target,target_id,target_uniprot,target_species,ligand,ligand_id,ligand_species,ligand_pubchem_cid,smiles,inchi,inchikey,type,action,action_comment,endogenous,primary_target,concentration_range,affinity_parameter,affinity_high,affinity_median,affinity_low,original_affinity_units,original_affinity_low_nm,original_affinity_median_nm,original_affinity_high_nm,original_affinity_relation,assay_description,receptor_site,ligand_context,pubmed_id CCR2,59,P41597,Human,CCL7,759,Human,,,,,Agonist,Full agonist,,yes,,,pIC50,8.7,,8.4,,,,,=,,,,9276730|9346309|12554737, CCR2,59,P41597,Human,vMIP-II,768,,486830,NCCCC[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC1=O)CCCN=C(N)N)CCCN=C(N)N)CCC(=O)N)C(C)C)C(=O)O)[C@H](O)C,"InChI=1S/C55H93N19O14S2/c1-28(2)23-37-50(84)74-43(30(5)75)52(86)69-35(15-9-10-20-56)47(81)67-33(16-11-21-63-54(59)60)45(79)65-25-41(77)66-34(17-12-22-64-55(61)62)46(80)68-36(18-19-40(58)76)48(82)73-42(29(3)4)51(85)72-39(53(87)88)27-90-89-26-32(57)44(78)70-38(49(83)71-37)24-31-13-7-6-8-14-31/h6-8,13-14,28-30,32-39,42-43,75H,9-12,15-27,56-57H2,1-5H3,(H2,58,76)(H,65,79)(H,66,77)(H,67,81)(H,68,80)(H,69,86)(H,70,78)(H,71,83)(H,72,85)(H,73,82)(H,74,84)(H,87,88)(H4,59,60,63)(H4,61,62,64)/t30-,32+,33+,34+,35+,36+,37+,38+,39+,42+,43+/m1/s1",JOEHPBQVSCDCHE-BKGQOYFSSA-N,Antagonist,Antagonist,,,,,pIC50,,9.1,,,,,,,,,,9287217, CCR2,59,P41597,Human,CCL11,769,Human,,,,,Agonist,Partial agonist,,yes,,,pIC50,7.7,,7.1,,,,,=,,,,12554737|15207250, CCR2,59,P41597,Human,CCL13,770,Human,,,,,Agonist,Full agonist,,yes,,,pIC50,8.7,,8.6,,,,,=,,,,9276730|12554737, CCR2,59,P41597,Human,CCL2,771,Human,,,,,Agonist,Full agonist,,yes,,,pIC50,10.2,,9.3,,,,,=,,,,9276730|9346309|12554737|15207250|10770925, CCR2,59,P41597,Human,CCL8,772,Human,,,,,Agonist,Full agonist,,yes,,,pIC50,,8.6,,,,,,=,,,,12554737, CCR2,59,P41597,Human,HIV-Tat,773,,,,,,Agonist,Full agonist,,,,,pIC50,,8.3,,,,,,,,,,9789057, CCR2,59,P41597,Human,vCCL4,774,,,,,,Agonist,Full agonist,,,,,pIC50,,7.1,,,,,,,,,,12554737, CCR2,59,P41597,Human,CCL24,775,Human,,,,,Antagonist,Antagonist,,yes,,,pIC50,,6.2,,,,,,,,,,15207250, CCR2,59,P41597,Human,CCL26,776,Human,,,,,Antagonist,Antagonist,,yes,,,pIC50,,8.5,,,,,,=,,,,15207250, CCR2,59,P51683,Mouse,INCB3344,777,,10008367,CCO[C@H]1CN(C[C@@H]1NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F)[C@@H]1CC[C@](CC1)(O)c1ccc2c(c1)OCO2,"InChI=1S/C29H34F3N3O6/c1-2-39-25-16-35(21-8-10-28(38,11-9-21)19-6-7-23-24(13-19)41-17-40-23)15-22(25)34-26(36)14-33-27(37)18-4-3-5-20(12-18)29(30,31)32/h3-7,12-13,21-22,25,38H,2,8-11,14-17H2,1H3,(H,33,37)(H,34,36)/t21-,22-,25-,28-/m0/s1",MZEOSVPWMSEFPW-UTWBDPIXSA-N,Antagonist,Antagonist,,,,,pIC50,,8.0,,,,,,,,,,16210643, CCR2,59,P41597,Human,MC148R,778,,,,,,Antagonist,Antagonist,,,,,pIC50,,8.8,,,,,,,,,,9600978, CCR2,59,P41597,Human,RS-102895,779,,10000456,O=C1Nc2ccccc2C2(O1)CCN(CC2)CCc1ccc(cc1)C(F)(F)F,"InChI=1S/C21H21F3N2O2/c22-21(23,24)16-7-5-15(6-8-16)9-12-26-13-10-20(11-14-26)17-3-1-2-4-18(17)25-19(27)28-20/h1-8H,9-14H2,(H,25,27)",HIDWEYPGMLIQSN-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pIC50,,6.3,,,,,,,,,,10770925, CCR2,59,P41597,Human,RS-136270,780,,5071702,Clc1cccc(c1)Cn1cccc1C(=O)O,"InChI=1S/C12H10ClNO2/c13-10-4-1-3-9(7-10)8-14-6-2-5-11(14)12(15)16/h1-7H,8H2,(H,15,16)",VPTUTBZAHHDMAA-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pIC50,,8.5,,,,,,,,,,10770925, CCR2,59,P41597,Human,RS-504393,781,,9953769,O=C1Nc2ccc(cc2C2(O1)CCN(CC2)CCc1nc(oc1C)c1ccccc1)C,"InChI=1S/C25H27N3O3/c1-17-8-9-22-20(16-17)25(31-24(29)27-22)11-14-28(15-12-25)13-10-21-18(2)30-23(26-21)19-6-4-3-5-7-19/h3-9,16H,10-15H2,1-2H3,(H,27,29)",ODNICNWASXKNNQ-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pKi,,6.7,,,,,,,,,,12954060, CCR2,59,P41597,Human,SB-282241,782,,10436045,O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2,"InChI=1S/C27H31Cl2N3O2/c28-24-7-4-19(16-25(24)29)5-9-27(34)30-12-2-1-3-13-32-14-10-20(11-15-32)23-18-31-26-8-6-21(33)17-22(23)26/h4-9,16-18,20,31,33H,1-3,10-15H2,(H,30,34)/b9-5+",QBRLVMQBZIFWTB-WEVVVXLNSA-N,Antagonist,Antagonist,,,,,pKi,,7.0,,,,,,,,,,12954060, CCR2,59,P41597,Human,TAK-779,783,,183790,Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C,"InChI=1S/C33H38N2O2/c1-24-7-11-27(12-8-24)28-14-13-26-5-4-6-29(22-30(26)21-28)33(36)34-31-15-9-25(10-16-31)23-35(2,3)32-17-19-37-20-18-32/h7-16,21-22,32H,4-6,17-20,23H2,1-3H3/p+1",XNHZXMPLVSJQFK-UHFFFAOYSA-O,Antagonist,Antagonist,,,,,pKi,,8.2,,,,,,,,,,12954060|10318947, CCR2,59,P41597,Human,TAK-779,783,,183790,Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C,"InChI=1S/C33H38N2O2/c1-24-7-11-27(12-8-24)28-14-13-26-5-4-6-29(22-30(26)21-28)33(36)34-31-15-9-25(10-16-31)23-35(2,3)32-17-19-37-20-18-32/h7-16,21-22,32H,4-6,17-20,23H2,1-3H3/p+1",XNHZXMPLVSJQFK-UHFFFAOYSA-O,Antagonist,Antagonist,,,,,pKi,,7.2,,,,,,,,,,12954060, CCR2,59,P41597,Human,Teijin-lead_cmp_5,785,,44353447,O=C(N[C@@H]1CCN(C1)Cc1ccc(cc1C)C)CNC(=O)c1cccc(c1)C(F)(F)F,"InChI=1S/C23H26F3N3O2/c1-15-6-7-18(16(2)10-15)13-29-9-8-20(14-29)28-21(30)12-27-22(31)17-4-3-5-19(11-17)23(24,25)26/h3-7,10-11,20H,8-9,12-14H2,1-2H3,(H,27,31)(H,28,30)/t20-/m1/s1",MRRGKBBDXLJMCV-HXUWFJFHSA-N,Antagonist,Antagonist,,,,,pKi,,6.5,,,,,,,,,,12954060, CCR2,59,P41597,Human,CCL16,1272,Human,,,,,Agonist,Full agonist,,yes,,,,,,,,,,,=,,,,, CCR2,59,P41597,Human,AZD2423,7825,,46213922,O=C(N1CCN(CC1)C(=O)[C@@H]1NCCN(C1)C(C)C)Nc1ccc(c(c1)F)Cl,"InChI=1S/C19H27ClFN5O2/c1-13(2)26-6-5-22-17(12-26)18(27)24-7-9-25(10-8-24)19(28)23-14-3-4-15(20)16(21)11-14/h3-4,11,13,17,22H,5-10,12H2,1-2H3,(H,23,28)/t17-/m1/s1",WERHXSXPOAOBJV-QGZVFWFLSA-N,Allosteric