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 RAR-related orphan receptor-γ,600,P51449,Human,ALRT 1550,2740,,5287705,C/C(=C\C=C\C(=C\C(=O)O)\C)/c1cc(cc(c1)C(C)(C)C)C(C)(C)C,"InChI=1S/C23H32O2/c1-16(12-21(24)25)10-9-11-17(2)18-13-19(22(3,4)5)15-20(14-18)23(6,7)8/h9-15H,1-8H3,(H,24,25)/b10-9+,16-12+,17-11+",JMPZTWDLOGTBPM-OUQSKUGOSA-N,Antagonist,Antagonist,,,,,,,,,,,,,,,,,12958591, RAR-related orphan receptor-γ,600,P51449,Human,T0901317,2755,,447912,FC(CN(S(=O)(=O)c1ccccc1)c1ccc(cc1)C(C(F)(F)F)(C(F)(F)F)O)(F)F,"InChI=1S/C17H12F9NO3S/c18-14(19,20)10-27(31(29,30)13-4-2-1-3-5-13)12-8-6-11(7-9-12)15(28,16(21,22)23)17(24,25)26/h1-9,28H,10H2",SGIWFELWJPNFDH-UHFFFAOYSA-N,Agonist,Inverse agonist,,,,,pKi,,7.29,,Ki,,51.0,,=,,,,19887649, RAR-related orphan receptor-γ,600,P51449,Human,25-hydroxycholesterol,2885,,65094,O[C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]2([C@H]3CC[C@@H]2[C@@H](CCCC(O)(C)C)C)C)C1)C,"InChI=1S/C27H46O2/c1-18(7-6-14-25(2,3)29)22-10-11-23-21-9-8-19-17-20(28)12-15-26(19,4)24(21)13-16-27(22,23)5/h8,18,20-24,28-29H,6-7,9-17H2,1-5H3/t18-,20+,21+,22-,23+,24+,26+,27-/m1/s1",INBGSXNNRGWLJU-ZHHJOTBYSA-N,Agonist,Agonist,,yes,,,,,,,,,,,,,,,20203100, RAR-related orphan receptor-γ,600,P51449,Human,GNE-3500,9660,,122379290,C[C@H]1CC[C@@H](S(=O)(=O)N1Cc1ccc(cc1F)N1CCN(CC1)C(=O)C)c1ccccc1,"InChI=1S/C24H30FN3O3S/c1-18-8-11-24(20-6-4-3-5-7-20)32(30,31)28(18)17-21-9-10-22(16-23(21)25)27-14-12-26(13-15-27)19(2)29/h3-7,9-10,16,18,24H,8,11-15,17H2,1-2H3/t18-,24+/m0/s1",WLCIIQPUMOJJOF-MHECFPHRSA-N,Agonist,Inverse agonist,,,yes,,pEC50,,7.92,,EC50,,12.0,,=,Measuring inhibition of SRC1 coactivator peptide recruitment by the ligand binding domain of human RORγ.,,,26061388, RAR-related orphan receptor-γ,600,P51449,Human,GSK2981278,9661,,89875987,OCc1cc(ccc1OCC1CCOCC1)S(=O)(=O)N(c1ccc(cc1)CC)CC(C)C,"InChI=1S/C25H35NO5S/c1-4-20-5-7-23(8-6-20)26(16-19(2)3)32(28,29)24-9-10-25(22(15-24)17-27)31-18-21-11-13-30-14-12-21/h5-10,15,19,21,27H,4,11-14,16-18H2,1-3H3",LZLBRISQTJVZNP-UHFFFAOYSA-N,Agonist,Inverse agonist,,,yes,,pIC50,,8.49,,IC50,,3.2,,=,Measuring inhibition of human T cell cytokine production under Th17 skewing conditions.,,,26870941, RAR-related orphan receptor-γ,600,P51449,Human,TAK-828F,9867,,118622692,COc1ccc2c(n1)CCN([C@H]2C(=O)Nc1cc(F)c2c(c1)CCC2(C)C)C(=O)[C@@H]1C[C@@H](C1)CC(=O)O,"InChI=1S/C28H32FN3O5/c1-28(2)8-6-16-13-18(14-20(29)24(16)28)30-26(35)25-19-4-5-22(37-3)31-21(19)7-9-32(25)27(36)17-10-15(11-17)12-23(33)34/h4-5,13-15,17,25H,6-12H2,1-3H3,(H,30,35)(H,33,34)/t15-,17+,25-/m1/s1",ICMFYVOUDGRBLG-VFHHBZAHSA-N,Agonist,Inverse agonist,,,yes,,pIC50,,8.72,,IC50,,1.9,,=,Binding to human RORγt isoform.,,,29510038, RAR-related orphan