Biased Signaling Atlas

Ligand source activities (1 row/activity)

Potency
Affinity

Get vendors

Ligands					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity (Potency)	# tested GPCRs (Potency)	Species	p-value (-log)	Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	8498	3251	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	3251	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	3251	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	3251	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	112448	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	112448	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	2687	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	2687	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	2687	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	179020	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	179020	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	195998	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	195998	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	126277	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	126277	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	112454	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	112454	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	213092	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	35179	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	35179	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	114418	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	114418	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	212653	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	104140	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	104140	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	122478	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	122478	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	86290	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	86290	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	104141	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	104141	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	104144	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	104144	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	104146	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	104146	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	122483	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	122483	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	196714	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	196714	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	124643	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	124643	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	140293	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	140293	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	213424	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	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	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	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	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	95156	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	95156	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	104145	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	104145	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	212754	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	213106	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	104139	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	104139	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	95156	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	95156	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	112445	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	112445	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	213396	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	179671	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	179671	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	112434	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	112434	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	112542	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	112542	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	126276	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	126276	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	79889	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	79889	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	114413	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	114413	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	212658	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	173156	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	173156	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	180309	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	180309	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	139921	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	139921	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	213467	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	104161	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	104161	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	112447	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	112447	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	103896	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	103896	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	173156	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	173156	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	112436	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	112436	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	212941	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	114409	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	114409	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	213276	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	124645	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	124645	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	114414	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	114414	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	112444	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	112444	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	104151	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	104151	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	104153	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	104153	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	104164	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	104164	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	94540	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	94540	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	126282	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	126282	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	124640	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	124640	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	79870	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	79870	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	213479	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	212764	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	3432	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	3432	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	3432	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	114422	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	114422	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	171032	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	171032	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	81686	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	81686	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	212800	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	126278	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	126278	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	104168	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	104168	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	118565	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	118565	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	122488	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	122488	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	213062	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	213297	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	3646	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	3646	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	3646	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	168574	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	168574	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	126279	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	126279	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	114411	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	114411	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	182719	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	182719	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	122477	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	122477	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	125307	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	125307	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	122487	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	122487	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	181173	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	181173	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	212593	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	122481	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	122481	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	213587	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	180575	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	180575	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	124642	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	124642	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	79184	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	79184	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	104165	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	104165	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	1513	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	1513	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	1513	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	1513	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	122482	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	122482	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	182969	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	182969	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	114415	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	114415	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	114410	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	114410	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	114416	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	114416	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	104162	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	104162	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	180101	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	180101	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	179372	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	179372	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	114419	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	114419	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	180928	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	180928	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	122485	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	122485	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	3432	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	3432	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	3432	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	95010	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	95010	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	179381	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	179381	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	182929	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	182929	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	1513	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	1513	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	1513	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	1513	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	180720	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	180720	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	168574	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	168574	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	112447	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	112447	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	112455	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	112455	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	86946	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	86946	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	212481	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	112543	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	112543	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	124644	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	124644	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	213364	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	213299	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	104152	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	104152	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	213410	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	112431	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	112431	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	112446	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	112446	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	3646	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	3646	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	3646	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	114408	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	114408	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	114405	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	114405	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	122489	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	122489	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	94540	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	94540	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	3432	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	3432	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	3432	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	146950	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	146950	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	212874	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	179309	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	179309	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	122476	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	122476	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	104143	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	104143	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	104149	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	104149	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	104167	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	104167	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	212928	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	212934	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	179410	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	179410	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	112440	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	112440	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	122490	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	122490	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	213705	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	196734	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	196734	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	147221	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	147221	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	112437	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	112437	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	104160	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	104160	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	181866	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	181866	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	112439	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	112439	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	171098	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	171098	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	103434	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	103434	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	94486	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	94486	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	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	297	4	1	5	3.8	CC(Sc1nc(O)c(C#N)c(C2CC2)n1)c1ccccc1	10.1016/j.bmcl.2014.06.011
