Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
8498 3263 46 None -33 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxisAntagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxis
ChEMBL 283 5 1 3 2.1 CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C 10.1021/jm300682j
9838712 3263 46 None -33 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxisAntagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxis
ChEMBL 283 5 1 3 2.1 CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C 10.1021/jm300682j
CHEMBL191413 3263 46 None -33 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxisAntagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxis
ChEMBL 283 5 1 3 2.1 CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C 10.1021/jm300682j
DB12614 3263 46 None -33 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxisAntagonist activity at CXCR2 assessed as inhibition of CXCL8-induced neutrophil chemotaxis
ChEMBL 283 5 1 3 2.1 CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C 10.1021/jm300682j
135907804 112461 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 363 5 2 6 2.8 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1[C@H]1C[C@@H]1C(=O)O 10.1016/j.bmcl.2014.06.011
CHEMBL3310786 112461 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 363 5 2 6 2.8 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1[C@H]1C[C@@H]1C(=O)O 10.1016/j.bmcl.2014.06.011
8497 2697 52 None 1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 10.1021/acsmedchemlett.1c00113
9865554 2697 52 None 1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 10.1021/acsmedchemlett.1c00113
CHEMBL216981 2697 52 None 1 3 Human 8.0 pIC50 = 8 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 10.1021/acsmedchemlett.1c00113
162646828 179030 0 None 912 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 413 4 3 6 3.1 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@@H](C3CCCCC3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4742368 179030 0 None 912 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 413 4 3 6 3.1 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@@H](C3CCCCC3)N2)c1O 10.1021/acsmedchemlett.1c00113
45485775 196008 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 424 8 3 8 2.3 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccc(OC)cc1 10.1016/j.bmcl.2009.08.014
CHEMBL571141 196008 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 424 8 3 8 2.3 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccc(OC)cc1 10.1016/j.bmcl.2009.08.014
24970094 126290 0 None - 1 Human 6.0 pIC50 = 6 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 397 8 2 4 3.6 CC(C)(NC(=O)c1ccc2c(c1OCCOc1ccccc1)CCCC2)C(=O)O nan
CHEMBL3654434 126290 0 None - 1 Human 6.0 pIC50 = 6 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 397 8 2 4 3.6 CC(C)(NC(=O)c1ccc2c(c1OCCOc1ccccc1)CCCC2)C(=O)O nan
136074345 112467 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 319 4 1 5 3.5 N#Cc1c(O)nc(CSc2cccc(F)c2F)nc1C1CC1 10.1016/j.bmcl.2014.06.011
CHEMBL3310793 112467 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 319 4 1 5 3.5 N#Cc1c(O)nc(CSc2cccc(F)c2F)nc1C1CC1 10.1016/j.bmcl.2014.06.011
CHEMBL5083610 213102 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccccc1F)Nc1ccc2c(c1O)S(=O)(=O)CCC2 10.1021/acs.jmedchem.1c01219
1485055 35194 21 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 271 3 1 5 3.0 Cc1cc2nc(CSc3ccccc3)cc(O)n2n1 10.1016/j.bmcl.2013.11.074
CHEMBL1437942 35194 21 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 271 3 1 5 3.0 Cc1cc2nc(CSc3ccccc3)cc(O)n2n1 10.1016/j.bmcl.2013.11.074
91937331 114431 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 380 6 4 6 2.0 O=C(Nc1ccc(O)cc1)c1ccc(SCc2ccccc2B(O)O)nc1 10.1021/jm500827t
CHEMBL3342318 114431 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 380 6 4 6 2.0 O=C(Nc1ccc(O)cc1)c1ccc(SCc2ccccc2B(O)O)nc1 10.1021/jm500827t
CHEMBL5076384 212663 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=c1c(Nc2ccccc2Cl)c(Nc2ccc3c(c2O)S(=O)(=O)CCC3)c1=O 10.1021/acs.jmedchem.1c01219
72948072 104153 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 319 5 1 5 2.3 COc1cc(CCc2cccc(F)c2F)nc2cc(CO)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3104898 104153 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 319 5 1 5 2.3 COc1cc(CCc2cccc(F)c2F)nc2cc(CO)nn12 10.1016/j.bmcl.2013.11.074
56839294 122491 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 379 6 3 5 1.8 CN(Cc1ccc(B(O)O)cc1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
CHEMBL3609005 122491 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 379 6 3 5 1.8 CN(Cc1ccc(B(O)O)cc1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
11222420 86304 0 None 40 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 368 2 3 7 2.5 O=[N+]([O-])c1cc(O)c2c(c1)S(=O)(=O)N=C(Nc1ccccc1Cl)N2 10.1016/j.bmcl.2007.05.011
CHEMBL231924 86304 0 None 40 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 368 2 3 7 2.5 O=[N+]([O-])c1cc(O)c2c(c1)S(=O)(=O)N=C(Nc1ccccc1Cl)N2 10.1016/j.bmcl.2007.05.011
66856548 104154 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 305 4 2 5 2.0 OCc1cc2nc(CCc3cccc(F)c3F)cc(O)n2n1 10.1016/j.bmcl.2013.11.074
CHEMBL3104899 104154 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 305 4 2 5 2.0 OCc1cc2nc(CCc3cccc(F)c3F)cc(O)n2n1 10.1016/j.bmcl.2013.11.074
72947877 104157 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 431 6 1 8 4.8 Oc1cc(CSc2nc(-c3ccccc3)cs2)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3104904 104157 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 431 6 1 8 4.8 Oc1cc(CSc2nc(-c3ccccc3)cs2)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
72948068 104159 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 408 7 1 8 3.7 COc1ccc(SCc2cc(O)n3nc(Cc4ccccc4)nc3n2)c(OC)c1 10.1016/j.bmcl.2013.11.074
CHEMBL3104906 104159 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 408 7 1 8 3.7 COc1ccc(SCc2cc(O)n3nc(Cc4ccccc4)nc3n2)c(OC)c1 10.1016/j.bmcl.2013.11.074
56839499 122496 0 None 5 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 380 6 3 6 1.2 CN(Cc1ccc(B(O)O)cc1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
CHEMBL3609011 122496 0 None 5 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 380 6 3 6 1.2 CN(Cc1ccc(B(O)O)cc1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
45485756 196724 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 360 6 3 7 0.6 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)C(C)=O 10.1016/j.bmcl.2009.08.014
CHEMBL576886 196724 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 360 6 3 7 0.6 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)C(C)=O 10.1016/j.bmcl.2009.08.014
24769501 124656 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 445 8 2 4 4.7 CC(C)(NC(=O)c1ccc2ccccc2c1OCCOc1ccc(F)c(Cl)c1)C(=O)O nan
CHEMBL3645133 124656 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 445 8 2 4 4.7 CC(C)(NC(=O)c1ccc2ccccc2c1OCCOc1ccc(F)c(Cl)c1)C(=O)O nan
9887803 140306 22 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL 409 3 4 4 3.6 NS(=O)(=O)c1c(Cl)ccc(NC(=O)Nc2cccc(Cl)c2Cl)c1O 10.1021/acs.jmedchem.1c01219
CHEMBL3819292 140306 22 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL 409 3 4 4 3.6 NS(=O)(=O)c1c(Cl)ccc(NC(=O)Nc2cccc(Cl)c2Cl)c1O 10.1021/acs.jmedchem.1c01219
CHEMBL5089441 213434 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccc2c(c1O)S(=O)(=O)CC=C2)Nc1cccc(Cl)c1Cl 10.1021/acs.jmedchem.1c01219
136074340 112460 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 391 6 1 7 3.3 CCOC(=O)[C@H]1C[C@@H]1c1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
CHEMBL3310785 112460 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 391 6 1 7 3.3 CCOC(=O)[C@H]1C[C@@H]1c1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
44447928 95169 0 None -30 2 Rabbit 5.9 pIC50 = 5.9 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 414 7 3 4 2.7 CNS(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
CHEMBL257829 95169 0 None -30 2 Rabbit 5.9 pIC50 = 5.9 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 414 7 3 4 2.7 CNS(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
72947878 104158 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 374 5 1 8 3.0 N#Cc1cccnc1SCc1cc(O)n2nc(Cc3ccccc3)nc2n1 10.1016/j.bmcl.2013.11.074
CHEMBL3104905 104158 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 374 5 1 8 3.0 N#Cc1cccnc1SCc1cc(O)n2nc(Cc3ccccc3)nc2n1 10.1016/j.bmcl.2013.11.074
CHEMBL5078087 212764 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None Cc1ccc(NC(=O)Nc2ccc3c(c2O)S(=O)(=O)CCC3)cc1 10.1021/acs.jmedchem.1c01219
CHEMBL5083848 213116 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None Cc1c(F)cccc1Nc1c(Nc2ccc3c(c2O)S(=O)(=O)CCC3)c(=O)c1=O 10.1021/acs.jmedchem.1c01219
72948073 104152 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 461 7 1 7 3.7 CS(=O)(=O)Nc1cc(CSc2cccc(F)c2F)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3104897 104152 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 461 7 1 7 3.7 CS(=O)(=O)Nc1cc(CSc2cccc(F)c2F)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
44447928 95169 0 None 30 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 414 7 3 4 2.7 CNS(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
CHEMBL257829 95169 0 None 30 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 414 7 3 4 2.7 CNS(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
135907764 112458 12 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 319 4 1 5 3.5 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1C1CC1 10.1016/j.bmcl.2014.06.011
CHEMBL3310783 112458 12 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 319 4 1 5 3.5 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1C1CC1 10.1016/j.bmcl.2014.06.011
CHEMBL5088825 213406 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccccc1Br)Nc1ccc2c(c1O)S(=O)(=O)CCC2 10.1021/acs.jmedchem.1c01219
162652088 179681 0 None 707 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 359 4 3 6 1.9 CCC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
CHEMBL4750465 179681 0 None 707 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 359 4 3 6 1.9 CCC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
135907767 112447 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 369 4 1 5 4.6 Cc1ccc(-c2nc(SCc3cccc(F)c3F)nc(O)c2C#N)cc1 10.1016/j.bmcl.2014.06.011
CHEMBL3310773 112447 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 369 4 1 5 4.6 Cc1ccc(-c2nc(SCc3cccc(F)c3F)nc(O)c2C#N)cc1 10.1016/j.bmcl.2014.06.011
136986993 112555 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 372 4 1 4 4.4 Oc1nc(SCc2cccc(F)c2F)nc(C2CC2)c1Br 10.1016/j.bmcl.2014.06.011
CHEMBL3311396 112555 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 372 4 1 4 4.4 Oc1nc(SCc2cccc(F)c2F)nc(C2CC2)c1Br 10.1016/j.bmcl.2014.06.011
24970093 126289 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 387 7 2 3 4.5 CC(C)(NC(=O)c1ccc2c(c1OCCC1CCCCC1)CCCC2)C(=O)O nan
CHEMBL3654433 126289 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 387 7 2 3 4.5 CC(C)(NC(=O)c1ccc2c(c1OCCC1CCCCC1)CCCC2)C(=O)O nan
10268984 79904 2 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of chemotaxis of CHO cells expressing human CXCR2Inhibition of chemotaxis of CHO cells expressing human CXCR2
ChEMBL 343 3 3 6 1.5 CN(C)C(=O)c1cccc(/N=c2\c(O)c(O)\c2=N/C2CCCC2)c1O 10.1016/j.bmcl.2006.04.082
CHEMBL214162 79904 2 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of chemotaxis of CHO cells expressing human CXCR2Inhibition of chemotaxis of CHO cells expressing human CXCR2
ChEMBL 343 3 3 6 1.5 CN(C)C(=O)c1cccc(/N=c2\c(O)c(O)\c2=N/C2CCCC2)c1O 10.1016/j.bmcl.2006.04.082
46897449 114426 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 382 6 2 4 4.5 O=C(Nc1ccc(F)cc1)c1ccc(SCc2ccccc2C(=O)O)nc1 10.1021/jm500827t
CHEMBL3342311 114426 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 382 6 2 4 4.5 O=C(Nc1ccc(F)cc1)c1ccc(SCc2ccccc2C(=O)O)nc1 10.1021/jm500827t
CHEMBL5076418 212668 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccc(Br)cc1)Nc1ccc2c(c1O)S(=O)(=O)CC=C2 10.1021/acs.jmedchem.1c01219
151755055 173166 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at CXCR2 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at CXCR2 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 392 5 3 6 3.8 CC(C)S(=O)(=O)c1c(Cl)ccc(Nc2nnc(-c3ccccc3)[nH]2)c1O 10.1016/j.ejmech.2019.111853
CHEMBL4536494 173166 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at CXCR2 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at CXCR2 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 392 5 3 6 3.8 CC(C)S(=O)(=O)c1c(Cl)ccc(Nc2nnc(-c3ccccc3)[nH]2)c1O 10.1016/j.ejmech.2019.111853
162657065 180319 0 None 1548 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 522 7 4 8 3.4 CC(C)(C)OC(=O)NCCCS(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4757674 180319 0 None 1548 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 522 7 4 8 3.4 CC(C)(C)OC(=O)NCCCS(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3)N2)c1O 10.1021/acsmedchemlett.1c00113