receptor-γ,600,P51449,Human,cintirorgon,10045,,124126348,FC(Oc1cc(F)cc(c1)c1ccc2c(c1)N(C[C@@H](O2)CC(C(=O)O)(C)C)S(=O)(=O)c1cccc(c1)C(F)(F)F)F,"InChI=1S/C27H23F6NO6S/c1-26(2,24(35)36)13-20-14-34(41(37,38)21-5-3-4-17(11-21)27(31,32)33)22-10-15(6-7-23(22)39-20)16-8-18(28)12-19(9-16)40-25(29)30/h3-12,20,25H,13-14H2,1-2H3,(H,35,36)/t20-/m0/s1",GULSIMHVQYBADX-FQEVSTJZSA-N,Agonist,Agonist,,,,,pEC50,,6.3,,EC50,,500.0,,<,Measured in a RORγ-ligand binding domain Gal4-RORγ luciferase reporter assay.,,,, RAR-related orphan receptor-γ,600,P51449,Human,cintirorgon,10045,,124126348,FC(Oc1cc(F)cc(c1)c1ccc2c(c1)N(C[C@@H](O2)CC(C(=O)O)(C)C)S(=O)(=O)c1cccc(c1)C(F)(F)F)F,"InChI=1S/C27H23F6NO6S/c1-26(2,24(35)36)13-20-14-34(41(37,38)21-5-3-4-17(11-21)27(31,32)33)22-10-15(6-7-23(22)39-20)16-8-18(28)12-19(9-16)40-25(29)30/h3-12,20,25H,13-14H2,1-2H3,(H,35,36)/t20-/m0/s1",GULSIMHVQYBADX-FQEVSTJZSA-N,Agonist,Agonist,,,,,pEC50,,6.3,,EC50,,500.0,,<,Measured in a RORγ-ligand binding domain TR-FRET assay.,,,, RAR-related orphan receptor-γ,600,P51449,Human,RORC2 inverse agonist 66 [PMID: 30130103],10078,,118977746,N#Cc1cccc(c1)C(=O)Nc1cnc2c(c1C(F)(F)F)c(cn2C)C1CCN(CC1)C(=O)C(C)C,"InChI=1S/C26H26F3N5O2/c1-15(2)25(36)34-9-7-17(8-10-34)19-14-33(3)23-21(19)22(26(27,28)29)20(13-31-23)32-24(35)18-6-4-5-16(11-18)12-30/h4-6,11,13-15,17H,7-10H2,1-3H3,(H,32,35)",BIHPJIJLDNUDGH-UHFFFAOYSA-N,Agonist,Inverse agonist,,,,,pIC50,,8.39,,IC50,,4.1,,=,In a TR-FRET assay measuring agonist-induced inhibition of co-factor recruitment to RORC2 ligand binding domain.,,,30130103, RAR-related orphan receptor-γ,600,P51449,Human,RORC2 inverse agonist 66 [PMID: 30130103],10078,,118977746,N#Cc1cccc(c1)C(=O)Nc1cnc2c(c1C(F)(F)F)c(cn2C)C1CCN(CC1)C(=O)C(C)C,"InChI=1S/C26H26F3N5O2/c1-15(2)25(36)34-9-7-17(8-10-34)19-14-33(3)23-21(19)22(26(27,28)29)20(13-31-23)32-24(35)18-6-4-5-16(11-18)12-30/h4-6,11,13-15,17H,7-10H2,1-3H3,(H,32,35)",BIHPJIJLDNUDGH-UHFFFAOYSA-N,Agonist,Inverse agonist,,,,,pIC50,,7.78,,IC50,,16.6,,=,In a TR-FRET assay measuring agonist-=induced inhibition of co-activator peptide recruitment to RORC2 ligand binding domain.,,,, RAR-related orphan receptor-γ,600,P51449,Human,SR1001,10143,,44241473,CC(=O)Nc1nc(c(s1)S(=O)(=O)Nc1ccc(cc1)C(C(F)(F)F)(C(F)(F)F)O)C,"InChI=1S/C15H13F6N3O4S2/c1-7-11(29-12(22-7)23-8(2)25)30(27,28)24-10-5-3-9(4-6-10)13(26,14(16,17)18)15(19,20)21/h3-6,24,26H,1-2H3,(H,22,23,25)",OZBSSKGBKHOLGA-UHFFFAOYSA-N,Agonist,Inverse agonist,,,yes,,pKi,,6.95,,Ki,,111.0,,=,Competitive radioligand binding assay using [3H]25-hydroxycholesterol as tracer.,,,21499262, RAR-related orphan receptor-γ,600,P51449,Human,SR2211,10144,,51035449,Fc1cc(ccc1c1ccc(cc1)CN1CCN(CC1)Cc1ccncc1)C(C(F)(F)F)(C(F)(F)F)O,"InChI=1S/C26H24F7N3O/c27-23-15-21(24(37,25(28,29)30)26(31,32)33)5-6-22(23)20-3-1-18(2-4-20)16-35-11-13-36(14-12-35)17-19-7-9-34-10-8-19/h1-10,15,37H,11-14,16-17H2",KVHKWAZUPPBMLL-UHFFFAOYSA-N,Agonist,Inverse