[C@@H](Cc1cccnc1)C(=O)NCC1(c2ccccc2)CC1 10.1016/j.ejmech.2017.09.023
146035588 170894 None 2 Human Functional pEC50 = 6.1 6.1 -5 2
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 453 9 1 5 5.2 CCCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2ccccc2OC)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL4454594 170894 None 2 Human Functional pEC50 = 6.1 6.1 -5 2
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 453 9 1 5 5.2 CCCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2ccccc2OC)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL6997 215864 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils
ChEMBL None None None CSCC[C@H](NC(=O)Nc1cccc(C)c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
71698531 90671 None 0 Human Functional pEC50 = 5.1 5.1 -2 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 503 7 1 5 4.9 COc1cccc(Cc2cc(-c3ccccc3)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
CHEMBL2391258 90671 None 0 Human Functional pEC50 = 5.1 5.1 -2 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 503 7 1 5 4.9 COc1cccc(Cc2cc(-c3ccccc3)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
168272319 190573 None 0 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 456 5 2 3 4.8 CC1(C)CN(C(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)Nc2ccc(F)cc2)c2ccccc21 10.1021/acs.jmedchem.1c02203
CHEMBL5180261 190573 None 0 Human Functional pEC50 = 5.1 5.1 1 2
Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 456 5 2 3 4.8 CC1(C)CN(C(=O)[C@@H](Cc2ccc(C#N)cc2)NC(=O)Nc2ccc(F)cc2)c2ccccc21 10.1021/acs.jmedchem.1c02203
71699062 90696 None 0 Human Functional pEC50 = 5.0 5.0 -3 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 412 5 1 5 2.9 Cc1cc(Cc2cccnc2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391439 90696 None 0 Human Functional pEC50 = 5.0 5.0 -3 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 412 5 1 5 2.9 Cc1cc(Cc2cccnc2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 10.1016/j.ejmech.2013.03.066
71699143 90706 None 0 Human Functional pEC50 = 5.0 5.0 -3 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 470 6 2 6 3.2 COc1cccc(C(=O)Nc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
CHEMBL2391450 90706 None 0 Human Functional pEC50 = 5.0 5.0 -3 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 470 6 2 6 3.2 COc1cccc(C(=O)Nc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1016/j.ejmech.2013.03.066
145954612 162568 None 0 Human Functional pEC50 = 6.0 6.0 -2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 482 9 4 3 4.8 COc1ccc(NC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC2(c3ccccc3)CC2)cc1 10.1016/j.ejmech.2017.09.023
CHEMBL4168567 162568 None 0 Human Functional pEC50 = 6.0 6.0 -2 2
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
ChEMBL 482 9 4 3 4.8 COc1ccc(NC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC2(c3ccccc3)CC2)cc1 10.1016/j.ejmech.2017.09.023
122181322 121861 None 0 Human Functional pEC50 = 6.0 6.0 -1 3
Agonist activity at human FPR1 transfected in human HL60 cells assessed as stimulation of Ca2+ influx measured every 5 secs for 240 secs by FLIPR assayAgonist activity at human FPR1 transfected in human HL60 cells assessed as stimulation of Ca2+ influx measured every 5 secs for 240 secs by FLIPR assay
ChEMBL 525 9 4 4 5.3 COc1ccc(NC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC2(c3ccccn3)CCCCC2)cc1 10.1016/j.bmc.2014.12.007
CHEMBL3590073 121861 None 0 Human Functional pEC50 = 6.0 6.0 -1 3
Agonist activity at human FPR1 transfected in human HL60 cells assessed as stimulation of Ca2+ influx measured every 5 secs for 240 secs by FLIPR assayAgonist activity at human FPR1 transfected in human HL60 cells assessed as stimulation of Ca2+ influx measured every 5 secs for 240 secs by FLIPR assay
ChEMBL 525 9 4 4 5.3 COc1ccc(NC(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC2(c3ccccn3)CCCCC2)cc1 10.1016/j.bmc.2014.12.007
71699139 90700 None 0 Human Functional pEC50 = 5.0 5.0 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 493 5 1 4 4.0 Cc1cc(Cc2cccc(Cl)c2)c(=O)n(CC(=O)Nc2ccc(I)cc2)n1 10.1016/j.ejmech.2013.03.066
CHEMBL2391443 90700 None 0 Human Functional pEC50 = 5.0 5.0 1 2
Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization
ChEMBL 493 5 1 4 4.0 Cc1cc(Cc2cccc(Cl)c2)c(=O)n(CC(=O)Nc2ccc(I)cc2)n1 10.1016/j.ejmech.2013.03.066
44232924 195321 None 0 Human Functional pEC50 = 5.0 5.0 -1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 455 7 1 5 3.9 COc1cccc(Cc2cc(C)nn(CCC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
CHEMBL551590 195321 None 0 Human Functional pEC50 = 5.0 5.0 -1 2
Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay
ChEMBL 455 7 1 5 3.9 COc1cccc(Cc2cc(C)nn(CCC(=O)Nc3ccc(Br)cc3)c2=O)c1 10.1021/jm900592h
155555363 174372 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 439 8 1 5 4.8 CCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2ccccc2OC)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL4551842 174372 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
ChEMBL 439 8 1 5 4.8 CCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2ccccc2OC)c1=O 10.1021/acs.jmedchem.8b01912
CHEMBL1628710 56272 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at FPR1Antagonist activity at FPR1
ChEMBL None None None None 10.1016/j.bmcl.2011.03.049
CHEMBL6450 215852 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
57399909 68284 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 452 6 2 5 4.3 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC3CCCCC3C)cnn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916276 68284 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 452 6 2 5 4.3 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC3CCCCC3C)cnn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
57398259 68293 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 446 6 2 5 4.4 Cc1nn(-c2ccccc2)c(NS(=O)(=O)C2CCCCC2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.08.085
CHEMBL1916286 68293 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 446 6 2 5 4.4 Cc1nn(-c2ccccc2)c(NS(=O)(=O)C2CCCCC2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.08.085
57394708 68294 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 459 6 2 6 3.7 Cc1nn(-c2ccc(F)cc2)c(NS(=O)(=O)c2cccnc2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.08.085