11625425 139934 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity against human CXCR2 in neutrophils assessed as blockade of GROalpha stimulated calcium mobilisation by FLIPRAntagonistic activity against human CXCR2 in neutrophils assessed as blockade of GROalpha stimulated calcium mobilisation by FLIPR
ChEMBL 397 6 3 8 3.4 CC(C)(CO)Nc1nc(SCc2cccc(F)c2F)nc2nc(N)sc12 10.1016/j.bmcl.2007.02.080
CHEMBL380947 139934 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity against human CXCR2 in neutrophils assessed as blockade of GROalpha stimulated calcium mobilisation by FLIPRAntagonistic activity against human CXCR2 in neutrophils assessed as blockade of GROalpha stimulated calcium mobilisation by FLIPR
ChEMBL 397 6 3 8 3.4 CC(C)(CO)Nc1nc(SCc2cccc(F)c2F)nc2nc(N)sc12 10.1016/j.bmcl.2007.02.080
CHEMBL5090244 213477 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=c1c(Nc2ccccc2Br)c(Nc2ccc3c(c2O)S(=O)(=O)CCC3)c1=O 10.1021/acs.jmedchem.1c01219
24953463 104174 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 359 4 1 6 4.3 Oc1cc(CSc2cccc(F)c2F)nc2cc(-c3ccco3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3105080 104174 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 359 4 1 6 4.3 Oc1cc(CSc2cccc(F)c2F)nc2cc(-c3ccco3)nn12 10.1016/j.bmcl.2013.11.074
136074340 112460 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 391 6 1 7 3.3 CCOC(=O)[C@H]1C[C@@H]1c1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
CHEMBL3310785 112460 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 391 6 1 7 3.3 CCOC(=O)[C@H]1C[C@@H]1c1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
24958572 103909 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 308 3 1 6 2.7 Cc1nc2nc(CSc3cccc(F)c3F)cc(O)n2n1 10.1016/j.bmcl.2013.11.074
CHEMBL3102879 103909 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 308 3 1 6 2.7 Cc1nc2nc(CSc3cccc(F)c3F)cc(O)n2n1 10.1016/j.bmcl.2013.11.074
151755055 173166 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 392 5 3 6 3.8 CC(C)S(=O)(=O)c1c(Cl)ccc(Nc2nnc(-c3ccccc3)[nH]2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4536494 173166 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 392 5 3 6 3.8 CC(C)S(=O)(=O)c1c(Cl)ccc(Nc2nnc(-c3ccccc3)[nH]2)c1O 10.1021/acsmedchemlett.1c00113
135907774 112449 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 413 6 1 6 5.1 CC(C)Oc1ccc(-c2nc(SCc3cccc(F)c3F)nc(O)c2C#N)cc1 10.1016/j.bmcl.2014.06.011
CHEMBL3310775 112449 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 413 6 1 6 5.1 CC(C)Oc1ccc(-c2nc(SCc3cccc(F)c3F)nc(O)c2C#N)cc1 10.1016/j.bmcl.2014.06.011
CHEMBL5081113 212951 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccccc1C(F)(F)F)Nc1ccc2c(c1O)S(=O)(=O)CC=C2 10.1021/acs.jmedchem.1c01219
46897452 114422 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 406 5 1 3 6.1 O=C(Nc1ccc(F)cc1)c1ccc(SCc2ccc(Cl)c(Cl)c2)nc1 10.1021/jm500827t
CHEMBL3342303 114422 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 406 5 1 3 6.1 O=C(Nc1ccc(F)cc1)c1ccc(SCc2ccc(Cl)c(Cl)c2)nc1 10.1021/jm500827t
CHEMBL5086977 213286 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None Cc1c(Cl)cccc1NC(=O)Nc1ccc2c(c1O)S(=O)(=O)CC=C2 10.1021/acs.jmedchem.1c01219
57864041 124658 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 399 6 2 2 4.8 CC(C)(NC(=O)c1ccc2ccccc2c1C#CCCCc1ccccc1)C(=O)O nan
CHEMBL3645135 124658 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 399 6 2 2 4.8 CC(C)(NC(=O)c1ccc2ccccc2c1C#CCCCc1ccccc1)C(=O)O nan
46897451 114427 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 406 6 2 6 3.9 O=C(Nc1ccc(F)cc1)c1ccc(SCc2ccccc2-c2nn[nH]n2)nc1 10.1021/jm500827t
CHEMBL3342312 114427 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 406 6 2 6 3.9 O=C(Nc1ccc(F)cc1)c1ccc(SCc2ccccc2-c2nn[nH]n2)nc1 10.1021/jm500827t
135907781 112457 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 333 4 1 5 3.9 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1C1CCC1 10.1016/j.bmcl.2014.06.011
CHEMBL3310782 112457 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 333 4 1 5 3.9 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1C1CCC1 10.1016/j.bmcl.2014.06.011
24959296 104164 2 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 416 5 1 6 5.0 Oc1cc(CSc2cccc(Cl)c2Cl)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3104911 104164 2 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 416 5 1 6 5.0 Oc1cc(CSc2cccc(Cl)c2Cl)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
24958938 104166 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 384 5 1 6 4.0 Oc1cc(CSc2ccc(F)c(F)c2)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3104913 104166 4 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 384 5 1 6 4.0 Oc1cc(CSc2ccc(F)c(F)c2)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
68603807 104177 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 347 3 1 5 3.9 Oc1cc(CSc2cccc(F)c2F)nc2c3c(nn12)CCCC3 10.1016/j.bmcl.2013.11.074
CHEMBL3105083 104177 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 347 3 1 5 3.9 Oc1cc(CSc2cccc(F)c2F)nc2c3c(nn12)CCCC3 10.1016/j.bmcl.2013.11.074
44447946 94553 0 None -77 2 Rabbit 5.8 pIC50 = 5.8 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 515 6 3 3 5.0 O=C(NCCc1c(-c2ccc(F)cc2)[nH]c2ccc(Br)cc12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.01.127
CHEMBL254773 94553 0 None -77 2 Rabbit 5.8 pIC50 = 5.8 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 515 6 3 3 5.0 O=C(NCCc1c(-c2ccc(F)cc2)[nH]c2ccc(Br)cc12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.01.127
24970255 126295 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 399 8 2 5 4.0 CC(C)(NC(=O)c1ccc2sccc2c1OCCOc1ccccc1)C(=O)O nan
CHEMBL3654439 126295 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 399 8 2 5 4.0 CC(C)(NC(=O)c1ccc2sccc2c1OCCOc1ccccc1)C(=O)O nan
57864038 124653 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 399 8 2 5 4.0 CC(C)(NC(=O)c1sc2ccccc2c1OCCOc1ccccc1)C(=O)O nan
CHEMBL3645130 124653 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 399 8 2 5 4.0 CC(C)(NC(=O)c1sc2ccccc2c1OCCOc1ccccc1)C(=O)O nan
9968028 79885 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of chemotaxis of CHO cells expressing human CXCR2Inhibition of chemotaxis of CHO cells expressing human CXCR2
ChEMBL 345 5 3 6 1.7 CCC(CC)/N=c1\c(O)c(O)\c1=N/c1cccc(C(=O)N(C)C)c1O 10.1016/j.bmcl.2006.04.082
CHEMBL214047 79885 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of chemotaxis of CHO cells expressing human CXCR2Inhibition of chemotaxis of CHO cells expressing human CXCR2
ChEMBL 345 5 3 6 1.7 CCC(CC)/N=c1\c(O)c(O)\c1=N/c1cccc(C(=O)N(C)C)c1O 10.1016/j.bmcl.2006.04.082
CHEMBL5090422 213489 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None Cc1ccc(NC(=O)Nc2ccc3c(c2O)S(=O)(=O)CC=C3)cc1 10.1021/acs.jmedchem.1c01219
CHEMBL5078246 212774 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccc2c(c1O)S(=O)(=O)CC=C2)Nc1cccc(F)c1Cl 10.1021/acs.jmedchem.1c01219
3854666 3445 78 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against CXCR2 (unknown origin) by calcium flux assayAntagonist activity against CXCR2 (unknown origin) by calcium flux assay
ChEMBL 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 10.1016/j.ejmech.2021.113812
833 3445 78 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against CXCR2 (unknown origin) by calcium flux assayAntagonist activity against CXCR2 (unknown origin) by calcium flux assay
ChEMBL 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 10.1016/j.ejmech.2021.113812
CHEMBL239767 3445 78 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against CXCR2 (unknown origin) by calcium flux assayAntagonist activity against CXCR2 (unknown origin) by calcium flux assay
ChEMBL 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 10.1016/j.ejmech.2021.113812
59446380 114435 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 440 8 3 6 1.9 O=C(O)CN(C(=O)c1ccc(SCc2ccccc2B(O)O)nc1)c1ccc(F)cc1 10.1021/jm500827t
CHEMBL3342323 114435 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 440 8 3 6 1.9 O=C(O)CN(C(=O)c1ccc(SCc2ccccc2B(O)O)nc1)c1ccc(F)cc1 10.1021/jm500827t
44610601 171042 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CXCR2 (unknown origin) by [35S]-GTPgammaS binding assayAntagonist activity at CXCR2 (unknown origin) by [35S]-GTPgammaS binding assay
ChEMBL 483 9 3 9 3.0 CC[C@@H](Nc1c(Nc2ccc(Cl)c(S(=O)(=O)N(C)OC)c2O)c(=O)c1=O)c1ccc(C)o1 10.1016/j.ejmech.2019.111853
CHEMBL4465379 171042 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CXCR2 (unknown origin) by [35S]-GTPgammaS binding assayAntagonist activity at CXCR2 (unknown origin) by [35S]-GTPgammaS binding assay
ChEMBL 483 9 3 9 3.0 CC[C@@H](Nc1c(Nc2ccc(Cl)c(S(=O)(=O)N(C)OC)c2O)c(=O)c1=O)c1ccc(C)o1 10.1016/j.ejmech.2019.111853
16098481 81700 0 None 218 2 Human 8.6 pIC50 = 8.6 Functional
Inhibition of CXCL1-induced human neutrophil chemotaxisInhibition of CXCL1-induced human neutrophil chemotaxis
ChEMBL 383 6 3 7 2.5 Cc1ccc([C@@H](C)Nc2c(Nc3cccc(C(=O)N(C)C)c3O)c(=O)c2=O)o1 10.1021/jm0609622
CHEMBL216602 81700 0 None 218 2 Human 8.6 pIC50 = 8.6 Functional
Inhibition of CXCL1-induced human neutrophil chemotaxisInhibition of CXCL1-induced human neutrophil chemotaxis
ChEMBL 383 6 3 7 2.5 Cc1ccc([C@@H](C)Nc2c(Nc3cccc(C(=O)N(C)C)c3O)c(=O)c2=O)o1 10.1021/jm0609622
CHEMBL5078730 212810 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=c1c(Nc2ccccc2Cl)c(Nc2ccc3c(c2O)S(=O)(=O)CC=C3)c1=O 10.1021/acs.jmedchem.1c01219
24970171 126291 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 409 9 2 3 4.6 CC(C)(NC(=O)c1ccc2c(c1OCCCCc1ccccc1)CCCC2)C(=O)O nan
CHEMBL3654435 126291 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 409 9 2 3 4.6 CC(C)(NC(=O)c1ccc2c(c1OCCCCc1ccccc1)CCCC2)C(=O)O nan
72948071 104181 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 321 4 1 5 3.6 CCc1cnn2c(O)cc(CSc3cccc(F)c3F)nc12 10.1016/j.bmcl.2013.11.074
CHEMBL3105087 104181 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 321 4 1 5 3.6 CCc1cnn2c(O)cc(CSc3cccc(F)c3F)nc12 10.1016/j.bmcl.2013.11.074
46897163 118578 4 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 466 7 3 6 3.3 O=C(Nc1ccc(F)cc1)c1ccc(SCc2cc(OC(F)(F)F)ccc2B(O)O)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3426944 118578 4 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 466 7 3 6 3.3 O=C(Nc1ccc(F)cc1)c1ccc(SCc2cc(OC(F)(F)F)ccc2B(O)O)nc1 10.1016/j.bmcl.2015.07.090
122187266 122501 0 None -6 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 446 8 3 7 2.3 O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccc(B(O)O)cn2)Cc2ccco2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609016 122501 0 None -6 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 446 8 3 7 2.3 O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccc(B(O)O)cn2)Cc2ccco2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL5083131 213072 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccc2c(c1O)S(=O)(=O)CCC2)Nc1cccc(Cl)c1Cl 10.1021/acs.jmedchem.1c01219
CHEMBL5087256 213307 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccccc1Cl)Nc1ccc2c(c1O)S(=O)(=O)CCC2 10.1021/acs.jmedchem.1c01219
46897162 3659 7 None 6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 10.1021/jm500827t
8501 3659 7 None 6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 10.1021/jm500827t
CHEMBL3342269 3659 7 None 6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 10.1021/jm500827t
44447915 168585 0 None -43 2 Rabbit 5.7 pIC50 = 5.7 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 399 6 2 4 3.2 CS(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
CHEMBL440405 168585 0 None -43 2 Rabbit 5.7 pIC50 = 5.7 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 399 6 2 4 3.2 CS(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
24970173 126292 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 411 9 2 4 4.0 CC(C)(NC(=O)c1ccc2c(c1OCCCOc1ccccc1)CCCC2)C(=O)O nan
CHEMBL3654436 126292 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 411 9 2 4 4.0 CC(C)(NC(=O)c1ccc2c(c1OCCCOc1ccccc1)CCCC2)C(=O)O nan
46897450 114424 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 382 6 2 4 4.5 O=C(O)c1cccc(CSc2ccc(C(=O)Nc3ccc(F)cc3)cn2)c1 10.1021/jm500827t
CHEMBL3342309 114424 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 382 6 2 4 4.5 O=C(O)c1cccc(CSc2ccc(C(=O)Nc3ccc(F)cc3)cn2)c1 10.1021/jm500827t
162675855 182729 0 None 45 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 425 4 3 6 3.0 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccc(F)cc3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4797191 182729 0 None 45 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 425 4 3 6 3.0 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccc(F)cc3)N2)c1O 10.1021/acsmedchemlett.1c00113
122187256 122490 0 None 1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 365 6 4 5 1.8 O=C(Nc1ccc(F)cc1)c1ccc(NCc2ccc(B(O)O)cc2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609004 122490 0 None 1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 365 6 4 5 1.8 O=C(Nc1ccc(F)cc1)c1ccc(NCc2ccc(B(O)O)cc2)nc1 10.1016/j.bmcl.2015.07.090
23642281 125320 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Calicum Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes).Calicum Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes).
