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G PROTEIN
STRUCTURE
RECEPTOR
OTHER PROTEINS
STRUCTURE LIGAND
PHYSIOLOGICAL LIGAND
REFERENCE
Fam. α Species Note % of Seq β Species γ Species Method
PDB
 Refined
structure
 Resolution
UniProt
 Gene IUPHAR Receptor family Class Species Receptor fusion Antibodies Other Name Type Function Name Type Authors Reference PDB Date
Gs αs Human DNGs: DN Gs to stabilize complex 58 β1 Rat γ2 Bovine Cryo-EM 7CZ5 7CZ5_refined 2.6 GHRHR GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 - GHRH (Human) pubchem gtoplig uniprot
Peptide Agonist GHRH (Mouse), GHRH (Rat), GHRH (Human) Peptide Zhou F, Zhang H, Cong Z, Zhao LH, Zhou Q, Mao C, Cheng X, Shen DD, Cai X, Ma C, Wang Y, Dai A, Zhou Y, Sun W, Zhao F, Zhao S, Jiang H, Jiang Y, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-020-18945-0 2020-11-18
Gi/o αi1 Human Gi: human Gαi1, rat Gβ1, bovine Gγ2 63 β1 Rat γ2 Bovine Cryo-EM 23SO - 3.0 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - cebranopadol pubchem gtoplig chembl_ligand chembl_ligand chembl_ligand drugbank pubchem
Small molecule Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2026-07-01
Gq/11 αq Human miniGsqiN: Gs scaffold w/ Gq α5 tail 57 β1 Human γ2 Mouse Cryo-EM 25IK - 3.0 MAS MAS1 MAS1 Orphan A (Rhodopsin) Human BRIL - LgBiT tag - None - - - - - 2026-05-20
Gq/11 αq Human miniGαs: Gαi1 N-term, scFv16; Gq specificity 59 β1 Human γ2 Human Cryo-EM 26XH - 2.8 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human BRIL Nanobody-35 - maleic acid pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist α-ketoglutaric acid Small molecule None 10.1038/S44318-026-00823-Y 2026-06-17
Gi/o αt1 Bovine Gnat1 CT2 fragment (340-350), K341L mutation 3 - - - - X-ray 3DQB 3DQB_refined 3.2 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - - None - - - Scheerer P, Park JH, Hildebrand PW, Kim YJ, Krauss N, Choe HW, Hofmann KP, Ernst OP 10.1038/NATURE07330 2008-09-23
Gi/o αt1 Bovine Gα CT2 peptide (residues 340-350) modeled 3 - - - - X-ray 4BEY 4BEY_refined 2.9 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - - None - - - Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J 10.1038/EMBOR.2013.44 2013-05-08
Gi/o αgust Bovine Gα C-terminal/α5 fragment (GaCT2 peptide) 3 - - - - X-ray 5EN0 5EN0_refined 2.8 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Singhal A, Guo Y, Matkovic M, Schertler G, Deupi X, Yan EC, Standfuss J 10.15252/EMBR.201642671 2016-08-10
Gi/o αi1 Human DN Gαi1: G203A/A326S, nucleotide-free complex 100 β1 Rat γ2 Bovine Cryo-EM 6CMO 6CMO_refined 4.5 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Human BRIL - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Kang Y, Kuybeda O, de Waal PW, Mukherjee S, Van Eps N, Dutka P, Zhou XE, Bartesaghi A, Erramilli S, Morizumi T, Gu X, Yin Y, Liu P, Jiang Y, Meng X, Zhao G, Melcher K, Ernst OP, Kossiakoff AA, Subramaniam S, Xu HE 10.1038/S41586-018-0215-Y 2018-06-20
Gs αs Human Gα C-term α5 fragment fused to receptor + T4L 44 - - - - X-ray 6E67 6E67_refined 3.7 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - CHEMBL1615159 chembl_ligand pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixa-Gonzalez R, Mathiesen JM, Hildebrand PW, Kobilka BK 10.1016/J.CELL.2019.04.021 2019-06-05