CHEMBL1916287 68294 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 459 6 2 6 3.7 Cc1nn(-c2ccc(F)cc2)c(NS(=O)(=O)c2cccnc2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.08.085
57396213 69569 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 420 6 2 5 4.0 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C(C)C)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934267 69569 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 420 6 2 5 4.0 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C(C)C)cc1 10.1016/j.bmcl.2011.10.090
57390868 69593 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 448 6 2 6 3.4 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCOC2)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934423 69593 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 448 6 2 6 3.4 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCOC2)cc1 10.1016/j.bmcl.2011.10.090
54580795 61474 None 0 Human Functional pIC50 = 6 6.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 424 8 2 6 4.6 CCOc1ccc2oc(C(=O)NC(CCSC)c3nc4cnccc4[nH]3)c(C)c2c1 10.1016/j.bmcl.2011.03.049
CHEMBL1770476 61474 None 0 Human Functional pIC50 = 6 6.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 424 8 2 6 4.6 CCOc1ccc2oc(C(=O)NC(CCSC)c3nc4cnccc4[nH]3)c(C)c2c1 10.1016/j.bmcl.2011.03.049
54580798 61480 None 0 Human Functional pIC50 = 6 6.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 391 7 2 4 5.3 CCC[C@H](NC(=O)c1oc2ccc(OCC)cc2c1C)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
CHEMBL1770484 61480 None 0 Human Functional pIC50 = 6 6.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 391 7 2 4 5.3 CCC[C@H](NC(=O)c1oc2ccc(OCC)cc2c1C)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
2528 3698 None 85 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at FPR1Antagonist activity at FPR1
ChEMBL 404 6 0 3 3.8 O=C1N(c2ccccc2)N(C(=O)C1CCS(=O)c1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.049
5342 3698 None 85 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at FPR1Antagonist activity at FPR1
ChEMBL 404 6 0 3 3.8 O=C1N(c2ccccc2)N(C(=O)C1CCS(=O)c1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.049
5826 3698 None 85 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at FPR1Antagonist activity at FPR1
ChEMBL 404 6 0 3 3.8 O=C1N(c2ccccc2)N(C(=O)C1CCS(=O)c1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.049
CHEMBL832 3698 None 85 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at FPR1Antagonist activity at FPR1
ChEMBL 404 6 0 3 3.8 O=C1N(c2ccccc2)N(C(=O)C1CCS(=O)c1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.049
DB01138 3698 None 85 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at FPR1Antagonist activity at FPR1
ChEMBL 404 6 0 3 3.8 O=C1N(c2ccccc2)N(C(=O)C1CCS(=O)c1ccccc1)c1ccccc1 10.1016/j.bmcl.2011.03.049
57394598 68248 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 446 7 2 5 3.9 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NCc3ccccc3)cnn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916086 68248 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 446 7 2 5 3.9 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NCc3ccccc3)cnn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
57401587 68265 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 440 6 2 6 2.9 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC3CCOCC3)cnn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916257 68265 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 440 6 2 6 2.9 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC3CCOCC3)cnn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
57394706 68271 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 426 8 2 5 3.9 CCC(CC)NC(=O)c1cn(-c2ccccc2)nc1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916263 68271 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 426 8 2 5 3.9 CCC(CC)NC(=O)c1cn(-c2ccccc2)nc1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
57401680 68272 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 460 8 2 5 4.6 CCC(CC)NC(=O)c1cnn(-c2ccccc2Cl)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916264 68272 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 460 8 2 5 4.6 CCC(CC)NC(=O)c1cnn(-c2ccccc2Cl)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
57403415 68276 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 392 8 2 5 3.5 CCC(CC)NC(=O)c1cnn(C(C)C)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916268 68276 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 392 8 2 5 3.5 CCC(CC)NC(=O)c1cnn(C(C)C)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
57397970 69589 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 510 6 2 7 3.2 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCS(=O)(=O)CC2)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934419 69589 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 510 6 2 7 3.2 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCS(=O)(=O)CC2)cc1 10.1016/j.bmcl.2011.10.090
54586641 61412 None 0 Human Functional pIC50 = 5 5.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 388 5 2 3 4.5 Cc1cccc(C)c1NC(=O)C(c1ccccc1)N(C)C(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
CHEMBL1770308 61412 None 0 Human Functional pIC50 = 5 5.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 388 5 2 3 4.5 Cc1cccc(C)c1NC(=O)C(c1ccccc1)N(C)C(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
24244526 61468 None 3 Human Functional pIC50 = 5 5.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 327 6 2 5 2.6 CSCCC(NC(=O)c1cnccn1)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
CHEMBL1770469 61468 None 3 Human Functional pIC50 = 5 5.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 327 6 2 5 2.6 CSCCC(NC(=O)c1cnccn1)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
54583762 61469 None 0 Human Functional pIC50 = 5 5.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 330 6 2 5 3.1 CSCCC(NC(=O)c1ocnc1C)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
CHEMBL1770470 61469 None 0 Human Functional pIC50 = 5 5.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 330 6 2 5 3.1 CSCCC(NC(=O)c1ocnc1C)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
5126271 61471 None 1 Human Functional pIC50 = 5 5.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 339 6 2 3 4.1 CSCCC(NC(=O)c1ccc(C)cc1)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
CHEMBL1770472 61471 None 1 Human Functional pIC50 = 5 5.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 339 6 2 3 4.1 CSCCC(NC(=O)c1ccc(C)cc1)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