ChEMBL 507 8 2 3 6.6 CCC(NC(=O)c1ccc2ccccc2c1OCc1ccc(C(F)(F)F)cc1)(C(=O)O)c1ccccc1 nan
CHEMBL3648347 125320 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Calicum Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes).Calicum Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes).
ChEMBL 507 8 2 3 6.6 CCC(NC(=O)c1ccc2ccccc2c1OCc1ccc(C(F)(F)F)cc1)(C(=O)O)c1ccccc1 nan
122187265 122500 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 464 8 3 7 2.0 O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccc(B(O)O)cn2)CC2CCOCC2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609015 122500 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 464 8 3 7 2.0 O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccc(B(O)O)cn2)CC2CCOCC2)nc1 10.1016/j.bmcl.2015.07.090
162644015 181183 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 292 2 3 5 1.9 N#Cc1ccc(NC2=NC(=O)C(c3ccccc3)N2)c(O)c1 10.1021/acsmedchemlett.1c00113
CHEMBL4777637 181183 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 292 2 3 5 1.9 N#Cc1ccc(NC2=NC(=O)C(c3ccccc3)N2)c(O)c1 10.1021/acsmedchemlett.1c00113
CHEMBL5075434 212603 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None Cc1c(Cl)cccc1NC(=O)Nc1ccc2c(c1O)S(=O)(=O)CCC2 10.1021/acs.jmedchem.1c01219
122187260 122494 0 None -1 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 380 6 3 6 1.2 CN(Cc1cccc(B(O)O)c1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
CHEMBL3609009 122494 0 None -1 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 380 6 3 6 1.2 CN(Cc1cccc(B(O)O)c1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
CHEMBL5092474 213597 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=c1c(Nc2ccc3c(c2O)S(=O)(=O)CC=C3)c(Nc2cccc(Cl)c2Cl)c1=O 10.1021/acs.jmedchem.1c01219
162657640 180585 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 421 5 3 6 2.7 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@H](Cc3ccccc3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4760919 180585 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 421 5 3 6 2.7 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@H](Cc3ccccc3)N2)c1O 10.1021/acsmedchemlett.1c00113
24769071 124655 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 435 10 2 4 4.9 CC(C)CC(C)(NC(=O)c1ccc2ccccc2c1OCCOc1ccccc1)C(=O)O nan
CHEMBL3645132 124655 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 435 10 2 4 4.9 CC(C)CC(C)(NC(=O)c1ccc2ccccc2c1OCCOc1ccccc1)C(=O)O nan
9928389 79199 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of chemotaxis of CHO cells expressing human CXCR2Inhibition of chemotaxis of CHO cells expressing human CXCR2
ChEMBL 351 3 3 6 1.8 CN(C)C(=O)c1cccc(/N=c2\c(O)c(O)\c2=N/c2ccccc2)c1O 10.1016/j.bmcl.2006.04.082
CHEMBL211468 79199 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of chemotaxis of CHO cells expressing human CXCR2Inhibition of chemotaxis of CHO cells expressing human CXCR2
ChEMBL 351 3 3 6 1.8 CN(C)C(=O)c1cccc(/N=c2\c(O)c(O)\c2=N/c2ccccc2)c1O 10.1016/j.bmcl.2006.04.082
24953464 104178 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 343 3 1 5 4.2 Oc1cc(CSc2cccc(F)c2F)nc2c3ccccc3nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3105084 104178 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 343 3 1 5 4.2 Oc1cc(CSc2cccc(F)c2F)nc2c3ccccc3nn12 10.1016/j.bmcl.2013.11.074
10479502 1519 15 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CXCR2 assessed as inhibition of neutrophil CD11b up-regulationAntagonist activity at CXCR2 assessed as inhibition of neutrophil CD11b up-regulation
ChEMBL 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 10.1021/jm300682j
8499 1519 15 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CXCR2 assessed as inhibition of neutrophil CD11b up-regulationAntagonist activity at CXCR2 assessed as inhibition of neutrophil CD11b up-regulation
ChEMBL 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 10.1021/jm300682j
CHEMBL2178579 1519 15 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CXCR2 assessed as inhibition of neutrophil CD11b up-regulationAntagonist activity at CXCR2 assessed as inhibition of neutrophil CD11b up-regulation
ChEMBL 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 10.1021/jm300682j
DB12135 1519 15 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CXCR2 assessed as inhibition of neutrophil CD11b up-regulationAntagonist activity at CXCR2 assessed as inhibition of neutrophil CD11b up-regulation
ChEMBL 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 10.1021/jm300682j
122187261 122495 0 None -1 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 366 6 4 6 1.2 O=C(Nc1ccc(F)cc1)c1cnc(NCc2ccc(B(O)O)cc2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609010 122495 0 None -1 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 366 6 4 6 1.2 O=C(Nc1ccc(F)cc1)c1cnc(NCc2ccc(B(O)O)cc2)nc1 10.1016/j.bmcl.2015.07.090
162677254 182979 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 345 3 3 6 1.5 CC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
CHEMBL4800297 182979 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 345 3 3 6 1.5 CC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
46897352 114428 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 464 6 1 5 5.1 CC1(C)OB(c2ccccc2CSc2ccc(C(=O)Nc3ccc(F)cc3)cn2)OC1(C)C 10.1021/jm500827t
CHEMBL3342313 114428 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 464 6 1 5 5.1 CC1(C)OB(c2ccccc2CSc2ccc(C(=O)Nc3ccc(F)cc3)cn2)OC1(C)C 10.1021/jm500827t
46897256 114423 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 354 5 2 4 4.5 O=C(Nc1ccc(F)cc1)c1ccc(SCc2ccccc2O)nc1 10.1021/jm500827t
CHEMBL3342304 114423 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 354 5 2 4 4.5 O=C(Nc1ccc(F)cc1)c1ccc(SCc2ccccc2O)nc1 10.1021/jm500827t
59446381 114429 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 448 7 3 6 3.2 O=C(Nc1ccc(OC(F)(F)F)cc1)c1ccc(SCc2ccccc2B(O)O)nc1 10.1021/jm500827t
CHEMBL3342314 114429 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 448 7 3 6 3.2 O=C(Nc1ccc(OC(F)(F)F)cc1)c1ccc(SCc2ccccc2B(O)O)nc1 10.1021/jm500827t
24953110 104175 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 370 4 1 6 4.1 Oc1cc(CSc2cccc(F)c2F)nc2cc(-c3ccccn3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3105081 104175 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 370 4 1 6 4.1 Oc1cc(CSc2cccc(F)c2F)nc2cc(-c3ccccn3)nn12 10.1016/j.bmcl.2013.11.074
162655442 180111 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 373 5 3 6 2.3 CCC[C@@H]1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
CHEMBL4755486 180111 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 373 5 3 6 2.3 CCC[C@@H]1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
162648477 179382 0 None 707 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 373 5 3 6 2.3 CCC[C@H]1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
CHEMBL4746698 179382 0 None 707 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 373 5 3 6 2.3 CCC[C@H]1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
91937332 114432 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 383 6 3 6 1.8 O=C(Nc1ccc(F)cn1)c1ccc(SCc2ccccc2B(O)O)nc1 10.1021/jm500827t
CHEMBL3342319 114432 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 383 6 3 6 1.8 O=C(Nc1ccc(F)cn1)c1ccc(SCc2ccccc2B(O)O)nc1 10.1021/jm500827t
162662122 180938 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 331 3 3 6 1.1 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)CN2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4765070 180938 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 331 3 3 6 1.1 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)CN2)c1O 10.1021/acsmedchemlett.1c00113
122187263 122498 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 456 8 3 6 2.8 O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccccc2)Cc2ccc(B(O)O)cn2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609013 122498 0 None 1 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 456 8 3 6 2.8 O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccccc2)Cc2ccc(B(O)O)cn2)nc1 10.1016/j.bmcl.2015.07.090
3854666 3445 78 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 10.1021/jm500827t
833 3445 78 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 10.1021/jm500827t
CHEMBL239767 3445 78 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 10.1021/jm500827t
44447923 95023 0 None -38 2 Rabbit 5.5 pIC50 = 5.5 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 453 6 2 4 4.1 N#Cc1ccc2[nH]c(-c3ccc(F)cc3)c(CCCC(=O)NS(=O)(=O)C(F)(F)F)c2c1 10.1016/j.bmcl.2008.01.127
CHEMBL257178 95023 0 None -38 2 Rabbit 5.5 pIC50 = 5.5 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 453 6 2 4 4.1 N#Cc1ccc2[nH]c(-c3ccc(F)cc3)c(CCCC(=O)NS(=O)(=O)C(F)(F)F)c2c1 10.1016/j.bmcl.2008.01.127
162648010 179391 0 None 138 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 387 5 3 6 2.5 CC(C)CC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
CHEMBL4746803 179391 0 None 138 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 387 5 3 6 2.5 CC(C)CC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
162676913 182939 0 None 158 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 441 4 3 6 3.5 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3cccc(Cl)c3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4799848 182939 0 None 158 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 441 4 3 6 3.5 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3cccc(Cl)c3)N2)c1O 10.1021/acsmedchemlett.1c00113
10479502 1519 15 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CXCR2 assessed as inhibition of neutrophil shape changeAntagonist activity at CXCR2 assessed as inhibition of neutrophil shape change
ChEMBL 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 10.1021/jm300682j
8499 1519 15 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CXCR2 assessed as inhibition of neutrophil shape changeAntagonist activity at CXCR2 assessed as inhibition of neutrophil shape change
ChEMBL 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 10.1021/jm300682j
CHEMBL2178579 1519 15 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CXCR2 assessed as inhibition of neutrophil shape changeAntagonist activity at CXCR2 assessed as inhibition of neutrophil shape change
ChEMBL 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 10.1021/jm300682j
DB12135 1519 15 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CXCR2 assessed as inhibition of neutrophil shape changeAntagonist activity at CXCR2 assessed as inhibition of neutrophil shape change
ChEMBL 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 10.1021/jm300682j
162660441 180730 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 345 3 3 6 1.5 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@H](C)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4762597 180730 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 345 3 3 6 1.5 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@H](C)N2)c1O 10.1021/acsmedchemlett.1c00113
44447915 168585 0 None 43 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 399 6 2 4 3.2 CS(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
CHEMBL440405 168585 0 None 43 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 399 6 2 4 3.2 CS(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
136074340 112460 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 391 6 1 7 3.3 CCOC(=O)[C@H]1C[C@@H]1c1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
CHEMBL3310785 112460 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 391 6 1 7 3.3 CCOC(=O)[C@H]1C[C@@H]1c1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
136986968 112468 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 294 4 1 4 3.6 Oc1cc(C2CC2)nc(SCc2cccc(F)c2F)n1 10.1016/j.bmcl.2014.06.011
CHEMBL3310794 112468 1 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 294 4 1 4 3.6 Oc1cc(C2CC2)nc(SCc2cccc(F)c2F)n1 10.1016/j.bmcl.2014.06.011
44432416 86960 0 None 151 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 415 3 3 6 4.4 O=S1(=O)N=C(Nc2ccccc2Oc2ccccc2)Nc2c(O)cc(Cl)cc21 10.1016/j.bmcl.2007.05.011
CHEMBL233346 86960 0 None 151 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 415 3 3 6 4.4 O=S1(=O)N=C(Nc2ccccc2Oc2ccccc2)Nc2c(O)cc(Cl)cc21 10.1016/j.bmcl.2007.05.011
CHEMBL5071577 212491 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccccc1F)Nc1ccc2c(c1O)S(=O)(=O)CC=C2 10.1021/acs.jmedchem.1c01219
136986994 112556 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 420 4 1 4 4.2 Oc1nc(SCc2cccc(F)c2F)nc(C2CC2)c1I 10.1016/j.bmcl.2014.06.011
CHEMBL3311397 112556 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 420 4 1 4 4.2 Oc1nc(SCc2cccc(F)c2F)nc(C2CC2)c1I 10.1016/j.bmcl.2014.06.011
24769330 124657 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 423 8 2 4 4.2 O=C(NC1(C(=O)O)CCC1)c1ccc2ccccc2c1OCCOc1ccc(F)cc1 nan
CHEMBL3645134 124657 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 423 8 2 4 4.2 O=C(NC1(C(=O)O)CCC1)c1ccc2ccccc2c1OCCOc1ccc(F)cc1 nan
CHEMBL5088269 213374 3 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None Cc1c(F)cccc1NC(=O)Nc1ccc2c(c1O)S(=O)(=O)CC=C2 10.1021/acs.jmedchem.1c01219
CHEMBL5087298 213309 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=c1c(Nc2ccc3c(c2O)S(=O)(=O)CCC3)c(Nc2cccc(F)c2Cl)c1=O 10.1021/acs.jmedchem.1c01219
24804051 104165 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 384 5 1 6 4.0 Oc1cc(CSc2cccc(F)c2F)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3104912 104165 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 384 5 1 6 4.0 Oc1cc(CSc2cccc(F)c2F)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL5089049 213420 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None Cc1c(F)cccc1Nc1c(Nc2ccc3c(c2O)S(=O)(=O)CC=C3)c(=O)c1=O 10.1021/acs.jmedchem.1c01219