agonist,,,yes,,pKi,,6.98,,Ki,,105.0,,=,Displacement of radioligand [3H]T1317 in a competition-based SPA assay.,,,22292739, RAR-related orphan receptor-γ,600,P51449,Human,SR1555,10145,,71470549,CC(=O)N1CCN(CC1)Cc1ccc(cc1)c1ccc(cc1)C(C(F)(F)F)(C(F)(F)F)O,"InChI=1S/C22H22F6N2O2/c1-15(31)30-12-10-29(11-13-30)14-16-2-4-17(5-3-16)18-6-8-19(9-7-18)20(32,21(23,24)25)22(26,27)28/h2-9,32H,10-14H2,1H3",LTFVNEZXOPUABB-UHFFFAOYSA-N,Agonist,Inverse agonist,,,yes,,pIC50,,6.0,,IC50,,1000.0,,=,In a competitive radioligand binding assay using [3H]T0901317 as tracer and measuring displacement from the ligand binding domain fragment of RORγ.,,,22769242, RAR-related orphan receptor-γ,600,P51449,Human,XY101,10366,,138105957,CCS(=O)(=O)c1ccc(cc1)CC(=O)Nc1ccc(cc1)c1ccc(cc1F)C(C(F)(F)F)(C(F)(F)F)O,"InChI=1S/C25H20F7NO4S/c1-2-38(36,37)19-10-3-15(4-11-19)13-22(34)33-18-8-5-16(6-9-18)20-12-7-17(14-21(20)26)23(35,24(27,28)29)25(30,31)32/h3-12,14,35H,2,13H2,1H3,(H,33,34)",AUIAOCHKUNGZHV-UHFFFAOYSA-N,Agonist,Inverse agonist,,,yes,,pIC50,,7.52,,IC50,,30.0,,=,Measuring disruprion of RORγ-driven transcriptional activity in a Gal4 reporter assay in 293 T cells.,,,30964293, RAR-related orphan receptor-γ,600,P51449,Human,XY101,10366,,138105957,CCS(=O)(=O)c1ccc(cc1)CC(=O)Nc1ccc(cc1)c1ccc(cc1F)C(C(F)(F)F)(C(F)(F)F)O,"InChI=1S/C25H20F7NO4S/c1-2-38(36,37)19-10-3-15(4-11-19)13-22(34)33-18-8-5-16(6-9-18)20-12-7-17(14-21(20)26)23(35,24(27,28)29)25(30,31)32/h3-12,14,35H,2,13H2,1H3,(H,33,34)",AUIAOCHKUNGZHV-UHFFFAOYSA-N,Agonist,Inverse agonist,,,yes,,pKd,,6.42,,Kd,,380.0,,=,In vitro binding to the RORγ LBD measured in a isothermal titration calorimetry (ITC) assay.,,,30964293, RAR-related orphan receptor-γ,600,P51449,Human,XY101,10366,,138105957,CCS(=O)(=O)c1ccc(cc1)CC(=O)Nc1ccc(cc1)c1ccc(cc1F)C(C(F)(F)F)(C(F)(F)F)O,"InChI=1S/C25H20F7NO4S/c1-2-38(36,37)19-10-3-15(4-11-19)13-22(34)33-18-8-5-16(6-9-18)20-12-7-17(14-21(20)26)23(35,24(27,28)29)25(30,31)32/h3-12,14,35H,2,13H2,1H3,(H,33,34)",AUIAOCHKUNGZHV-UHFFFAOYSA-N,Agonist,Inverse agonist,,,yes,,pKd,,6.12,,Kd,,750.0,,=,In vitro binding to the RORγ LBD measured using AlphaScreen technology.,,,30964293, RAR-related orphan receptor-γ,600,P51449,Human,compound 32 [PMID: 31638797],10528,,122669265,Fc1ccc(cc1)S(=O)(=O)[C@@]12CCN([C@@H]1CCc1c2ccc(c1)C(C(F)(F)F)(C(F)(F)F)F)C(=O)C1(O)CCS(=O)(=O)CC1,"InChI=1S/C27H25F8NO6S2/c28-18-3-5-19(6-4-18)44(41,42)24-9-12-36(22(37)23(38)10-13-43(39,40)14-11-23)21(24)8-1-16-15-17(2-7-20(16)24)25(29,26(30,31)32)27(33,34)35/h2-7,15,21,38H,1,8-14H2/t21-,24-/m1/s1",ONXFNBOZJKXCNC-ZJSXRUAMSA-N,Agonist,Inverse agonist,,,,,pEC50,,7.62,,EC50,,24.0,,=,Determined in a luciferase reporter assay; measuring inhibition of