54582778 61479 None 0 Human Functional pIC50 = 5 5.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 441 7 2 6 3.5 CCOc1ccc2oc(C(=O)NC(CS(C)(=O)=O)c3nc4ccccc4[nH]3)c(C)c2c1 10.1016/j.bmcl.2011.03.049
CHEMBL1770482 61479 None 0 Human Functional pIC50 = 5 5.0 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 441 7 2 6 3.5 CCOc1ccc2oc(C(=O)NC(CS(C)(=O)=O)c3nc4ccccc4[nH]3)c(C)c2c1 10.1016/j.bmcl.2011.03.049
155517073 170160 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL4444413 170160 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
155529906 171470 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 421 8 3 4 2.8 COC(=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1)C(C)C 10.1039/C9MD00336C
CHEMBL4463562 171470 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 421 8 3 4 2.8 COC(=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1)C(C)C 10.1039/C9MD00336C
57398260 68296 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 526 6 2 5 5.3 Cc1nn(-c2ccc(F)cc2)c(NS(=O)(=O)c2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.08.085
CHEMBL1916289 68296 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 526 6 2 5 5.3 Cc1nn(-c2ccc(F)cc2)c(NS(=O)(=O)c2ccc(C(F)(F)F)cc2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.08.085
71698276 173797 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 475 9 3 4 4.1 COC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL4538076 173797 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 475 9 3 4 4.1 COC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
57398258 68289 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 454 6 2 5 4.5 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC(C)C(C)(C)C)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916281 68289 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 454 6 2 5 4.5 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC(C)C(C)(C)C)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
3089940 61388 None 2 Human Functional pIC50 = 5.9 5.9 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 374 5 3 3 4.1 Cc1cccc(C)c1NC(=O)C(NC(=O)c1ccccc1O)c1ccccc1 10.1016/j.bmcl.2011.03.049
CHEMBL1770153 61388 None 2 Human Functional pIC50 = 5.9 5.9 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 374 5 3 3 4.1 Cc1cccc(C)c1NC(=O)C(NC(=O)c1ccccc1O)c1ccccc1 10.1016/j.bmcl.2011.03.049
92263206 174171 None 0 Human Functional pIC50 = 4.9 4.9 -1 2
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 465 8 3 5 3.5 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1039/C9MD00336C
CHEMBL4547265 174171 None 0 Human Functional pIC50 = 4.9 4.9 -1 2
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 465 8 3 5 3.5 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1039/C9MD00336C
118707168 113019 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of fMLP-induced calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 methodAntagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of fMLP-induced calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 method
ChEMBL 893 22 6 8 6.6 CC(C)C[C@@H](NC(=O)[C@H](CC1=CCCCC1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2014.06.048
CHEMBL3311300 113019 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of fMLP-induced calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 methodAntagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of fMLP-induced calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 method
ChEMBL 893 22 6 8 6.6 CC(C)C[C@@H](NC(=O)[C@H](CC1=CCCCC1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2014.06.048
155524563 170923 None 0 Human Functional pIC50 = 4.8 4.8 -1 2
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 435 9 3 4 3.2 COC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL4455225 170923 None 0 Human Functional pIC50 = 4.8 4.8 -1 2
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 435 9 3 4 3.2 COC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
168286767 191680 None 0 Human Functional pIC50 = 4.8 4.8 -53 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5196551 191680 None 0 Human Functional pIC50 = 4.8 4.8 -53 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
4329947 2499 None 1 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
5829 2499 None 1 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
CHEMBL1770297 2499 None 1 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
57392963 68285 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 466 6 2 5 4.6 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC3CCCCC3C)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916277 68285 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 466 6 2 5 4.6 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC3CCCCC3C)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
57399910 68288 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 426 7 2 5 3.8 CCC(C)NC(=O)c1c(C)nn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916280 68288 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 426 7 2 5 3.8 CCC(C)NC(=O)c1c(C)nn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
56949966 69595 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 488 7 2 6 4.4 Cc1nn(C2CCOCC2)c(NS(=O)(=O)c2ccc(C3CC3)cc2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.10.090
CHEMBL1934426 69595 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 488 7 2 6 4.4 Cc1nn(C2CCOCC2)c(NS(=O)(=O)c2ccc(C3CC3)cc2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.10.090
53233899 1410 None 0 Human Functional pIC50 = 5.8 5.8 69 2
Antagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assayAntagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
5830 1410 None 0 Human Functional pIC50 = 5.8 5.8 69 2
Antagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assayAntagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
CHEMBL1770298 1410 None 0 Human Functional pIC50 = 5.8 5.8 69 2
Antagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assayAntagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
57392872 68247 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 452 6 1 5 4.4 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N(C)C3CCCCC3)cnn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916085 68247 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 452 6 1 5 4.4 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N(C)C3CCCCC3)cnn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