modulator,Negative,,,yes,,pIC50,,8.59,,IC50,,2.6,,=,,,,, CCR2,59,P41597,Human,plozalizumab,8921,,,,,,Antibody,Binding,,,yes,,pEC50,,9.72,,EC50,,0.19,,=,Calculated from ng/ml based on a mol weight of ~150kDa.,,,, CCR2,59,P41597,Human,INCB8761,9032,,11192346,O=C(N1CC[C@@H](C1)NC1CCC(CC1)(O)c1ccc(cn1)c1ncccn1)CNC(=O)c1cccc(c1)C(F)(F)F,"InChI=1S/C29H31F3N6O3/c30-29(31,32)21-4-1-3-19(15-21)27(40)36-17-25(39)38-14-9-23(18-38)37-22-7-10-28(41,11-8-22)24-6-5-20(16-35-24)26-33-12-2-13-34-26/h1-6,12-13,15-16,22-23,37,41H,7-11,14,17-18H2,(H,36,40)/t22?,23-,28?/m0/s1",ZNSVOHSYDRPBGI-CBQRAPNFSA-N,Antagonist,Antagonist,,,yes,,pIC50,,8.28,,IC50,,5.2,,=,,,,24900280, CCR2,59,P41597,Human,INCB3284,9045,,11527661,COc1ccc(cn1)C1(O)CCC(CC1)N1CC[C@H](C1)NC(=O)CNC(=O)c1cccc(c1)C(F)(F)F,"InChI=1S/C26H31F3N4O4/c1-37-23-6-5-19(14-30-23)25(36)10-7-21(8-11-25)33-12-9-20(16-33)32-22(34)15-31-24(35)17-3-2-4-18(13-17)26(27,28)29/h2-6,13-14,20-21,36H,7-12,15-16H2,1H3,(H,31,35)(H,32,34)/t20-,21?,25?/m1/s1",NXZNYBUBXWWKCP-JMOWIOHXSA-N,Antagonist,Antagonist,,,yes,,pIC50,,8.43,,IC50,,3.7,,=,,,,24900329, CCR2,59,,Monkey,MK-0812,9048,,11180808,CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1CCc2c(C1)cc(cn2)C(F)(F)F,"InChI=1S/C24H34F3N3O3/c1-15(2)23(7-4-18(11-23)29-20-6-9-33-14-21(20)32-3)22(31)30-8-5-19-16(13-30)10-17(12-28-19)24(25,26)27/h10,12,15,18,20-21,29H,4-9,11,13-14H2,1-3H3/t18-,20+,21-,23+/m1/s1",MTMDXAIUENDNDL-RJSMDTJLSA-N,Antagonist,Antagonist,,,,,pIC50,,8.35,,IC50,,4.5,,=,Measuring inhibition of [125]I-MCP-1 binding by MK-0812 on isolated monocytes.,,,19913021, CCR2,59,P41597,Human,BMS-681,9430,,68764898,CCC[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C,"InChI=1S/C26H36F3N5O/c1-5-6-17-13-19(33(4)16(2)3)8-10-23(17)34-12-11-22(25(34)35)32-24-20-14-18(26(27,28)29)7-9-21(20)30-15-31-24/h7,9,14-17,19,22-23H,5-6,8,10-13H2,1-4H3,(H,30,31,32)/t17-,19-,22+,23+/m1/s1",NUJWKQSEJDYCDB-GNRVTEMESA-N,Antagonist,Antagonist,,,yes,,pIC50,,9.15,,IC50,,0.7,,=,,,,25893046, CCR2,59,P41597,Human,CCR2-RA-[R],9431,,12093170,Clc1ccc(c(c1)F)N1[C@H](C2CCCCC2)C(=C(C1=O)O)C(=O)C,"InChI=1S/C18H19ClFNO3/c1-10(22)15-16(11-5-3-2-4-6-11)21(18(24)17(15)23)14-8-7-12(19)9-13(14)20/h7-9,11,16,23H,2-6H2,1H3/t16-/m1/s1",VQNLJXWZGVRLBA-MRXNPFEDSA-N,Allosteric modulator,Antagonist,,,,,pIC50,,5.3,,IC50,,5000.0,,<,Antagonism of 125I-MCP-1 binding to THP-1 cells,,,, CCR2,59,P41597,Human,PF-04634817,9979,,46198579,CO[C@@H]1COCC[C@@H]1N[C@@H]1CC[C@](C1)(C(C)C)C(=O)N1C[C@@H]2C[C@H]1CN2c1ncnc(c1)C(F)(F)F,"InChI=1S/C25H36F3N5O3/c1-15(2)24(6-4-16(10-24)31-19-5-7-36-13-20(19)35-3)23(34)33-12-17-8-18(33)11-32(17)22-9-21(25(26,27)28)29-14-30-22/h9,14-20,31H,4-8,10-13H2,1-3H3/t16-,17+,18+,19+,20-,24+/m1/s1",MCRWZBYTLVCCJJ-DKALBXGISA-N,Antagonist,Antagonist,,,,,pIC50,,8.43,,IC50,,3.68,,=,Whole