constitutive activity of RORγt in Jurkat cells overexpressing full length RORγt proteins fused with the Gal4 Luc reporter.,,,31638797, RAR-related orphan receptor-γ,600,P51449,Human,compound 32 [PMID: 31638797],10528,,122669265,Fc1ccc(cc1)S(=O)(=O)[C@@]12CCN([C@@H]1CCc1c2ccc(c1)C(C(F)(F)F)(C(F)(F)F)F)C(=O)C1(O)CCS(=O)(=O)CC1,"InChI=1S/C27H25F8NO6S2/c28-18-3-5-19(6-4-18)44(41,42)24-9-12-36(22(37)23(38)10-13-43(39,40)14-11-23)21(24)8-1-16-15-17(2-7-20(16)24)25(29,26(30,31)32)27(33,34)35/h2-7,15,21,38H,1,8-14H2/t21-,24-/m1/s1",ONXFNBOZJKXCNC-ZJSXRUAMSA-N,Agonist,Inverse agonist,,,,,pIC50,,10.44,,IC50,,0.036,,=,"Determined in a competition binding scintillation proximity assay (SPA), using recombinant His-tagged RORγ ligand binding domain (A262-S507) and [3H] 25-hydroxycholesterol as tracer.",,,, RAR-related orphan receptor-γ,600,P51449,Human,MRL-871,10642,,68159303,OC(=O)c1ccc(cc1)c1nn(c2c1cccc2)C(=O)c1c(Cl)cccc1C(F)(F)F,"InChI=1S/C22H12ClF3N2O3/c23-16-6-3-5-15(22(24,25)26)18(16)20(29)28-17-7-2-1-4-14(17)19(27-28)12-8-10-13(11-9-12)21(30)31/h1-11H,(H,30,31)",DANLZOIRUUHIIX-UHFFFAOYSA-N,Agonist,Inverse agonist,,,,,pEC50,,7.8,,EC50,,16.0,,=,Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486); assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis,,,26048793, RAR-related orphan receptor-γ,600,P51449,Human,"compound 25 [Zhang et al., 2020]",10643,,72943563,OC(=O)[C@@H]1CCN(C[C@H]1O)c1nn(c2c1c(F)ccc2)C(=O)c1c(Cl)cccc1C1CC1,"InChI=1S/C23H21ClFN3O4/c24-15-4-1-3-13(12-7-8-12)19(15)22(30)28-17-6-2-5-16(25)20(17)21(26-28)27-10-9-14(23(31)32)18(29)11-27/h1-6,12,14,18,29H,7-11H2,(H,31,32)/t14-,18-/m1/s1",IBIKHMZPHNKTHM-RDTXWAMCSA-N,Allosteric modulator,Negative,,,,,pIC50,,9.0,,IC50,,1.0,,=,Inhibition of cofactor (LXXLL-motif containing steroid receptor coactivator SRC1 peptide) recruitment to RORγ ligand binding domain in a TR-FRET biochemical assay.,,,32071676, RAR-related orphan receptor-γ,600,P51449,Human,AZD0284,11711,,129205086,FC(F)(F)C(O)(C(F)(F)F)c1ccc(cc1)NC(=O)[C@@H]1N(Cc2c1ccc(c2)S(=O)(=O)C)C(=O)C,"InChI=1S/C21H18F6N2O5S/c1-11(30)29-10-12-9-15(35(2,33)34)7-8-16(12)17(29)18(31)28-14-5-3-13(4-6-14)19(32,20(22,23)24)21(25,26)27/h3-9,17,32H,10H2,1-2H3,(H,28,31)/t17-/m1/s1",QYYZXEPEVBXNNA-QGZVFWFLSA-N,Agonist,Inverse agonist,,,,,pIC50,,7.39,,IC50,,41.0,,=,,,,34464130, RAR-related orphan receptor-γ,600,P51449,Human,"compound 14 [Schnute et al., 2023]",12351,,167993636,CC(C)C(=O)N1CCN2C[C@@H]1CCCCCS(=O)(=O)Nc1cccc(C2)c1C,"InChI=1S/C21H33N3O3S/c1-16(2)21(25)24-12-11-23-14-18-8-7-10-20(17(18)3)22-28(26,27)13-6-4-5-9-19(24)15-23/h7-8,10,16,19,22H,4-6,9,11-15H2,1-3H3/t19-/m0/s1",GMUUZFVHYAPQEI-IBGZPJMESA-N,Agonist,Inverse agonist,,,,,pIC50,,8.03,,IC50,,9.3,,=,Inhibitory potency in a TR-FRET cofactor recruitment assay,,,,