57399908 68270 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 426 8 2 5 3.9 CCC(CC)NC(=O)c1ncn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916262 68270 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 426 8 2 5 3.9 CCC(CC)NC(=O)c1ncn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
57399672 69572 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 434 5 2 5 4.2 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C(C)(C)C)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934270 69572 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 434 5 2 5 4.2 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C(C)(C)C)cc1 10.1016/j.bmcl.2011.10.090
54581781 61407 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 378 5 3 5 2.9 Cc1cccc(C)c1NC(=O)C(NC(=O)c1ccccc1O)c1cn(C)cn1 10.1016/j.bmcl.2011.03.049
CHEMBL1770301 61407 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 378 5 3 5 2.9 Cc1cccc(C)c1NC(=O)C(NC(=O)c1ccccc1O)c1cn(C)cn1 10.1016/j.bmcl.2011.03.049
57396467 68273 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 451 8 2 6 3.8 CCC(CC)NC(=O)c1cnn(-c2ccc(C#N)cc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916265 68273 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 451 8 2 6 3.8 CCC(CC)NC(=O)c1cnn(-c2ccc(C#N)cc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL6997 215864 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None CSCC[C@H](NC(=O)Nc1cccc(C)c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
117993763 171602 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL4465341 171602 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
92263206 174171 None 0 Human Functional pIC50 = 4.8 4.8 -1 2
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 465 8 3 5 3.5 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1039/C9MD00336C
CHEMBL4547265 174171 None 0 Human Functional pIC50 = 4.8 4.8 -1 2
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 465 8 3 5 3.5 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C 10.1039/C9MD00336C
168281597 191268 None 0 Human Functional pIC50 = 4.8 4.8 -50 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.4 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5190571 191268 None 0 Human Functional pIC50 = 4.8 4.8 -50 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.4 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
164916036 191585 None 0 Human Functional pIC50 = 4.8 4.8 -147 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5195186 191585 None 0 Human Functional pIC50 = 4.8 4.8 -147 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
71697968 174569 None 21 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL4556626 174569 None 21 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
155510570 174029 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 449 10 3 4 3.1 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1039/C9MD00336C
CHEMBL4543372 174029 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 449 10 3 4 3.1 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1039/C9MD00336C
57401368 69583 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 432 6 2 5 4.2 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCC2)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934413 69583 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 432 6 2 5 4.2 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCC2)cc1 10.1016/j.bmcl.2011.10.090
57399796 68245 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 426 8 2 5 3.9 CCC(CC)NC(=O)c1cnn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916082 68245 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 426 8 2 5 3.9 CCC(CC)NC(=O)c1cnn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
57401684 68287 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 440 6 2 5 4.1 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NCC(C)(C)C)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916279 68287 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 440 6 2 5 4.1 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NCC(C)(C)C)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
54581826 61470 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 365 6 2 4 4.5 CSCCC(NC(=O)c1sccc1Cl)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
CHEMBL1770471 61470 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 365 6 2 4 4.5 CSCCC(NC(=O)c1sccc1Cl)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
57398252 68274 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 427 8 2 6 3.3 CCC(CC)NC(=O)c1cnn(-c2ccccn2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916266 68274 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 427 8 2 6 3.3 CCC(CC)NC(=O)c1cnn(-c2ccccn2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL7486 215872 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None Cc1cccc(NC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)O)c1 10.1021/jm950908d
CHEMBL3311030 211336 None 26 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of fMLP-induced calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 methodAntagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of fMLP-induced calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 method
ChEMBL None None None CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2014.06.048
10579232 203734 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL 586 14 5 5 3.7 CSCC[C@H](NC(=O)NC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
CHEMBL6779 203734 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL 586 14 5 5 3.7 CSCC[C@H](NC(=O)NC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
CHEMBL415299 213180 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None CSCC[C@H](NC(=O)NC(C)(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
CHEMBL7181 215867 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None CNC(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
168278228 191078 None 0 Human Functional pIC50 = 4.7 4.7 -3 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 394 5 2 3 3.4 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCCC2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5187530 191078 None 0 Human Functional pIC50 = 4.7 4.7 -3 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 394 5 2 3 3.4 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCCC2)cc1 10.1021/acs.jmedchem.1c02203