135907765 112444 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 355 4 1 5 4.3 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1-c1ccccc1 10.1016/j.bmcl.2014.06.011
CHEMBL3310769 112444 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 355 4 1 5 4.3 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1-c1ccccc1 10.1016/j.bmcl.2014.06.011
135907789 112459 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 335 3 1 5 3.9 CC(C)(C)c1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
CHEMBL3310784 112459 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 335 3 1 5 3.9 CC(C)(C)c1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
46897162 3659 7 None 6 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 10.1021/jm500827t
8501 3659 7 None 6 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 10.1021/jm500827t
CHEMBL3342269 3659 7 None 6 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 10.1021/jm500827t
44775716 114421 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 338 5 1 3 4.8 O=C(Nc1ccc(F)cc1)c1ccc(SCc2ccccc2)nc1 10.1021/jm500827t
CHEMBL3342291 114421 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 338 5 1 3 4.8 O=C(Nc1ccc(F)cc1)c1ccc(SCc2ccccc2)nc1 10.1021/jm500827t
59446412 114418 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 330 5 2 6 2.3 O=C(Nc1ccc(F)cc1)c1ccc(SCc2nn[nH]n2)nc1 10.1021/jm500827t
CHEMBL3342270 114418 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 330 5 2 6 2.3 O=C(Nc1ccc(F)cc1)c1ccc(SCc2nn[nH]n2)nc1 10.1021/jm500827t
122187268 122502 0 None 1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 457 8 3 7 2.2 O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccccc2)Cc2ccc(B(O)O)cn2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609018 122502 0 None 1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 457 8 3 7 2.2 O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccccc2)Cc2ccc(B(O)O)cn2)nc1 10.1016/j.bmcl.2015.07.090
44447946 94553 0 None 77 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 515 6 3 3 5.0 O=C(NCCc1c(-c2ccc(F)cc2)[nH]c2ccc(Br)cc12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.01.127
CHEMBL254773 94553 0 None 77 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 515 6 3 3 5.0 O=C(NCCc1c(-c2ccc(F)cc2)[nH]c2ccc(Br)cc12)NS(=O)(=O)c1ccccc1 10.1016/j.bmcl.2008.01.127
3854666 3445 78 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 10.1021/jm500827t
833 3445 78 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 10.1021/jm500827t
CHEMBL239767 3445 78 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 10.1021/jm500827t
44432386 146962 0 None 79 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 401 1 3 5 3.4 O=S1(=O)N=C(Nc2ccccc2Br)Nc2c(O)cc(Cl)cc21 10.1016/j.bmcl.2007.05.011
CHEMBL393047 146962 0 None 79 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 401 1 3 5 3.4 O=S1(=O)N=C(Nc2ccccc2Br)Nc2c(O)cc(Cl)cc21 10.1016/j.bmcl.2007.05.011
CHEMBL5079979 212884 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccc2c(c1O)S(=O)(=O)CCC2=O)Nc1cccc(Cl)c1Cl 10.1021/acs.jmedchem.1c01219
162647583 179319 0 None 25 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 413 4 3 6 3.1 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@H](C3CCCCC3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4745933 179319 0 None 25 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 413 4 3 6 3.1 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@H](C3CCCCC3)N2)c1O 10.1021/acsmedchemlett.1c00113
122187255 122489 0 None 10 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 379 6 3 5 1.8 CN(Cc1cccc(B(O)O)c1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
CHEMBL3609003 122489 0 None 10 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 379 6 3 5 1.8 CN(Cc1cccc(B(O)O)c1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
24960030 104156 2 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 366 5 1 7 3.9 Cc1cc(SCc2cc(O)n3nc(Cc4ccccc4)nc3n2)c(C)o1 10.1016/j.bmcl.2013.11.074
CHEMBL3104903 104156 2 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 366 5 1 7 3.9 Cc1cc(SCc2cc(O)n3nc(Cc4ccccc4)nc3n2)c(C)o1 10.1016/j.bmcl.2013.11.074
24959669 104162 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 438 6 1 6 5.7 Cc1ccc(-c2cccc(SCc3cc(O)n4nc(Cc5ccccc5)nc4n3)c2)cc1 10.1016/j.bmcl.2013.11.074
CHEMBL3104909 104162 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 438 6 1 6 5.7 Cc1ccc(-c2cccc(SCc3cc(O)n4nc(Cc5ccccc5)nc4n3)c2)cc1 10.1016/j.bmcl.2013.11.074
24952761 104180 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 318 3 1 6 2.9 N#Cc1cnn2c(O)cc(CSc3cccc(F)c3F)nc12 10.1016/j.bmcl.2013.11.074
CHEMBL3105086 104180 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 318 3 1 6 2.9 N#Cc1cnn2c(O)cc(CSc3cccc(F)c3F)nc12 10.1016/j.bmcl.2013.11.074
CHEMBL5080880 212938 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None Cc1c(F)cccc1NC(=O)Nc1ccc2c(c1O)S(=O)(=O)CCC2=O 10.1021/acs.jmedchem.1c01219
CHEMBL5081049 212944 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccc2c(c1O)S(=O)(=O)CCC2)Nc1cccc(F)c1Cl 10.1021/acs.jmedchem.1c01219
162650232 179420 0 None 1288 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 387 6 3 6 2.7 CCCCC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
CHEMBL4747035 179420 0 None 1288 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 387 6 3 6 2.7 CCCCC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
135907792 112453 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 293 3 1 5 2.9 Cc1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
CHEMBL3310779 112453 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 293 3 1 5 2.9 Cc1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
122187269 122503 0 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 458 8 3 8 1.5 O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccccn2)Cc2ccc(B(O)O)cn2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609019 122503 0 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 458 8 3 8 1.5 O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccccn2)Cc2ccc(B(O)O)cn2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL5094410 213715 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccccc1C(F)(F)F)Nc1ccc2c(c1O)S(=O)(=O)CCC2 10.1021/acs.jmedchem.1c01219
44626319 196744 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 346 7 3 7 1.1 CCN(CC)Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O 10.1016/j.bmcl.2009.08.014
CHEMBL577075 196744 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 346 7 3 7 1.1 CCN(CC)Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O 10.1016/j.bmcl.2009.08.014
44432391 147233 0 None 75 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 375 1 3 5 3.4 O=S1(=O)N=C(Nc2cccc(F)c2Cl)Nc2c(O)cc(Cl)cc21 10.1016/j.bmcl.2007.05.011
CHEMBL393253 147233 0 None 75 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 375 1 3 5 3.4 O=S1(=O)N=C(Nc2cccc(F)c2Cl)Nc2c(O)cc(Cl)cc21 10.1016/j.bmcl.2007.05.011
135907780 112450 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 399 5 1 6 4.6 COc1ccc(-c2nc(SCc3cccc(F)c3F)nc(O)c2C#N)cc1C 10.1016/j.bmcl.2014.06.011
CHEMBL3310776 112450 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 399 5 1 6 4.6 COc1ccc(-c2nc(SCc3cccc(F)c3F)nc(O)c2C#N)cc1C 10.1016/j.bmcl.2014.06.011
24958934 104173 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 398 6 1 6 4.2 Oc1cc(CSc2cccc(F)c2F)nc2nc(CCc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3105079 104173 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 398 6 1 6 4.2 Oc1cc(CSc2cccc(F)c2F)nc2nc(CCc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
162667020 181876 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 345 3 3 6 1.5 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@@H](C)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4786309 181876 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 345 3 3 6 1.5 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@@H](C)N2)c1O 10.1021/acsmedchemlett.1c00113
135907772 112452 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 369 4 1 5 4.6 Cc1cccc(-c2nc(SCc3cccc(F)c3F)nc(O)c2C#N)c1 10.1016/j.bmcl.2014.06.011
CHEMBL3310778 112452 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 369 4 1 5 4.6 Cc1cccc(-c2nc(SCc3cccc(F)c3F)nc(O)c2C#N)c1 10.1016/j.bmcl.2014.06.011
155531736 171108 0 None 60 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CXCR2 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at CXCR2 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 395 5 3 6 2.6 O=C(c1cccc(Nc2c(NC3C[C@@H]4CC[C@H]3C4)c(=O)c2=O)c1O)N1CCCC1 10.1016/j.ejmech.2019.111853
CHEMBL4466314 171108 0 None 60 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CXCR2 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at CXCR2 (unknown origin) stably expressed in HEK293 cells co-expressing Galpha16 assessed as reduction in IL-8-induced intracellular calcium change incubated for 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 395 5 3 6 2.6 O=C(c1cccc(Nc2c(NC3C[C@@H]4CC[C@H]3C4)c(=O)c2=O)c1O)N1CCCC1 10.1016/j.ejmech.2019.111853
9927727 103447 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CXCR2 in human neutrophils assessed as reduction in GROalpha stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at CXCR2 in human neutrophils assessed as reduction in GROalpha stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 335 3 1 4 4.6 Sc1nc(-c2ccccc2Cl)nn1Cc1cccc(Cl)c1 10.1016/j.ejmech.2019.111853
CHEMBL309253 103447 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CXCR2 in human neutrophils assessed as reduction in GROalpha stimulated intracellular calcium mobilisation by FLIPR assayAntagonist activity at CXCR2 in human neutrophils assessed as reduction in GROalpha stimulated intracellular calcium mobilisation by FLIPR assay
ChEMBL 335 3 1 4 4.6 Sc1nc(-c2ccccc2Cl)nn1Cc1cccc(Cl)c1 10.1016/j.ejmech.2019.111853
10200589 94499 0 None 2 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of CXCL1-induced human neutrophil chemotaxisInhibition of CXCL1-induced human neutrophil chemotaxis
ChEMBL 393 7 3 6 3.0 CC[C@@H](Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccccc1 10.1021/jm0609622
CHEMBL254370 94499 0 None 2 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of CXCL1-induced human neutrophil chemotaxisInhibition of CXCL1-induced human neutrophil chemotaxis
ChEMBL 393 7 3 6 3.0 CC[C@@H](Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccccc1 10.1021/jm0609622
136074342 112465 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 297 4 1 5 3.8 CC(Sc1nc(O)c(C#N)c(C2CC2)n1)c1ccccc1 10.1016/j.bmcl.2014.06.011
CHEMBL3310790 112465 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 297 4 1 5 3.8 CC(Sc1nc(O)c(C#N)c(C2CC2)n1)c1ccccc1 10.1016/j.bmcl.2014.06.011
24959664 104163 2 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 416 5 1 6 5.0 Oc1cc(CSc2ccc(Cl)cc2Cl)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3104910 104163 2 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 416 5 1 6 5.0 Oc1cc(CSc2ccc(Cl)cc2Cl)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
122187264 122499 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 457 8 3 7 2.2 O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccccn2)Cc2ccc(B(O)O)cn2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609014 122499 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 457 8 3 7 2.2 O=C(Nc1ccc(F)cc1)c1ccc(N(Cc2ccccn2)Cc2ccc(B(O)O)cn2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL5076154 212645 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccccc1Br)Nc1ccc2c(c1O)S(=O)(=O)CC=C2 10.1021/acs.jmedchem.1c01219
11304851 154068 0 None 46 4 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 426 4 3 8 3.7 O=[N+]([O-])c1cc(O)c2c(c1)S(=O)(=O)N=C(Nc1ccccc1Oc1ccccc1)N2 10.1016/j.bmcl.2007.05.011
CHEMBL399203 154068 0 None 46 4 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 426 4 3 8 3.7 O=[N+]([O-])c1cc(O)c2c(c1)S(=O)(=O)N=C(Nc1ccccc1Oc1ccccc1)N2 10.1016/j.bmcl.2007.05.011
135907779 112456 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 347 4 1 5 4.3 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1C1CCCC1 10.1016/j.bmcl.2014.06.011
CHEMBL3310781 112456 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 347 4 1 5 4.3 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1C1CCCC1 10.1016/j.bmcl.2014.06.011
24780598 1289 33 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 441 4 4 5 3.7 O=C(Nc1cccc(c1C)F)Nc1ccc(c(c1O)S(=O)(=O)[C@H]1CCCNC1)Cl nan
8500 1289 33 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 441 4 4 5 3.7 O=C(Nc1cccc(c1C)F)Nc1ccc(c(c1O)S(=O)(=O)[C@H]1CCCNC1)Cl nan
CHEMBL3039531 1289 33 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 441 4 4 5 3.7 O=C(Nc1cccc(c1C)F)Nc1ccc(c(c1O)S(=O)(=O)[C@H]1CCCNC1)Cl nan
DB11922 1289 33 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 441 4 4 5 3.7 O=C(Nc1cccc(c1C)F)Nc1ccc(c(c1O)S(=O)(=O)[C@H]1CCCNC1)Cl nan
57649039 142010 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 423 5 4 5 3.4 CCc1ccccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CCNC2)c1O nan
CHEMBL3890888 142010 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 423 5 4 5 3.4 CCc1ccccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CCNC2)c1O nan
57649037 142174 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 444 4 4 6 3.3 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O nan
CHEMBL3892206 142174 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 444 4 4 6 3.3 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O nan