cell binding assay measuring displacement of [125I]MCP-1 from CCR2 by PF-04634817 in human peripheral blood mononuclear cells.,,,, CCR2,59,P41597,Human,compound 39 [PMID: 31742400],10585,,145996522,Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C,"InChI=1S/C15H15Cl2N5O/c1-7(2)12-9(6-8-4-3-5-10(16)11(8)17)13(23)22-15(19-12)20-14(18)21-22/h3-5,7H,6H2,1-2H3,(H3,18,19,20,21)",KLBHHUODQVCBKX-UHFFFAOYSA-N,Allosteric modulator,Antagonist,,,,,pKi,,8.8,,Ki,,1.6,,=,"Binding affinity determined from a radioligand binding assay, measuring displacement of [3H]-CCR2-RA-[R] from U2OS cells stably expressing human CCR2.",,,31742400, CCR2,59,P41597,Human,JNJ-27141491,10586,,11617815,CC[C@@H](n1c(=S)[nH]c(c1C(=O)OC)c1ccno1)c1ccc(c(c1)F)F,"InChI=1S/C17H15F2N3O3S/c1-3-12(9-4-5-10(18)11(19)8-9)22-15(16(23)24-2)14(21-17(22)26)13-6-7-20-25-13/h4-8,12H,3H2,1-2H3,(H,21,26)/t12-/m1/s1",SYARXICKXVXWNA-GFCCVEGCSA-N,Allosteric modulator,Antagonist,,,,,pIC50,,7.02,,IC50,,95.0,,=,Measuring antagonism of 125I-MCP-1binding to human CCR2 expressed by CHO cells in a competition binding assay.,,,18599682, CCR2,59,P41597,Human,ilacirnon,11185,,25134303,Cc1cnc(c(c1)NS(=O)(=O)c1ccc(c(c1)C(F)(F)F)Cl)C(=O)c1ncnc2c1cc[nH]2,"InChI=1S/C20H13ClF3N5O3S/c1-10-6-15(29-33(31,32)11-2-3-14(21)13(7-11)20(22,23)24)17(26-8-10)18(30)16-12-4-5-25-19(12)28-9-27-16/h2-9,29H,1H3,(H,25,27,28)",LUUMLYXKTPBTQR-UHFFFAOYSA-N,Antagonist,Antagonist,,,,,pIC50,,8.3,,IC50,,5.0,,=,Inhibition of MCP-1-mediated migration of THP- 1 cells in a chemotaxis assay.,,,, CCR2,59,P41597,Human,BMS-753426,11597,,23725180,CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)NC(C)(C)C,"InChI=1S/C25H33F3N6O2/c1-14(35)31-20-12-16(33-24(2,3)4)6-8-21(20)34-10-9-19(23(34)36)32-22-17-11-15(25(26,27)28)5-7-18(17)29-13-30-22/h5,7,11,13,16,19-21,33H,6,8-10,12H2,1-4H3,(H,31,35)(H,29,30,32)/t16-,19+,20-,21+/m1/s1",QAPTWHXHEYAIKG-RCOXNQKVSA-N,Antagonist,Antagonist,,,,,pIC50,,8.57,,IC50,,2.7,,=,,,,34141082, CCR2,59,P41597,Human,BMS-741672,11598,,23725177,CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N1CC[C@@H](C1=O)Nc1ncnc2c1cc(cc2)C(F)(F)F)N(C(C)C)C,"InChI=1S/C25H33F3N6O2/c1-14(2)33(4)17-6-8-22(21(12-17)31-15(3)35)34-10-9-20(24(34)36)32-23-18-11-16(25(26,27)28)5-7-19(18)29-13-30-23/h5,7,11,13-14,17,20-22H,6,8-10,12H2,1-4H3,(H,31,35)(H,29,30,32)/t17-,20+,21-,22+/m1/s1",GVOISEJVFFIGQE-YCZSINBZSA-N,Antagonist,Antagonist,,,,,pIC50,,8.96,,IC50,,1.1,,=,Antagonism of MCP-1 (CCL2) binding to human peripheral blood mononuclear cells.,,,30891130,