155517009 170153 None 0 Human Functional pIC50 = 5.6 5.6 3 2
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL4444320 170153 None 0 Human Functional pIC50 = 5.6 5.6 3 2
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
168279295 191044 None 0 Human Functional pIC50 = 4.6 4.6 -91 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.4 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5187135 191044 None 0 Human Functional pIC50 = 4.6 4.6 -91 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 442 5 2 3 4.4 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCc3ccccc32)cc1 10.1021/acs.jmedchem.1c02203
155524563 170923 None 0 Human Functional pIC50 = 4.6 4.6 -1 2
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 435 9 3 4 3.2 COC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL4455225 170923 None 0 Human Functional pIC50 = 4.6 4.6 -1 2
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 435 9 3 4 3.2 COC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
57403416 68292 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 508 6 2 5 5.2 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C(F)(F)F)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916284 68292 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 508 6 2 5 5.2 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C(F)(F)F)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
54752118 68295 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 483 6 2 6 4.2 Cc1nn(-c2ccc(F)cc2)c(NS(=O)(=O)c2ccc(C#N)cc2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.08.085
CHEMBL1916288 68295 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 483 6 2 6 4.2 Cc1nn(-c2ccc(F)cc2)c(NS(=O)(=O)c2ccc(C#N)cc2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.08.085
54752118 68295 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 483 6 2 6 4.2 Cc1nn(-c2ccc(F)cc2)c(NS(=O)(=O)c2ccc(C#N)cc2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.10.090
CHEMBL1916288 68295 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 483 6 2 6 4.2 Cc1nn(-c2ccc(F)cc2)c(NS(=O)(=O)c2ccc(C#N)cc2)c1C(=O)N[C@@H](C)C(C)(C)C 10.1016/j.bmcl.2011.10.090
CHEMBL1770296 208877 None 33 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at FPR1Antagonist activity at FPR1
ChEMBL None None None CSCC[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2011.03.049
57401370 69586 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 450 8 2 6 3.7 COCC(C)n1nc(C)c(C(=O)N[C@@H](C)C(C)(C)C)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934416 69586 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 450 8 2 6 3.7 COCC(C)n1nc(C)c(C(=O)N[C@@H](C)C(C)(C)C)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.10.090
4652862 47515 None 12 Human Functional pIC50 = 5.6 5.6 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 331 6 2 3 4.1 CSCCC(NC(=O)C1CCCCC1)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
CHEMBL1545798 47515 None 12 Human Functional pIC50 = 5.6 5.6 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 331 6 2 3 4.1 CSCCC(NC(=O)C1CCCCC1)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
54587661 61410 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 386 5 3 3 4.0 O=C(NC(C(=O)NC1CCCCC1)c1ccc(Cl)cc1)c1ccccc1O 10.1016/j.bmcl.2011.03.049
CHEMBL1770304 61410 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 386 5 3 3 4.0 O=C(NC(C(=O)NC1CCCCC1)c1ccc(Cl)cc1)c1ccccc1O 10.1016/j.bmcl.2011.03.049
54586640 61411 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 460 5 3 4 4.3 Cc1cccc(C)c1NC(=O)C(NC(=O)c1nc2ccccc2[nH]c1=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2011.03.049
CHEMBL1770307 61411 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 460 5 3 4 4.3 Cc1cccc(C)c1NC(=O)C(NC(=O)c1nc2ccccc2[nH]c1=O)c1ccc(Cl)cc1 10.1016/j.bmcl.2011.03.049
3825824 61472 None 12 Human Functional pIC50 = 5.6 5.6 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 415 8 1 4 5.3 CSCCC(NC(=O)c1ccccc1)c1nc2ccccc2n1Cc1ccccc1 10.1016/j.bmcl.2011.03.049
CHEMBL1770474 61472 None 12 Human Functional pIC50 = 5.6 5.6 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 415 8 1 4 5.3 CSCCC(NC(=O)c1ccccc1)c1nc2ccccc2n1Cc1ccccc1 10.1016/j.bmcl.2011.03.049
57403176 69568 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 406 8 2 5 3.8 CCC(CC)NC(=O)c1c(C)nn(C(C)C)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934266 69568 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 406 8 2 5 3.8 CCC(CC)NC(=O)c1c(C)nn(C(C)C)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.10.090
53233899 1410 None 0 Mouse Functional pIC50 = 4.6 4.6 -69 2
Antagonist activity at mouse FPR1 expressed in HEK293 cells assessed as inhibition of fMLFF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at mouse FPR1 expressed in HEK293 cells assessed as inhibition of fMLFF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
5830 1410 None 0 Mouse Functional pIC50 = 4.6 4.6 -69 2
Antagonist activity at mouse FPR1 expressed in HEK293 cells assessed as inhibition of fMLFF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at mouse FPR1 expressed in HEK293 cells assessed as inhibition of fMLFF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
CHEMBL1770298 1410 None 0 Mouse Functional pIC50 = 4.6 4.6 -69 2
Antagonist activity at mouse FPR1 expressed in HEK293 cells assessed as inhibition of fMLFF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at mouse FPR1 expressed in HEK293 cells assessed as inhibition of fMLFF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
155529906 171470 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 421 8 3 4 2.8 COC(=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1)C(C)C 10.1039/C9MD00336C
CHEMBL4463562 171470 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 421 8 3 4 2.8 COC(=O)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1)C(C)C 10.1039/C9MD00336C
168280238 190952 None 0 Human Functional pIC50 = 4.6 4.6 -6 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2Cc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5185921 190952 None 0 Human Functional pIC50 = 4.6 4.6 -6 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 428 5 2 3 4.0 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2Cc3ccccc3C2)cc1 10.1021/acs.jmedchem.1c02203
155510570 174029 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 449 10 3 4 3.1 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1039/C9MD00336C