	CHEMBL3310790	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	297	4	1	5	3.8	CC(Sc1nc(O)c(C#N)c(C2CC2)n1)c1ccccc1	10.1016/j.bmcl.2014.06.011
	24959664	104150	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	104150	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	122486	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	122486	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	212635	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	154056	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	154056	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	112443	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	112443	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	1284	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	1284	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	1284	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	1284	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	141998	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	141998	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	142162	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	142162	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	142227	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	142227	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	142596	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	142596	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	143240	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	143240	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	143903	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	143903	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	144391	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	144391	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	144445	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	144445	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	144650	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	144650	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	144732	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	144732	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	145002	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	145002	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	145164	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	145164	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	146511	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	146511	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	146636	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	146636	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	146844	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	146844	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	146986	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	146986	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	147400	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	147400	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	147726	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	147726	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	148402	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	148402	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	148910	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	148910	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	149202	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	149202	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	149296	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	149296	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	149418	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	149418	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	149455	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	149455	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	149471	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	149471	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	149588	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	149588	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	149742	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	149742	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	149769	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	149769	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	149791	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	149791	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	149889	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	149889	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	150353	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	150353	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	150678	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	150678	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	151412	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	151412	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	151549	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	151549	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	151839	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	151839	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	151963	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	151963	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	152274	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	152274	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	154804	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	154804	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	112451	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	112451	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	104158	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	104158	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	114417	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	114417	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	87529	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	87529	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	195823	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	195823	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	179848	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	179848	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	114406	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	114406	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	155076	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	155076	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	212603	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	112449	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	112449	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	181842	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	181842	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	3646	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	3646	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	3646	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	168995	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	168995	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	126280	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	126280	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	125308	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	125308	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	195684	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	195684	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	112453	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	112453	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	104148	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	104148	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	122491	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	122491	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	212804	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	182391	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	182391	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	112450	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	112450	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	95010	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	95010	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	212982	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	154804	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	154804	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	112435	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	112435	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	122475	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	122475	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	112433	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	112433	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	197350	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	197350	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	114412	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	114412	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	181104	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	181104	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	114420	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	114420	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	212469	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	112438	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	112438	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	171900	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	171900	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	104147	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	104147	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	126281	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	126281	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	122479	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	122479	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	104166	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	104166	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	104142	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	104142	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	195824	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	195824	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	196927	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	196927	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	104159	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	104159	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	104163	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	104163	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	114421	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	114421	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	180785	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	180785	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	155076	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	155076	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	112442	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	112442	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	104154	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	104154	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	180287	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	180287	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	122480	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	122480	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	124641	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	124641	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	122484	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	122484	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	213674	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	178978	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	178978	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	213150	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	152098	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	152098	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	170976	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	170976	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	117523	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	117523	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	117524	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	117524	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	117527	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	117527	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	117525	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	117525	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	152098	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	152098	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	117526	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	117526	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	117528	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	117528	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	117520	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	117520	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	2687	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	2687	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	2687	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	2687	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	2687	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	2687	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	3251	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	3251	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	3251	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	3251	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	3646	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	3646	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	3646	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	1513	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	1513	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	1513	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	1513	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	3432	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	3432	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	3432	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	1233	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8702798
	24780598	1284	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	1284	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	1284	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	1284	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	1229	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8702798
	827	1224	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8702798
	8496	3904	0	None	7	2	Human	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	20044480
	828	1228	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8702798
	3618472	2837	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	2837	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	2837	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

Get vendors

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	2687	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	2687	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	2687	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	67149	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	67149	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	67149	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	170817	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	170817	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	196734	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	196734	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	155878	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	155878	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	157174	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	157174	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	158674	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	158674	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	161007	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	161007	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	155301	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	155301	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	155481	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	155481	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	156355	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	156355	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	156760	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	156760	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	140260	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	140260	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	140272	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	140272	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	140306

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)