50996598 142239 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 489 4 4 7 3.5 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O)Nc1cccc2c1OC(F)(F)O2 nan
CHEMBL3892666 142239 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 489 4 4 7 3.5 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O)Nc1cccc2c1OC(F)(F)O2 nan
50996778 142608 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 533 5 3 6 4.9 CCOC(=O)N1CCC(S(=O)(=O)c2c(Cl)ccc(NC(=O)Nc3cccc(F)c3Cl)c2O)CC1 nan
CHEMBL3895808 142608 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 533 5 3 6 4.9 CCOC(=O)N1CCC(S(=O)(=O)c2c(Cl)ccc(NC(=O)Nc3cccc(F)c3Cl)c2O)CC1 nan
50996594 143252 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 413 4 4 5 2.9 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CNC2)c1O nan
CHEMBL3901031 143252 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 413 4 4 5 2.9 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CNC2)c1O nan
50995535 143915 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 461 4 4 5 4.0 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O)Nc1cccc(F)c1Cl nan
CHEMBL3906495 143915 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 461 4 4 5 4.0 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O)Nc1cccc(F)c1Cl nan
57649033 144403 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 487 6 4 6 4.6 O=C(Nc1ccccc1Oc1ccccc1)Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCNC2)c1O nan
CHEMBL3910320 144403 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 487 6 4 6 4.6 O=C(Nc1ccccc1Oc1ccccc1)Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCNC2)c1O nan
50996421 144457 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 461 5 4 5 3.9 O=C(Nc1ccc(Cl)c(S(=O)(=O)CC2CCNC2)c1O)Nc1cccc(F)c1Cl nan
CHEMBL3910854 144457 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 461 5 4 5 3.9 O=C(Nc1ccc(Cl)c(S(=O)(=O)CC2CCNC2)c1O)Nc1cccc(F)c1Cl nan
57649040 144662 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 527 6 4 6 5.5 O=C(Nc1ccccc1Oc1ccccc1)Nc1ccc(Cl)c(S(=O)(=O)C2C[C@@H]3CC[C@H](C2)N3)c1O nan
CHEMBL3912422 144662 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 527 6 4 6 5.5 O=C(Nc1ccccc1Oc1ccccc1)Nc1ccc(Cl)c(S(=O)(=O)C2C[C@@H]3CC[C@H](C2)N3)c1O nan
57649042 144744 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 447 4 4 5 3.6 O=C(Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCNC2)c1O)Nc1cccc(F)c1Cl nan
CHEMBL3912983 144744 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 447 4 4 5 3.6 O=C(Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCNC2)c1O)Nc1cccc(F)c1Cl nan
57649022 145014 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 479 5 4 6 3.7 O=C(Nc1ccccc1OC(F)(F)F)Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CCNC2)c1O nan
CHEMBL3915083 145014 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 479 5 4 6 3.7 O=C(Nc1ccccc1OC(F)(F)F)Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CCNC2)c1O nan
50996424 145176 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 477 4 4 5 4.5 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O)Nc1cccc(Cl)c1Cl nan
CHEMBL3916281 145176 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 477 4 4 5 4.5 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O)Nc1cccc(Cl)c1Cl nan
50996422 146523 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 437 5 4 5 3.8 CCc1ccccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O nan
CHEMBL3926993 146523 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 437 5 4 5 3.8 CCc1ccccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O nan
50996595 146648 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 493 5 4 6 4.1 O=C(Nc1ccccc1OC(F)(F)F)Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O nan
CHEMBL3927944 146648 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 493 5 4 6 4.1 O=C(Nc1ccccc1OC(F)(F)F)Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O nan
16755746 146856 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 444 4 4 6 3.3 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O nan
CHEMBL3929680 146856 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 444 4 4 6 3.3 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O nan
50996596 146998 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 437 5 4 5 3.8 CCc1ccccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O nan
CHEMBL3930695 146998 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 437 5 4 5 3.8 CCc1ccccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O nan
50997127 147412 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 513 5 3 6 4.5 CCOC(=O)N1CCC(S(=O)(=O)c2c(Cl)ccc(NC(=O)Nc3cccc(F)c3C)c2O)CC1 nan
CHEMBL3933806 147412 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 513 5 3 6 4.5 CCOC(=O)N1CCC(S(=O)(=O)c2c(Cl)ccc(NC(=O)Nc3cccc(F)c3C)c2O)CC1 nan
57649024 147738 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 487 4 4 5 4.5 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2C[C@@H]3CC[C@H](C2)N3)c1O)Nc1cccc(F)c1Cl nan
CHEMBL3936567 147738 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 487 4 4 5 4.5 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2C[C@@H]3CC[C@H](C2)N3)c1O)Nc1cccc(F)c1Cl nan
58994916 148414 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 481 4 3 5 4.5 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)[C@H]2C[C@@H]3CC[C@H](C2)N3C)c1O nan
CHEMBL3941989 148414 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 481 4 3 5 4.5 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)[C@H]2C[C@@H]3CC[C@H](C2)N3C)c1O nan
50996245 148922 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 441 5 4 5 3.5 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)CC2CCNC2)c1O nan
CHEMBL3946021 148922 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 441 5 4 5 3.5 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)CC2CCNC2)c1O nan
50996777 149214 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 501 6 4 6 5.0 O=C(Nc1ccccc1Oc1ccccc1)Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O nan
CHEMBL3948111 149214 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 501 6 4 6 5.0 O=C(Nc1ccccc1Oc1ccccc1)Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O nan
57649029 149308 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 470 4 4 6 3.8 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)C2C[C@@H]3CC[C@H](C2)N3)c1O nan
CHEMBL3948929 149308 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 470 4 4 6 3.8 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)C2C[C@@H]3CC[C@H](C2)N3)c1O nan
24780599 149430 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 444 4 4 6 3.3 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCCNC2)c1O nan
CHEMBL3949893 149430 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 444 4 4 6 3.3 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCCNC2)c1O nan
57649043 149467 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 475 4 4 7 3.1 O=C(Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CCNC2)c1O)Nc1cccc2c1OC(F)(F)O2 nan
CHEMBL3950195 149467 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 475 4 4 7 3.1 O=C(Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CCNC2)c1O)Nc1cccc2c1OC(F)(F)O2 nan
50996243 149483 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 493 6 4 6 4.0 O=C(Nc1ccccc1OC(F)(F)F)Nc1ccc(Cl)c(S(=O)(=O)CC2CCNC2)c1O nan
CHEMBL3950351 149483 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 493 6 4 6 4.0 O=C(Nc1ccccc1OC(F)(F)F)Nc1ccc(Cl)c(S(=O)(=O)CC2CCNC2)c1O nan
50996423 149600 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 493 5 4 6 4.1 O=C(Nc1ccccc1OC(F)(F)F)Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O nan
CHEMBL3951311 149600 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 493 5 4 6 4.1 O=C(Nc1ccccc1OC(F)(F)F)Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O nan
50996246 149754 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 433 4 4 5 3.2 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CNC2)c1O)Nc1cccc(F)c1Cl nan
CHEMBL3952713 149754 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 433 4 4 5 3.2 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CNC2)c1O)Nc1cccc(F)c1Cl nan
57649026 149781 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 467 4 4 5 4.2 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2C[C@@H]3CC[C@H](C2)N3)c1O nan
CHEMBL3952903 149781 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 467 4 4 5 4.2 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2C[C@@H]3CC[C@H](C2)N3)c1O nan
50996244 149803 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 416 4 4 6 2.5 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)C2CNC2)c1O nan
CHEMBL3953055 149803 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 416 4 4 6 2.5 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)C2CNC2)c1O nan
50995536 149901 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 441 4 4 5 3.7 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O nan
CHEMBL3953988 149901 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 441 4 4 5 3.7 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CCCNC2)c1O nan
50996776 150365 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 573 7 3 7 5.9 CCOC(=O)N1CCC(S(=O)(=O)c2c(Cl)ccc(NC(=O)Nc3ccccc3Oc3ccccc3)c2O)CC1 nan
CHEMBL3957549 150365 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 573 7 3 7 5.9 CCOC(=O)N1CCC(S(=O)(=O)c2c(Cl)ccc(NC(=O)Nc3ccccc3Oc3ccccc3)c2O)CC1 nan
24780600 150690 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 461 4 4 5 4.0 O=C(Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCCNC2)c1O)Nc1cccc(F)c1Cl nan
CHEMBL3960024 150690 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 461 4 4 5 4.0 O=C(Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCCNC2)c1O)Nc1cccc(F)c1Cl nan
57649038 151424 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 447 4 4 5 3.6 O=C(Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CCNC2)c1O)Nc1cccc(F)c1Cl nan
CHEMBL3966527 151424 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 447 4 4 5 3.6 O=C(Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CCNC2)c1O)Nc1cccc(F)c1Cl nan
50996425 151561 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 461 4 4 5 4.0 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O)Nc1cccc(F)c1Cl nan
CHEMBL3967642 151561 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 461 4 4 5 4.0 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O)Nc1cccc(F)c1Cl nan
50996426 151851 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 441 4 4 5 3.7 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O nan
CHEMBL3970321 151851 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 441 4 4 5 3.7 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2CCNCC2)c1O nan
57649032 151975 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 427 4 4 5 3.3 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCNC2)c1O nan
CHEMBL3971309 151975 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 427 4 4 5 3.3 Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCNC2)c1O nan
57649036 152286 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 430 4 4 6 2.9 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCNC2)c1O nan
CHEMBL3973880 152286 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assayAntagonist activity at CXCR2 (unknown origin) expressed in CHO-K1 cells co-expressing Galpha-16 assessed as inhibition of IL8-induced calcium mobilization measured after 10 mins by Fluo-4AM dye based FLIPR assay
ChEMBL 430 4 4 6 2.9 O=C(Nc1cccnc1Cl)Nc1ccc(Cl)c(S(=O)(=O)[C@H]2CCNC2)c1O nan
24879232 154816 0 None 43 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 428 7 2 4 3.1 CN(C)S(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
CHEMBL403313 154816 0 None 43 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 428 7 2 4 3.1 CN(C)S(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
135964204 112464 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 283 4 1 5 3.2 N#Cc1c(O)nc(SCc2ccccc2)nc1C1CC1 10.1016/j.bmcl.2014.06.011
CHEMBL3310789 112464 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 283 4 1 5 3.2 N#Cc1c(O)nc(SCc2ccccc2)nc1C1CC1 10.1016/j.bmcl.2014.06.011
24958936 104171 2 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 376 4 1 6 4.4 Oc1cc(CSc2cccc(F)c2F)nc2nc(C3CCCCC3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3105077 104171 2 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 376 4 1 6 4.4 Oc1cc(CSc2cccc(F)c2F)nc2nc(C3CCCCC3)nn12 10.1016/j.bmcl.2013.11.074
91937330 114430 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 365 6 3 6 1.7 O=C(Nc1ccncc1)c1ccc(SCc2ccccc2B(O)O)nc1 10.1021/jm500827t
CHEMBL3342317 114430 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 365 6 3 6 1.7 O=C(Nc1ccncc1)c1ccc(SCc2ccccc2B(O)O)nc1 10.1021/jm500827t
11371755 87543 0 None 109 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 357 1 3 5 3.3 O=S1(=O)N=C(Nc2ccccc2Cl)Nc2c(O)cc(Cl)cc21 10.1016/j.bmcl.2007.05.011
CHEMBL234186 87543 0 None 109 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 357 1 3 5 3.3 O=S1(=O)N=C(Nc2ccccc2Cl)Nc2c(O)cc(Cl)cc21 10.1016/j.bmcl.2007.05.011
45485757 195833 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 394 7 3 7 2.3 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccccc1 10.1016/j.bmcl.2009.08.014
CHEMBL570042 195833 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 394 7 3 7 2.3 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccccc1 10.1016/j.bmcl.2009.08.014
162652658 179858 0 None 407 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 441 4 3 6 3.5 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3Cl)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4752486 179858 0 None 407 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 441 4 3 6 3.5 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3Cl)N2)c1O 10.1021/acsmedchemlett.1c00113