CHEMBL4543372 174029 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 449 10 3 4 3.1 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CC(C)C 10.1039/C9MD00336C
56949822 69594 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 490 7 2 6 4.6 CO[C@H]1CC[C@@H](n2nc(C)c(C(=O)N[C@@H](C)C(C)(C)C)c2NS(=O)(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2011.10.090
CHEMBL1934424 69594 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 490 7 2 6 4.6 CO[C@H]1CC[C@@H](n2nc(C)c(C(=O)N[C@@H](C)C(C)(C)C)c2NS(=O)(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2011.10.090
9988173 161914 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL 862 21 7 6 5.5 CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)NC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
CHEMBL415296 161914 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL 862 21 7 6 5.5 CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)NC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
CHEMBL266448 210682 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None CCCNC(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
CHEMBL7214 215868 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None CCNC(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
168278342 191149 None 0 Human Functional pIC50 = 4.5 4.5 1 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 394 5 2 3 3.4 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCCC2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5188537 191149 None 0 Human Functional pIC50 = 4.5 4.5 1 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 394 5 2 3 3.4 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCCC2)cc1 10.1021/acs.jmedchem.1c02203
57390867 69585 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 460 6 2 5 5.0 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCCCC2)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934415 69585 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 460 6 2 5 5.0 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCCCC2)cc1 10.1016/j.bmcl.2011.10.090
117993763 171602 None 0 Human Functional pIC50 = 4.5 4.5 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL4465341 171602 None 0 Human Functional pIC50 = 4.5 4.5 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
57392882 68264 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 440 9 2 5 4.3 CCCC(CC)NC(=O)c1cnn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916255 68264 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 440 9 2 5 4.3 CCCC(CC)NC(=O)c1cnn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
57394389 69587 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 464 9 2 6 4.1 COCCC(C)n1nc(C)c(C(=O)N[C@@H](C)C(C)(C)C)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934417 69587 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 464 9 2 6 4.1 COCCC(C)n1nc(C)c(C(=O)N[C@@H](C)C(C)(C)C)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.10.090
57396150 69592 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 462 6 2 6 3.8 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCOCC2)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934422 69592 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 462 6 2 6 3.8 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCOCC2)cc1 10.1016/j.bmcl.2011.10.090
53233899 1410 None 0 Human Functional pIC50 = 6.5 6.5 69 2
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
5830 1410 None 0 Human Functional pIC50 = 6.5 6.5 69 2
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
CHEMBL1770298 1410 None 0 Human Functional pIC50 = 6.5 6.5 69 2
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
3939767 61473 None 3 Human Functional pIC50 = 6.5 6.5 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 440 8 1 5 5.2 CSCCC(NC(=O)c1ccccc1)c1nc2ccccc2n1Cc1ccc(C#N)cc1 10.1016/j.bmcl.2011.03.049
CHEMBL1770475 61473 None 3 Human Functional pIC50 = 6.5 6.5 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 440 8 1 5 5.2 CSCCC(NC(=O)c1ccccc1)c1nc2ccccc2n1Cc1ccc(C#N)cc1 10.1016/j.bmcl.2011.03.049
4329947 2499 None 1 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assayAntagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
5829 2499 None 1 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assayAntagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
CHEMBL1770297 2499 None 1 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assayAntagonist activity at human FPR1 in expressed in HEK293 cells assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation after 5 mins by FLIPR assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
57398257 68283 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 466 6 1 5 4.7 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N(C)C3CCCCC3)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916275 68283 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 466 6 1 5 4.7 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N(C)C3CCCCC3)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
57392729 69571 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 460 6 2 5 4.0 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2CC(F)(F)F)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934269 69571 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 460 6 2 5 4.0 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2CC(F)(F)F)cc1 10.1016/j.bmcl.2011.10.090
57399614 69591 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 543 7 2 6 4.7 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCN(CC(F)(F)F)CC2)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934421 69591 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 543 7 2 6 4.7 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCN(CC(F)(F)F)CC2)cc1 10.1016/j.bmcl.2011.10.090
54584753 61475 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 424 8 2 6 4.6 CCOc1ccc2oc(C(=O)NC(CCSC)c3nc4ncccc4[nH]3)c(C)c2c1 10.1016/j.bmcl.2011.03.049
CHEMBL1770477 61475 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 424 8 2 6 4.6 CCOc1ccc2oc(C(=O)NC(CCSC)c3nc4ncccc4[nH]3)c(C)c2c1 10.1016/j.bmcl.2011.03.049
155523344 170739 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 475 9 3 4 3.7 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCC1 10.1039/C9MD00336C