Gs αs Bovine DNGs: G226A/A366S; α5→Gi1 for Nb35 binding 58 β1 Rat γ2 Bovine Cryo-EM 6NBF - 3.0 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyroid hormone analog pubchem
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17
Gs αs Bovine DN bovine Gs/Gi1 chimera: G226A/A366S 57 β1 Rat γ2 Bovine Cryo-EM 6NBH - 3.5 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyroid hormone analog pubchem
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17
Gs αs Bovine DN Gαs (G226A) + bovine Gi1 C-term, Nb35 56 β1 Rat γ2 Bovine Cryo-EM 6NBI - 4.0 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyroid hormone analog pubchem
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Zhao LH, Ma S, Sutkeviciute I, Shen DD, Zhou XE, de Waal PW, Li CY, Kang Y, Clark LJ, Jean-Alphonse FG, White AD, Yang D, Dai A, Cai X, Chen J, Li C, Jiang Y, Watanabe T, Gardella TJ, Melcher K, Wang MW, Vilardaga JP, Xu HE, Zhang Y 10.1126/SCIENCE.AAV7942 2019-04-17
Gi/o αt1 Bovine Transducin Gα1 C-terminal α5 fragment (CT2) 3 - - - - X-ray 6NWE 6NWE_refined 2.7 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - - None - - - - - 2020-02-12
Gq/11 α11 Human Gα11iN: αN helix from Gαi1, for scFv16 63 β1 Human γ2 Human Cryo-EM 6OIJ 6OIJ_refined 3.3 ACM1 CHRM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - iperoxo pubchem gtoplig chembl_ligand
Small molecule Agonist acetylcholine Small molecule Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08
Gi/o αt1 Bovine rGaT: Gt/Gi1 chimera (18 res), nucleotide-free 64 β1 Bovine γT1 Bovine Cryo-EM 6OY9 - 3.9 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G 10.1016/J.MOLCEL.2019.06.007 2019-07-24
Gs αs Human GsiN18: Gαs N-term→Gαi(1-18), scFv16 56 β1 Human γ2 Human Cryo-EM 6XOX - 3.1 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - orforglipron pubchem gtoplig chembl_ligand pubchem drugbank
Small molecule Agonist (partial) glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Kawai T, Sun B, Yoshino H, Feng D, Suzuki Y, Fukazawa M, Nagao S, Wainscott DB, Showalter AD, Droz BA, Kobilka TS, Coghlan MP, Willard FS, Kawabe Y, Kobilka BK, Sloop KW 10.1073/PNAS.2014879117 2020-11-18
GPa1 family αPa1 strain ATCC 204508 / S288c Mini-Gpa1: muts, ΔAHD/switch III; α5 fragment 46 STE4 strain ATCC 204508 / S288c γ strain ATCC 204508 / S288c Cryo-EM 7AD3 - 3.5 STE2 STE2 STE2 STE2 D1 (Ste2-like fungal pheromone) strain ATCC 204508 / S288c - - - Alpha-factor mating pheromone pubchem
Peptide Agonist - - Velazhahan V, Ma N, Pandy-Szekeres G, Kooistra AJ, Lee Y, Gloriam DE, Vaidehi N, Tate CG 10.1038/S41586-020-2994-1 2020-12-09
Gs αs Human Engineered Gs protein for stabilization 57 β1 Rat γ2 Bovine Cryo-EM 7BW0 7BW0_refined 3.9 GPBAR GPBAR1 GPBA Bile acid A (Rhodopsin) Human BRIL Nanobody-35 - 23H
Small molecule Agonist lithocholic acid, deoxycholic acid, cholic acid, chenodeoxycholic acid Small molecule Chen G, Wang X, Ge Y, Ma L, Chen Q, Liu H, Du Y, Ye RD, Hu H, Ren R 10.1038/S41392-020-00262-Z 2020-09-02
Gs αs Human DN Gs: 8 muts S54N/G226A/E268A...I285T 58 β1 Human γ2 Human Cryo-EM 7CFM - 3.0 GPBAR GPBAR1 GPBA Bile acid A (Rhodopsin) Human BRIL Nanobody-35 - CHEMBL2331646 chembl_ligand pubchem