46896680 114419 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 332 5 1 4 3.7 O=C(Nc1ccc(F)cc1)c1ccc(SCC2CCCO2)nc1 10.1021/jm500827t
CHEMBL3342282 114419 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 332 5 1 4 3.7 O=C(Nc1ccc(F)cc1)c1ccc(SCC2CCCO2)nc1 10.1021/jm500827t
44447944 155088 0 None -38 2 Rabbit 5.2 pIC50 = 5.2 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 453 5 3 3 3.5 CS(=O)(=O)NC(=O)NCCc1c(-c2ccc(F)cc2)[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2008.01.127
CHEMBL404661 155088 0 None -38 2 Rabbit 5.2 pIC50 = 5.2 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 453 5 3 3 3.5 CS(=O)(=O)NC(=O)NCCc1c(-c2ccc(F)cc2)[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2008.01.127
CHEMBL5075579 212613 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccc(Cl)cc1Cl)Nc1ccc2c(c1O)S(=O)(=O)CC=C2 10.1021/acs.jmedchem.1c01219
135949064 112462 1 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 349 5 2 6 2.7 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1[C@H]1C[C@@H]1CO 10.1016/j.bmcl.2014.06.011
CHEMBL3310787 112462 1 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 349 5 2 6 2.7 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1[C@H]1C[C@@H]1CO 10.1016/j.bmcl.2014.06.011
162667668 181852 0 None 776 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 407 4 3 6 2.9 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4786074 181852 0 None 776 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 407 4 3 6 2.9 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3)N2)c1O 10.1021/acsmedchemlett.1c00113
46897162 3659 7 None 6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CVCL8-induced [35S]GTPgammaS binding after 60 minsAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CVCL8-induced [35S]GTPgammaS binding after 60 mins
ChEMBL 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 10.1021/jm500827t
8501 3659 7 None 6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CVCL8-induced [35S]GTPgammaS binding after 60 minsAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CVCL8-induced [35S]GTPgammaS binding after 60 mins
ChEMBL 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 10.1021/jm500827t
CHEMBL3342269 3659 7 None 6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CVCL8-induced [35S]GTPgammaS binding after 60 minsAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CVCL8-induced [35S]GTPgammaS binding after 60 mins
ChEMBL 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 10.1021/jm500827t
11750288 169006 0 None 25 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 412 2 3 7 2.6 O=[N+]([O-])c1cc(O)c2c(c1)S(=O)(=O)N=C(Nc1ccccc1Br)N2 10.1016/j.bmcl.2007.05.011
CHEMBL443583 169006 0 None 25 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPRAntagonist activity at CXCR2 receptor expressed in CHOK1 cells assessed as human IL8-induced calcium mobilization by FLIPR
ChEMBL 412 2 3 7 2.6 O=[N+]([O-])c1cc(O)c2c(c1)S(=O)(=O)N=C(Nc1ccccc1Br)N2 10.1016/j.bmcl.2007.05.011
23642171 126293 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 397 8 2 4 4.5 CC(C)(NC(=O)c1ccc2ccsc2c1OCCCc1ccccc1)C(=O)O nan
CHEMBL3654437 126293 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 397 8 2 4 4.5 CC(C)(NC(=O)c1ccc2ccsc2c1OCCCc1ccccc1)C(=O)O nan
57831224 125321 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Calicum Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes).Calicum Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes).
ChEMBL 523 7 2 5 5.5 O=C(NC1(C(=O)O)CCOCC1)c1cc(F)c2ccccc2c1OCc1ccc(SC(F)(F)F)cc1 nan
CHEMBL3648348 125321 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Calicum Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes).Calicum Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes).
ChEMBL 523 7 2 5 5.5 O=C(NC1(C(=O)O)CCOCC1)c1cc(F)c2ccccc2c1OCc1ccc(SC(F)(F)F)cc1 nan
45485788 195694 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 426 8 3 7 2.4 CCN(Cc1ccc(F)cc1)Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O 10.1016/j.bmcl.2009.08.014
CHEMBL569210 195694 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 426 8 3 7 2.4 CCN(Cc1ccc(F)cc1)Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O 10.1016/j.bmcl.2009.08.014
136074343 112466 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 311 4 1 5 4.0 CC(C)(Sc1nc(O)c(C#N)c(C2CC2)n1)c1ccccc1 10.1016/j.bmcl.2014.06.011
CHEMBL3310791 112466 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 311 4 1 5 4.0 CC(C)(Sc1nc(O)c(C#N)c(C2CC2)n1)c1ccccc1 10.1016/j.bmcl.2014.06.011
24959665 104161 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 432 6 1 7 4.6 Oc1cc(CSc2cccc(OC(F)(F)F)c2)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3104908 104161 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 432 6 1 7 4.6 Oc1cc(CSc2cccc(OC(F)(F)F)c2)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
122187271 122504 0 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 447 8 3 8 1.7 O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccc(B(O)O)cn2)Cc2ccco2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609021 122504 0 None -1 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 447 8 3 8 1.7 O=C(Nc1ccc(F)cc1)c1cnc(N(Cc2ccc(B(O)O)cn2)Cc2ccco2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL5078788 212814 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=C(Nc1ccccc1Cl)Nc1ccc2c(c1O)S(=O)(=O)CC=C2 10.1021/acs.jmedchem.1c01219
162673727 182401 0 None 218 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 373 5 3 6 2.3 CCCC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
CHEMBL4793352 182401 0 None 218 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 373 5 3 6 2.3 CCCC1NC(Nc2ccc(Cl)c(S(=O)(=O)C(C)C)c2O)=NC1=O 10.1021/acsmedchemlett.1c00113
136074341 112463 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 362 5 2 6 2.2 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1[C@H]1C[C@@H]1C(N)=O 10.1016/j.bmcl.2014.06.011
CHEMBL3310788 112463 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 362 5 2 6 2.2 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1[C@H]1C[C@@H]1C(N)=O 10.1016/j.bmcl.2014.06.011
44447923 95023 0 None 38 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 453 6 2 4 4.1 N#Cc1ccc2[nH]c(-c3ccc(F)cc3)c(CCCC(=O)NS(=O)(=O)C(F)(F)F)c2c1 10.1016/j.bmcl.2008.01.127
CHEMBL257178 95023 0 None 38 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 453 6 2 4 4.1 N#Cc1ccc2[nH]c(-c3ccc(F)cc3)c(CCCC(=O)NS(=O)(=O)C(F)(F)F)c2c1 10.1016/j.bmcl.2008.01.127
CHEMBL5081756 212992 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=c1c(Nc2ccc3c(c2O)S(=O)(=O)CC=C3)c(Nc2cccc(F)c2Cl)c1=O 10.1021/acs.jmedchem.1c01219
24879232 154816 0 None -43 2 Rabbit 6.2 pIC50 = 6.2 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 428 7 2 4 3.1 CN(C)S(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
CHEMBL403313 154816 0 None -43 2 Rabbit 6.2 pIC50 = 6.2 Functional
Antagonist activity at rabbit CXCR2 by neutrophil chemotaxis assayAntagonist activity at rabbit CXCR2 by neutrophil chemotaxis assay
ChEMBL 428 7 2 4 3.1 CN(C)S(=O)(=O)NC(=O)CCCc1c(-c2ccc(F)cc2)[nH]c2ccc(C#N)cc12 10.1016/j.bmcl.2008.01.127
135907759 112448 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 385 5 1 6 4.3 COc1ccc(-c2nc(SCc3cccc(F)c3F)nc(O)c2C#N)cc1 10.1016/j.bmcl.2014.06.011
CHEMBL3310774 112448 1 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 385 5 1 6 4.3 COc1ccc(-c2nc(SCc3cccc(F)c3F)nc(O)c2C#N)cc1 10.1016/j.bmcl.2014.06.011
122187254 122488 0 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 365 6 4 5 1.8 O=C(Nc1ccc(F)cc1)c1ccc(NCc2cccc(B(O)O)c2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609002 122488 0 None -1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 365 6 4 5 1.8 O=C(Nc1ccc(F)cc1)c1ccc(NCc2cccc(B(O)O)c2)nc1 10.1016/j.bmcl.2015.07.090
135907766 112446 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 389 4 1 5 4.9 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.06.011
CHEMBL3310772 112446 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 389 4 1 5 4.9 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2014.06.011
45485784 197360 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 395 7 3 8 1.7 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccccn1 10.1016/j.bmcl.2009.08.014
CHEMBL585928 197360 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 395 7 3 8 1.7 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccccn1 10.1016/j.bmcl.2009.08.014
46897356 114425 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 396 6 1 5 4.6 COC(=O)c1ccccc1CSc1ccc(C(=O)Nc2ccc(F)cc2)cn1 10.1021/jm500827t
CHEMBL3342310 114425 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 396 6 1 5 4.6 COC(=O)c1ccccc1CSc1ccc(C(=O)Nc2ccc(F)cc2)cn1 10.1021/jm500827t
1163244 181114 3 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of CXCR2 (unknown origin) expressed in HEK293T cells cotransfected with GFP-p22F assessed as reduction in IL-8-induced cAMP incubated for 10 mins followed by IL-8 stimulation and measured after 10 mins by luminescence based assayInhibition of CXCR2 (unknown origin) expressed in HEK293T cells cotransfected with GFP-p22F assessed as reduction in IL-8-induced cAMP incubated for 10 mins followed by IL-8 stimulation and measured after 10 mins by luminescence based assay
ChEMBL 382 2 0 7 4.3 CSc1nnc2n(-c3ccccc3)c(=O)c3c4c(sc3n12)CCC[C@H]4C 10.1016/j.ejmech.2020.112387
CHEMBL4776704 181114 3 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of CXCR2 (unknown origin) expressed in HEK293T cells cotransfected with GFP-p22F assessed as reduction in IL-8-induced cAMP incubated for 10 mins followed by IL-8 stimulation and measured after 10 mins by luminescence based assayInhibition of CXCR2 (unknown origin) expressed in HEK293T cells cotransfected with GFP-p22F assessed as reduction in IL-8-induced cAMP incubated for 10 mins followed by IL-8 stimulation and measured after 10 mins by luminescence based assay
ChEMBL 382 2 0 7 4.3 CSc1nnc2n(-c3ccccc3)c(=O)c3c4c(sc3n12)CCC[C@H]4C 10.1016/j.ejmech.2020.112387
59446384 114433 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 473 8 2 6 3.4 O=C(c1ccc(SCc2ccccc2B(O)O)nc1)N(Cc1ccccn1)c1ccc(F)cc1 10.1021/jm500827t
CHEMBL3342320 114433 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 473 8 2 6 3.4 O=C(c1ccc(SCc2ccccc2B(O)O)nc1)N(Cc1ccccn1)c1ccc(F)cc1 10.1021/jm500827t
CHEMBL5070965 212479 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=c1c(Nc2ccccc2Br)c(Nc2ccc3c(c2O)S(=O)(=O)CC=C3)c1=O 10.1021/acs.jmedchem.1c01219
135907763 112451 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 371 4 2 6 4.0 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1-c1ccc(O)cc1 10.1016/j.bmcl.2014.06.011
CHEMBL3310777 112451 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 371 4 2 6 4.0 N#Cc1c(O)nc(SCc2cccc(F)c2F)nc1-c1ccc(O)cc1 10.1016/j.bmcl.2014.06.011
990571 171910 2 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at GFP-tagged CXCR2 (unknown origin) expressed in 293T cells assessed as suppression of IL-8-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by IL-8 addition and measured after 10 mins by cAMP assayAntagonist activity at GFP-tagged CXCR2 (unknown origin) expressed in 293T cells assessed as suppression of IL-8-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by IL-8 addition and measured after 10 mins by cAMP assay
ChEMBL 396 3 0 7 4.6 CCSc1nnc2n(-c3ccccc3)c(=O)c3c4c(sc3n12)CCC[C@H]4C 10.1016/j.ejmech.2019.111853
CHEMBL4482876 171910 2 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at GFP-tagged CXCR2 (unknown origin) expressed in 293T cells assessed as suppression of IL-8-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by IL-8 addition and measured after 10 mins by cAMP assayAntagonist activity at GFP-tagged CXCR2 (unknown origin) expressed in 293T cells assessed as suppression of IL-8-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by IL-8 addition and measured after 10 mins by cAMP assay
ChEMBL 396 3 0 7 4.6 CCSc1nnc2n(-c3ccccc3)c(=O)c3c4c(sc3n12)CCC[C@H]4C 10.1016/j.ejmech.2019.111853
24959666 104160 2 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 410 5 1 6 5.0 Cc1cc(SCc2cc(O)n3nc(Cc4ccccc4)nc3n2)c(C)cc1Cl 10.1016/j.bmcl.2013.11.074
CHEMBL3104907 104160 2 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 410 5 1 6 5.0 Cc1cc(SCc2cc(O)n3nc(Cc4ccccc4)nc3n2)c(C)cc1Cl 10.1016/j.bmcl.2013.11.074
24970254 126294 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 417 8 2 5 4.1 CC(C)(NC(=O)c1ccc2ccsc2c1OCCOc1ccc(F)cc1)C(=O)O nan
CHEMBL3654438 126294 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.Calcium Fluorescence Assay: The assay is based on the detection of intracellular calcium changes detected by the selective, calcium-chelating dye, Fluo-4 (Molecular Probes). A large fluorescence intensity increase is observed upon calcium association with Fluo-4. The dye is delivered to the cell interior using an acetoxymethylester form of Fluo-4, where the intracellular esterase activity results in the charged species being released and trapped within the cytoplasm of the cell. hence, influx of calcium to this cytoplasmic pocket, via release from intracellular pools and the phospholipase C cascade can be detected. By co-expressing the CXCR2 receptor and the promiscuous Galpha 16 protein, activation of this chemokine receptor is directed into this phospholipase C cascade resulting in intracellular calcium mobilization.The CHOK1 cells stably transfected with human CXCR2 and the promiscuous Galpha 16 protein were maintained in a log phase of growth at 37 C. and 5% CO2 in the following media: Iscove's.