CHEMBL4452346 170739 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 in human neutrophils assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 475 9 3 4 3.7 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1CCCCC1 10.1039/C9MD00336C
168283359 190810 None 0 Human Functional pIC50 = 4.5 4.5 -5 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 5 2 3 3.1 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCC2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5183856 190810 None 0 Human Functional pIC50 = 4.5 4.5 -5 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 5 2 3 3.1 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCC2)cc1 10.1021/acs.jmedchem.1c02203
164916034 191688 None 0 Human Functional pIC50 = 5.5 5.5 -6 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 437 6 4 4 2.2 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)NC2CCCCNC2=O)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5196771 191688 None 0 Human Functional pIC50 = 5.5 5.5 -6 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 437 6 4 4 2.2 N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)NC2CCCCNC2=O)cc1 10.1021/acs.jmedchem.1c02203
155517073 170160 None 0 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL4444413 170160 None 0 Human Functional pIC50 = 4.4 4.4 - 1
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
57396149 69588 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 478 6 2 6 4.5 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCSCC2)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934418 69588 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 478 6 2 6 4.5 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@@H](C)C(C)(C)C)c(C)nn2C2CCSCC2)cc1 10.1016/j.bmcl.2011.10.090
53233899 1410 None 0 Human Functional pIC50 = 6.4 6.4 69 2
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
5830 1410 None 0 Human Functional pIC50 = 6.4 6.4 69 2
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
CHEMBL1770298 1410 None 0 Human Functional pIC50 = 6.4 6.4 69 2
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
53233899 1410 None 0 Human Functional pIC50 = 6.4 6.4 69 2
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
5830 1410 None 0 Human Functional pIC50 = 6.4 6.4 69 2
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
CHEMBL1770298 1410 None 0 Human Functional pIC50 = 6.4 6.4 69 2
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated degranulation after 15 mins by fluorescence assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.03.049
53233899 1410 None 0 Human Functional pIC50 = 6.4 6.4 69 2
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.08.085
5830 1410 None 0 Human Functional pIC50 = 6.4 6.4 69 2
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.08.085
CHEMBL1770298 1410 None 0 Human Functional pIC50 = 6.4 6.4 69 2
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 394 5 3 4 4.5 Cc1ccc(s1)C(C(=O)Nc1c(C)cccc1C)NC(=O)c1ccccc1O 10.1016/j.bmcl.2011.08.085
57396214 69573 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 448 8 2 5 4.8 CCC(CC)n1nc(C)c(C(=O)N[C@@H](C)C(C)(C)C)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.10.090
CHEMBL1934271 69573 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assayAntagonist activity at human recombinant FPR1 in expressed in HEK293 cells assessed as inhibition of FMLP-stimulated intracellular calcium mobilisation after 1 hr by FLIPR assay
ChEMBL 448 8 2 5 4.8 CCC(CC)n1nc(C)c(C(=O)N[C@@H](C)C(C)(C)C)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.10.090
57392871 68246 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 438 6 2 5 4.0 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC3CCCCC3)cnn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916084 68246 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 438 6 2 5 4.0 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC3CCCCC3)cnn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
57394609 68269 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 427 8 2 6 3.3 CCC(CC)NC(=O)c1nnn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916261 68269 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 427 8 2 6 3.3 CCC(CC)NC(=O)c1nnn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
4881668 61413 None 6 Human Functional pIC50 = 5.4 5.4 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 379 6 2 4 4.8 CSCCC(NC(=O)c1oc2ccccc2c1C)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
CHEMBL1770309 61413 None 6 Human Functional pIC50 = 5.4 5.4 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 379 6 2 4 4.8 CSCCC(NC(=O)c1oc2ccccc2c1C)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
47012371 61415 None 5 Human Functional pIC50 = 5.4 5.4 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 329 6 2 4 3.7 CSCCC(NC(=O)c1occc1C)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
CHEMBL1770310 61415 None 5 Human Functional pIC50 = 5.4 5.4 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 329 6 2 4 3.7 CSCCC(NC(=O)c1occc1C)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
54584752 61467 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 341 6 3 4 3.5 CSCCC(NC(=O)c1ccccc1O)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
CHEMBL1770468 61467 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 341 6 3 4 3.5 CSCCC(NC(=O)c1ccccc1O)c1nc2ccccc2[nH]1 10.1016/j.bmcl.2011.03.049
CHEMBL268823 210766 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None CSCC[C@H](NC(=O)NCC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
168273654 190324 None 0 Human Functional pIC50 = 4.4 4.4 -6 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 437 6 4 4 2.2 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)NC2CCCCNC2=O)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5176452 190324 None 0 Human Functional pIC50 = 4.4 4.4 -6 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 437 6 4 4 2.2 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)NC2CCCCNC2=O)cc1 10.1021/acs.jmedchem.1c02203
102234371 113002 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of fMLP-induced calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 methodAntagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of fMLP-induced calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 method
ChEMBL 889 22 6 8 6.0 CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2014.06.048
CHEMBL3311137 113002 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of fMLP-induced calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 methodAntagonist activity at formyl peptide receptor in human HL60 cells assessed as inhibition of fMLP-induced calcium mobilization incubated for 5 mins prior to fMLP challenge by Fura-2 method
ChEMBL 889 22 6 8 6.0 CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(C(=O)c2ccccc2)cc1)NC(=O)OC(C)(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2014.06.048
168283383 190842 None 0 Human Functional pIC50 = 4.4 4.4 -3 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 5 2 3 3.1 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCC2)cc1 10.1021/acs.jmedchem.1c02203
CHEMBL5184396 190842 None 0 Human Functional pIC50 = 4.4 4.4 -3 2
Antagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAntagonist activity at human FPR1 transfected in human HL-60 cells assessed as inhibition of fMLF-induced intracellular calcium mobilization preincubated for 10 mins followed by fMLF addition and measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay
ChEMBL 380 5 2 3 3.1 N#Cc1ccc(C[C@@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCC2)cc1 10.1021/acs.jmedchem.1c02203
71697968 174569 None 21 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL4556626 174569 None 21 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometryAntagonist activity against FPR1 (unknown origin) transfected in human HL60 cells assessed as calcium mobilization preincubated for 30 mins followed by fMLF addition and measured for 5 sec for 240 sec by fluorometry
ChEMBL 469 9 3 4 3.4 COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)c1ccccc1 10.1039/C9MD00336C
CHEMBL162488 208808 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)Nc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
CHEMBL7122 215866 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)NC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
CHEMBL7034 215865 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophilsAntagonistic activity was determined by measuring the ability to inhibit superoxide production (stimulated by fMLF) using human neutrophils
ChEMBL None None None CSCC[C@H](NC(=O)NC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm950908d
4329947 2499 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
5829 2499 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
CHEMBL1770297 2499 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assayAntagonist activity at FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated calcium mobilization by FLIPR assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
4329947 2499 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.08.085
5829 2499 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.08.085
CHEMBL1770297 2499 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.08.085
57401682 68280 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 440 8 2 5 4.2 CCC(CC)NC(=O)c1c(C)nn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916272 68280 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 440 8 2 5 4.2 CCC(CC)NC(=O)c1c(C)nn(-c2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
57396468 68291 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 454 6 2 5 4.5 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@H](C)C(C)(C)C)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916283 68291 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 454 6 2 5 4.5 Cc1ccc(S(=O)(=O)Nc2c(C(=O)N[C@H](C)C(C)(C)C)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
4329947 2499 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
5829 2499 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
CHEMBL1770297 2499 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Intrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLFIntrinsic activity at FPR1 in human neutrophils assessed as increase in calcium mobilization by FLIPR assay relative to fMLF
ChEMBL 423 8 2 5 5.2 CSCCC(c1nc2c([nH]1)cccc2)NC(=O)c1oc2c(c1C)cc(cc2)OCC 10.1016/j.bmcl.2011.03.049
5322194 1863 None 10 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at FPR1Antagonist activity at FPR1
ChEMBL 376 3 1 5 2.3 CC(C(N1C(=S)S/C(=C\2/c3ccccc3N(C2=O)C)/C1=O)C(=O)O)C 10.1016/j.bmcl.2011.03.049
5827 1863 None 10 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at FPR1Antagonist activity at FPR1
ChEMBL 376 3 1 5 2.3 CC(C(N1C(=S)S/C(=C\2/c3ccccc3N(C2=O)C)/C1=O)C(=O)O)C 10.1016/j.bmcl.2011.03.049
CHEMBL1770295 1863 None 10 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at FPR1Antagonist activity at FPR1
ChEMBL 376 3 1 5 2.3 CC(C(N1C(=S)S/C(=C\2/c3ccccc3N(C2=O)C)/C1=O)C(=O)O)C 10.1016/j.bmcl.2011.03.049
57398165 68267 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 412 8 2 5 3.6 CCC(CC)NC(=O)c1cnn(-c2ccccc2)c1NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916259 68267 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 412 8 2 5 3.6 CCC(CC)NC(=O)c1cnn(-c2ccccc2)c1NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2011.08.085
57398166 68268 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 404 8 2 5 3.5 CCC(CC)NC(=O)c1cnn(-c2ccccc2)c1NS(=O)(=O)C1CCCC1 10.1016/j.bmcl.2011.08.085
CHEMBL1916260 68268 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 404 8 2 5 3.5 CCC(CC)NC(=O)c1cnn(-c2ccccc2)c1NS(=O)(=O)C1CCCC1 10.1016/j.bmcl.2011.08.085
57398253 68275 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 440 9 2 5 4.0 CCC(CC)NC(=O)c1cnn(Cc2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916267 68275 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 440 9 2 5 4.0 CCC(CC)NC(=O)c1cnn(Cc2ccccc2)c1NS(=O)(=O)c1ccc(C)cc1 10.1016/j.bmcl.2011.08.085
57398255 68278 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 479 9 2 7 4.2 CCC(CC)NC(=O)c1cnn(-c2ccccc2)c1NS(=O)(=O)c1ccc(-c2cnco2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916270 68278 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 479 9 2 7 4.2 CCC(CC)NC(=O)c1cnn(-c2ccccc2)c1NS(=O)(=O)c1ccc(-c2cnco2)cc1 10.1016/j.bmcl.2011.08.085
57392964 68286 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 454 6 2 6 3.2 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC3CCOCC3)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
CHEMBL1916278 68286 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at human FPR1 in human neutrophils assessed as inhibition of fMLF-stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 454 6 2 6 3.2 Cc1ccc(S(=O)(=O)Nc2c(C(=O)NC3CCOCC3)c(C)nn2-c2ccccc2)cc1 10.1016/j.bmcl.2011.08.085
54581782 61409 None 0 Human Functional pIC50 = 5.3