ChEMBL 417 8 2 5 4.1 CC(C)(NC(=O)c1ccc2ccsc2c1OCCOc1ccc(F)cc1)C(=O)O nan
122187257 122492 0 None 20 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 380 6 3 6 1.2 CN(Cc1ccc(B(O)O)cn1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
CHEMBL3609006 122492 0 None 20 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 380 6 3 6 1.2 CN(Cc1ccc(B(O)O)cn1)c1ccc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
24952757 104179 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 293 3 1 5 3.0 Oc1cc(CSc2cccc(F)c2F)nc2ccnn12 10.1016/j.bmcl.2013.11.074
CHEMBL3105085 104179 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 293 3 1 5 3.0 Oc1cc(CSc2cccc(F)c2F)nc2ccnn12 10.1016/j.bmcl.2013.11.074
24958937 104155 4 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 348 5 1 6 3.7 Oc1cc(CSc2ccccc2)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3104900 104155 4 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 348 5 1 6 3.7 Oc1cc(CSc2ccccc2)nc2nc(Cc3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
45485758 195834 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 412 7 3 7 2.4 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccc(F)cc1 10.1016/j.bmcl.2009.08.014
CHEMBL570043 195834 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 412 7 3 7 2.4 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccc(F)cc1 10.1016/j.bmcl.2009.08.014
45485798 196937 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 440 7 3 7 2.1 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)C(=O)c1ccc(F)cc1 10.1016/j.bmcl.2009.08.014
CHEMBL578807 196937 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxisAntagonist activity at CXCR2 expressed in CHO cells assessed as inhibition of IL-8-induced chemotaxis
ChEMBL 440 7 3 7 2.1 CCN(Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)C(=O)c1ccc(F)cc1 10.1016/j.bmcl.2009.08.014
24958935 104172 4 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 370 4 1 6 4.1 Oc1cc(CSc2cccc(F)c2F)nc2nc(-c3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
CHEMBL3105078 104172 4 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 370 4 1 6 4.1 Oc1cc(CSc2cccc(F)c2F)nc2nc(-c3ccccc3)nn12 10.1016/j.bmcl.2013.11.074
24953816 104176 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 373 4 1 6 4.6 Cc1ccoc1-c1cc2nc(CSc3cccc(F)c3F)cc(O)n2n1 10.1016/j.bmcl.2013.11.074
CHEMBL3105082 104176 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 373 4 1 6 4.6 Cc1ccoc1-c1cc2nc(CSc3cccc(F)c3F)cc(O)n2n1 10.1016/j.bmcl.2013.11.074
91937333 114434 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 473 8 2 6 3.4 O=C(c1ccc(SCc2ccccc2B(O)O)nc1)N(Cc1ccncc1)c1ccc(F)cc1 10.1021/jm500827t
CHEMBL3342321 114434 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assayAntagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay
ChEMBL 473 8 2 6 3.4 O=C(c1ccc(SCc2ccccc2B(O)O)nc1)N(Cc1ccncc1)c1ccc(F)cc1 10.1021/jm500827t
162659583 180795 0 None 602 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 423 6 3 7 2.1 COCCS(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4763312 180795 0 None 602 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 423 6 3 7 2.1 COCCS(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccccc3)N2)c1O 10.1021/acsmedchemlett.1c00113
44447944 155088 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 453 5 3 3 3.5 CS(=O)(=O)NC(=O)NCCc1c(-c2ccc(F)cc2)[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2008.01.127
CHEMBL404661 155088 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human cloned CXCR2 by calcium flux FLIPR assayAntagonist activity at human cloned CXCR2 by calcium flux FLIPR assay
ChEMBL 453 5 3 3 3.5 CS(=O)(=O)NC(=O)NCCc1c(-c2ccc(F)cc2)[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2008.01.127
135907782 112455 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 321 4 1 5 3.7 CC(C)c1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
CHEMBL3310780 112455 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assayAntagonist activity against human recombinant CXCR2 receptor expressed in CHO cell membranes by SPA based [35S]GTPgammaS binding assay
ChEMBL 321 4 1 5 3.7 CC(C)c1nc(SCc2cccc(F)c2F)nc(O)c1C#N 10.1016/j.bmcl.2014.06.011
24958574 104167 4 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 336 4 1 6 3.5 CC(C)c1nc2nc(CSc3cccc(F)c3F)cc(O)n2n1 10.1016/j.bmcl.2013.11.074
CHEMBL3104914 104167 4 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA methodAntagonist activity at human recombinant CXCR2 receptor expressed in CHO cells assessed as inhibition of IL8-induced [35S]GTPgammaS binding by SPA method
ChEMBL 336 4 1 6 3.5 CC(C)c1nc2nc(CSc3cccc(F)c3F)cc(O)n2n1 10.1016/j.bmcl.2013.11.074
162656425 180297 0 None 41 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 441 4 3 6 3.5 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccc(Cl)cc3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4757462 180297 0 None 41 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 441 4 3 6 3.5 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)C(c3ccc(Cl)cc3)N2)c1O 10.1021/acsmedchemlett.1c00113
122187259 122493 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 366 6 4 6 1.2 O=C(Nc1ccc(F)cc1)c1cnc(NCc2cccc(B(O)O)c2)nc1 10.1016/j.bmcl.2015.07.090
CHEMBL3609008 122493 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 366 6 4 6 1.2 O=C(Nc1ccc(F)cc1)c1cnc(NCc2cccc(B(O)O)c2)nc1 10.1016/j.bmcl.2015.07.090
24768854 124654 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 431 8 2 3 5.4 CC(CCc1ccccc1)Oc1c(C(=O)NC2(C(=O)O)CCCC2)ccc2ccccc12 nan
CHEMBL3645131 124654 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).Calcium Fluorescence Assay (FLIPR) : CXCR2 inhibition using calcium fluorescence assay (FLIPR).
ChEMBL 431 8 2 3 5.4 CC(CCc1ccccc1)Oc1c(C(=O)NC2(C(=O)O)CCCC2)ccc2ccccc12 nan
122187262 122497 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 381 6 3 7 0.6 CN(Cc1ccc(B(O)O)cn1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
CHEMBL3609012 122497 0 None 1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysisAntagonist activity at CXCR2 (unknown origin) transfected in RBL cells assessed as inhibition of IL-8-mediated intracellular calcium release preincubated for 30 mins followed by IL-8 addition by FLUO-4AM-based fluorescent microplate reader analysis
ChEMBL 381 6 3 7 0.6 CN(Cc1ccc(B(O)O)cn1)c1ncc(C(=O)Nc2ccc(F)cc2)cn1 10.1016/j.bmcl.2015.07.090
CHEMBL5093947 213684 3 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None Cc1c(F)cccc1NC(=O)Nc1ccc2c(c1O)S(=O)(=O)CCC2 10.1021/acs.jmedchem.1c01219
162646248 178988 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 421 5 3 6 2.7 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@@H](Cc3ccccc3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL4741864 178988 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assayAntagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 421 5 3 6 2.7 CC(C)S(=O)(=O)c1c(Cl)ccc(NC2=NC(=O)[C@@H](Cc3ccccc3)N2)c1O 10.1021/acsmedchemlett.1c00113
CHEMBL5084752 213160 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assayAntagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced beta-arrestin recruitment preincubated for 30 mins followed by addition of agonist incubated for 90 mins by beta arrestin assay
ChEMBL None None None O=c1c(Nc2ccc3c(c2O)S(=O)(=O)CCC3)c(Nc2cccc(Cl)c2Cl)c1=O 10.1021/acs.jmedchem.1c01219
11440492 152110 0 None - 1 Human 9.0 pKd = 9 Functional
Antagonistic activity against human CXCR2 in neutrophils assessed as blockade of GROalpha stimulated calcium mobilisation by FLIPRAntagonistic activity against human CXCR2 in neutrophils assessed as blockade of GROalpha stimulated calcium mobilisation by FLIPR
ChEMBL 383 6 3 8 3.0 C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2nc(N)sc12 10.1016/j.bmcl.2007.02.080
CHEMBL397237 152110 0 None - 1 Human 9.0 pKd = 9 Functional
Antagonistic activity against human CXCR2 in neutrophils assessed as blockade of GROalpha stimulated calcium mobilisation by FLIPRAntagonistic activity against human CXCR2 in neutrophils assessed as blockade of GROalpha stimulated calcium mobilisation by FLIPR
ChEMBL 383 6 3 8 3.0 C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2nc(N)sc12 10.1016/j.bmcl.2007.02.080
12073810 170986 8 None - 1 Human 8.9 pKd = 8.9 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 384 6 3 7 2.7 C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2[nH]c(=O)sc12 10.1016/j.bmcl.2015.01.067
CHEMBL446458 170986 8 None - 1 Human 8.9 pKd = 8.9 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 384 6 3 7 2.7 C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2[nH]c(=O)sc12 10.1016/j.bmcl.2015.01.067
10003645 117536 1 None - 1 Human 8.7 pKd = 8.7 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 445 9 3 7 2.2 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCC2)nc(SCc2cccc(F)c2F)n1 10.1016/j.bmcl.2015.01.067
CHEMBL3403850 117536 1 None - 1 Human 8.7 pKd = 8.7 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 445 9 3 7 2.2 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCC2)nc(SCc2cccc(F)c2F)n1 10.1016/j.bmcl.2015.01.067
10479451 117537 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 461 9 3 7 2.7 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCC2)nc(SCc2cccc(Cl)c2F)n1 10.1016/j.bmcl.2015.01.067
CHEMBL3403851 117537 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 461 9 3 7 2.7 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCC2)nc(SCc2cccc(Cl)c2F)n1 10.1016/j.bmcl.2015.01.067
11754699 117540 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 475 9 3 8 1.8 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCOCC2)nc(SCc2cccc(F)c2F)n1 10.1016/j.bmcl.2015.01.067
CHEMBL3403854 117540 0 None - 1 Human 8.0 pKd = 8 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 475 9 3 8 1.8 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCOCC2)nc(SCc2cccc(F)c2F)n1 10.1016/j.bmcl.2015.01.067
10072910 117538 0 None - 1 Human 7.9 pKd = 7.9 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 459 9 3 7 2.6 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCCC2)nc(SCc2cccc(F)c2F)n1 10.1016/j.bmcl.2015.01.067
CHEMBL3403852 117538 0 None - 1 Human 7.9 pKd = 7.9 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 459 9 3 7 2.6 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCCC2)nc(SCc2cccc(F)c2F)n1 10.1016/j.bmcl.2015.01.067
11440492 152110 0 None - 1 Human 7.9 pKd = 7.9 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 383 6 3 8 3.0 C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2nc(N)sc12 10.1016/j.bmcl.2015.01.067
CHEMBL397237 152110 0 None - 1 Human 7.9 pKd = 7.9 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 383 6 3 8 3.0 C[C@H](CO)Nc1nc(SCc2cccc(F)c2F)nc2nc(N)sc12 10.1016/j.bmcl.2015.01.067
10050534 117539 0 None - 1 Human 7.8 pKd = 7.8 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 473 9 3 7 3.0 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCCCC2)nc(SCc2cccc(F)c2F)n1 10.1016/j.bmcl.2015.01.067
CHEMBL3403853 117539 0 None - 1 Human 7.8 pKd = 7.8 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 473 9 3 7 3.0 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCCCC2)nc(SCc2cccc(F)c2F)n1 10.1016/j.bmcl.2015.01.067
57833185 117541 0 None - 1 Human 7.8 pKd = 7.8 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 491 9 3 8 2.3 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCOCC2)nc(SCc2cccc(Cl)c2F)n1 10.1016/j.bmcl.2015.01.067
CHEMBL3403855 117541 0 None - 1 Human 7.8 pKd = 7.8 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 491 9 3 8 2.3 C[C@H](CO)Nc1cc(NS(=O)(=O)N2CCOCC2)nc(SCc2cccc(Cl)c2F)n1 10.1016/j.bmcl.2015.01.067
10345330 117533 0 None - 1 Human 6.7 pKd = 6.7 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 486 9 3 9 2.9 C[C@H](CO)Nc1cc(NS(=O)(=O)c2cn(C)cn2)nc(SCc2cccc(Cl)c2F)n1 10.1016/j.bmcl.2015.01.067
CHEMBL3403847 117533 0 None - 1 Human 6.7 pKd = 6.7 Functional
Antagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysisAntagonist activity at CXCR2 receptor in HEK293 cells assessed as mobilization of intracellular calcium by FLIPR analysis
ChEMBL 486 9 3 9 2.9 C[C@H](CO)Nc1cc(NS(=O)(=O)c2cn(C)cn2)nc(SCc2cccc(Cl)c2F)n1 10.1016/j.bmcl.2015.01.067
8497 2697 52 None 1 3 Human 10.3 pIC50 = 10.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 17181143
8497 2697 52 None 1 3 Human 10.3 pIC50 = 10.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 24218476
9865554 2697 52 None 1 3 Human 10.3 pIC50 = 10.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 17181143
9865554 2697 52 None 1 3 Human 10.3 pIC50 = 10.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 24218476
CHEMBL216981 2697 52 None 1 3 Human 10.3 pIC50 = 10.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 17181143
CHEMBL216981 2697 52 None 1 3 Human 10.3 pIC50 = 10.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 24218476
8498 3263 46 None -33 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 283 5 1 3 2.1 CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C 15282370
9838712 3263 46 None -33 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 283 5 1 3 2.1 CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C 15282370
CHEMBL191413 3263 46 None -33 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 283 5 1 3 2.1 CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C 15282370
DB12614 3263 46 None -33 2 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 283 5 1 3 2.1 CC(Cc1ccc(cc1)[C@H](C(=O)NS(=O)(=O)C)C)C 15282370
46897162 3659 7 None 6 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 25254640
8501 3659 7 None 6 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 25254640
CHEMBL3342269 3659 7 None 6 2 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 382 6 3 5 2.4 Fc1ccc(cc1)NC(=O)c1ccc(nc1)SCc1ccccc1B(O)O 25254640
10479502 1519 15 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 24218476
8499 1519 15 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 24218476
CHEMBL2178579 1519 15 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 24218476
DB12135 1519 15 None - 1 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 462 4 4 5 3.1 O=C(Nc1cccc(c1Cl)F)Nc1ccc(c(c1O)S(=O)(=O)N1CCNCC1)Cl 24218476
3854666 3445 78 None -1 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 9553055
833 3445 78 None -1 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 9553055
CHEMBL239767 3445 78 None -1 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 3 3 4 3.7 O=C(Nc1ccccc1Br)Nc1ccc(cc1O)[N+](=O)[O-] 9553055
830 1238 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702798
24780598 1289 33 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 4 4 5 3.7 O=C(Nc1cccc(c1C)F)Nc1ccc(c(c1O)S(=O)(=O)[C@H]1CCCNC1)Cl 26092545
8500 1289 33 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 4 4 5 3.7 O=C(Nc1cccc(c1C)F)Nc1ccc(c(c1O)S(=O)(=O)[C@H]1CCCNC1)Cl 26092545
CHEMBL3039531 1289 33 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 4 4 5 3.7 O=C(Nc1cccc(c1C)F)Nc1ccc(c(c1O)S(=O)(=O)[C@H]1CCCNC1)Cl 26092545
DB11922 1289 33 None - 1 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 441 4 4 5 3.7 O=C(Nc1cccc(c1C)F)Nc1ccc(c(c1O)S(=O)(=O)[C@H]1CCCNC1)Cl 26092545
829 1234 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702798
827 1228 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702798
8496 3916 0 None 7 2 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20044480
828 1232 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8702798
3618472 2849 17 None 45 2 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 273 3 3 4 2.9 O=C(Nc1ccc(cc1O)[N+](=O)[O-])Nc1ccccc1 9553055
834 2849 17 None 45 2 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 273 3 3 4 2.9 O=C(Nc1ccc(cc1O)[N+](=O)[O-])Nc1ccccc1 9553055
CHEMBL280711 2849 17 None 45 2 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 273 3 3 4 2.9 O=C(Nc1ccc(cc1O)[N+](=O)[O-])Nc1ccccc1 9553055




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
8497 2697 52 None 4 2 Human 10.3 pIC50 = 10.3 Binding
Binding affinity to CXCR2Binding affinity to CXCR2
ChEMBL 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 10.1021/jm300682j
9865554 2697 52 None 4 2 Human 10.3 pIC50 = 10.3 Binding
Binding affinity to CXCR2Binding affinity to CXCR2
ChEMBL 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 10.1021/jm300682j
CHEMBL216981 2697 52 None 4 2 Human 10.3 pIC50 = 10.3 Binding
Binding affinity to CXCR2Binding affinity to CXCR2
ChEMBL 397 7 3 7 2.9 CC[C@H](c1ccc(o1)C)NC1=C(C(=O)C1=O)Nc1cccc(c1O)C(=O)N(C)C 10.1021/jm300682j
11372270 67164 18 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of CXCR2 (unknown origin)Inhibition of CXCR2 (unknown origin)
ChEMBL 375 5 1 6 1.1 C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 10.1021/acs.jmedchem.8b00875
CHEMBL189475 67164 18 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of CXCR2 (unknown origin)Inhibition of CXCR2 (unknown origin)
ChEMBL 375 5 1 6 1.1 C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 10.1021/acs.jmedchem.8b00875
CHEMBL4442431 67164 18 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of CXCR2 (unknown origin)Inhibition of CXCR2 (unknown origin)
ChEMBL 375 5 1 6 1.1 C[C@@H](C(=O)NS(C)(=O)=O)c1ccc(OS(=O)(=O)C(F)(F)F)cc1 10.1021/acs.jmedchem.8b00875
88545431 170827 0 None - 0 Mouse 10.0 pIC50 = 10 Binding
Inhibition of CXCR2-mediated chemotaxis in mouse BAF3 cellsInhibition of CXCR2-mediated chemotaxis in mouse BAF3 cells
ChEMBL 478 7 3 8 3.1 CC[C@@H](Nc1c(Nc2cccc(C(=O)N3CCN4CCC[C@H]4C3)c2O)c(=O)c1=O)c1ccc(C)o1 10.1016/j.ejmech.2019.111853
CHEMBL4462143 170827 0 None - 0 Mouse 10.0 pIC50 = 10 Binding
Inhibition of CXCR2-mediated chemotaxis in mouse BAF3 cellsInhibition of CXCR2-mediated chemotaxis in mouse BAF3 cells
ChEMBL 478 7 3 8 3.1 CC[C@@H](Nc1c(Nc2cccc(C(=O)N3CCN4CCC[C@H]4C3)c2O)c(=O)c1=O)c1ccc(C)o1 10.1016/j.ejmech.2019.111853
44626319 196744 0 None 81 2 Human 9.9 pIC50 = 9.9 Binding
Antagonist activity at CXCR2 (unknown origin)Antagonist activity at CXCR2 (unknown origin)
ChEMBL 346 7 3 7 1.1 CCN(CC)Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O 10.1016/j.ejmech.2019.111853
CHEMBL577075 196744 0 None 81 2 Human 9.9 pIC50 = 9.9 Binding
Antagonist activity at CXCR2 (unknown origin)Antagonist activity at CXCR2 (unknown origin)
ChEMBL 346 7 3 7 1.1 CCN(CC)Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O 10.1016/j.ejmech.2019.111853
137633598 155890 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 445 5 3 5 4.0 CC1=CCC[C@H]1NC(=O)Nc1ccc(C#N)c(S(=O)(=O)C(C)(C)CC(F)(F)F)c1O 10.1021/acs.jmedchem.7b01854
CHEMBL4066904 155890 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 445 5 3 5 4.0 CC1=CCC[C@H]1NC(=O)Nc1ccc(C#N)c(S(=O)(=O)C(C)(C)CC(F)(F)F)c1O 10.1021/acs.jmedchem.7b01854
118540892 157186 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 377 3 3 5 3.1 CC1=CCC[C@H]1NC(=O)Nc1ccc(C#N)c(S(=O)(=O)C(C)(C)C)c1O 10.1021/acs.jmedchem.7b01854
CHEMBL4082136 157186 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 377 3 3 5 3.1 CC1=CCC[C@H]1NC(=O)Nc1ccc(C#N)c(S(=O)(=O)C(C)(C)C)c1O 10.1021/acs.jmedchem.7b01854
118554832 158686 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 432 4 3 5 3.5 CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2(F)CCOCC2)c1O 10.1021/acs.jmedchem.7b01854
CHEMBL4098864 158686 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 432 4 3 5 3.5 CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C2(F)CCOCC2)c1O 10.1021/acs.jmedchem.7b01854
72548703 161019 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]IL-8 from human recombinant CXCR2 receptor after 60 mins by scintillation counting analysisDisplacement of [125I]IL-8 from human recombinant CXCR2 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161019 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]IL-8 from human recombinant CXCR2 receptor after 60 mins by scintillation counting analysisDisplacement of [125I]IL-8 from human recombinant CXCR2 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
129316069 155313 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 436 6 4 5 3.4 CC(C)(CCO)S(=O)(=O)c1c(Cl)ccc(NC(=O)N[C@@H]2CCC=C2Cl)c1O 10.1021/acs.jmedchem.7b01854
CHEMBL4060139 155313 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 436 6 4 5 3.4 CC(C)(CCO)S(=O)(=O)c1c(Cl)ccc(NC(=O)N[C@@H]2CCC=C2Cl)c1O 10.1021/acs.jmedchem.7b01854
118554743 155493 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 428 5 3 5 3.5 CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C(C)(C)C2COC2)c1O 10.1021/acs.jmedchem.7b01854
CHEMBL4062361 155493 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 428 5 3 5 3.5 CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)C(C)(C)C2COC2)c1O 10.1021/acs.jmedchem.7b01854
118540867 156367 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 414 4 4 5 3.0 CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CC[C@@H](O)C2)c1O 10.1021/acs.jmedchem.7b01854
CHEMBL4072270 156367 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 414 4 4 5 3.0 CC1=CCC[C@H]1NC(=O)Nc1ccc(Cl)c(S(=O)(=O)[C@@H]2CC[C@@H](O)C2)c1O 10.1021/acs.jmedchem.7b01854
129316028 156772 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 442 5 3 5 4.0 CCC1(S(=O)(=O)c2c(Cl)ccc(NC(=O)N[C@@H]3CCC=C3C)c2O)CCOCC1 10.1021/acs.jmedchem.7b01854
CHEMBL4077201 156772 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assayAntagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL 442 5 3 5 4.0 CCC1(S(=O)(=O)c2c(Cl)ccc(NC(=O)N[C@@H]3CCC=C3C)c2O)CCOCC1 10.1021/acs.jmedchem.7b01854
58180205 140273 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation
ChEMBL 446 4 3 4 5.2 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCC2)c1O)Nc1cccc(F)c1Cl 10.1021/acsmedchemlett.5b00489
CHEMBL3818853 140273 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation
ChEMBL 446 4 3 4 5.2 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCC2)c1O)Nc1cccc(F)c1Cl 10.1021/acsmedchemlett.5b00489
58180198 140285 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation
ChEMBL 432 4 3 4 4.8 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCC2)c1O)Nc1cccc(F)c1Cl 10.1021/acsmedchemlett.5b00489
CHEMBL3818984 140285 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation
ChEMBL 432 4 3 4 4.8 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCC2)c1O)Nc1cccc(F)c1Cl 10.1021/acsmedchemlett.5b00489
58180199 140319 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubationAntagonist activity at human recombinant Gal4-VP16 fused-CXCR2 assessed as inhibition of CXCL1-mediated lactamase reporter gene expression after overnight incubation
ChEMBL 460 4 3 4 5.6 O=C(Nc1ccc(Cl)c(S(=O)(=O)C2CCCCC2)c1O)Nc1cccc(F)c1Cl 10.1021/acsmedchemlett.5b00489
CHEMBL3819480 140319 0 None - 0 Human 9.5