Small molecule Agonist lithocholic acid, deoxycholic acid, cholic acid, chenodeoxycholic acid Small molecule Yang F, Mao C, Guo L, Lin J, Ming Q, Xiao P, Wu X, Shen Q, Guo S, Shen DD, Lu R, Zhang L, Huang S, Ping Y, Zhang C, Ma C, Zhang K, Liang X, Shen Y, Nan F, Yi F, Luca VC, Zhou J, Jiang C, Sun JP, Xie X, Yu X, Zhang Y 10.1038/S41586-020-2569-1 2020-09-09
Gs αs Human DN Gs: S54N/G226A/E268A +5 more mutations 59 β1 Human γ2 Human Cryo-EM 7CFN 7CFN_refined 3.0 GPBAR GPBAR1 GPBA Bile acid A (Rhodopsin) Human BRIL Nanobody-35 - S-EMCA pubchem gtoplig chembl_ligand chembl_ligand pubchem
S-EMCA pubchem gtoplig chembl_ligand chembl_ligand pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		lithocholic acid, deoxycholic acid, cholic acid, chenodeoxycholic acid Small molecule - - 2020-09-09
Gs αs Human DNGas: DN Gs protein 60 β1 Human γ2 Human Cryo-EM 7CKZ - 3.1 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
mevidalen pubchem gtoplig chembl_ligand pubchem
Small molecule
Small molecule 		Agonist
PAM 		5-hydroxytryptamine, noradrenaline, dopamine Small molecule Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z 10.1016/J.CELL.2021.01.028 2021-03-03
Gq/11 αq Human mini-Gαs: Gαi1 N-term, Gαq α5; G203A/A326S 61 β1 Rat γ2 Bovine Cryo-EM 7EIB - 3.0 BKRB1 BDKRB1 B1 Bradykinin A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		[des-Arg10]kallidin (Human) pubchem gtoplig chembl_ligand uniprot
Peptide Agonist [des-Arg10]kallidin (Human), kallidin (Human), T-kinin (Human), Lys-[Hyp3]-bradykinin (Human), bradykinin (Human), [des-Arg9]bradykinin (Human), [Hyp3]bradykinin (Human) Peptide Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y 10.1038/S41594-021-00645-Y 2021-10-13
Gs αs Bovine Gαs: thermostab muts + bovine Gαi1 N-term 60 β1 Rat γ2 Bovine Cryo-EM 7EQ1 - 3.3 AGRG5 ADGRG5 ADGRG5 ADGRG B2 (Adhesion) Human - - - - - - - - Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP 10.1038/S41586-022-04619-Y 2022-05-11
Gq/11 αq Human Multifunctional Gα: Gs+Gi1 N-term+Gq α5 chimera 59 β1 Human γ2 Human Cryo-EM 7F9Y - 2.9 GHSR GHSR ghrelin Ghrelin A (Rhodopsin) Human BRIL Nanobody-35 - Ghrelin pubchem
OCTANOIC ACID chembl_ligand pubchem pubchem drugbank drug_central
Small molecule
Small molecule 		Agonist [des-Gln14]ghrelin (Mouse), liver enriched antimicrobial peptide 2 (Human), ghrelin (Mouse), [des-Gln14]ghrelin (Human), ghrelin (Human) Peptide Wang Y, Guo S, Zhuang Y, Yun Y, Xu P, He X, Guo J, Yin W, Xu HE, Xie X, Jiang Y 10.1038/S41467-021-25364-2 2021-08-18
Gq/11 αq Human mini-Gαs: Gαi1 N-term, Gαq α5 specificity 59 β1 Human γ2 Human Cryo-EM 7F9Z 7F9Z_refined 3.2 GHSR GHSR ghrelin Ghrelin A (Rhodopsin) Human BRIL Nanobody-35 - GHRP-6 pubchem gtoplig
Peptide Agonist [des-Gln14]ghrelin (Mouse), liver enriched antimicrobial peptide 2 (Human), ghrelin (Mouse), [des-Gln14]ghrelin (Human), ghrelin (Human) Peptide Wang Y, Guo S, Zhuang Y, Yun Y, Xu P, He X, Guo J, Yin W, Xu HE, Xie X, Jiang Y 10.1038/S41467-021-25364-2 2021-08-18
Gs αs Bovine mini-Gs: Gαi1 N-term/AHD; G226A/A366S/L272D 91 β1 Rat γ2 Bovine Cryo-EM 7FIG - 3.9 LSHR LHCGR LH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Glycoprotein hormones alpha chain
Choriogonadotropin subunit beta 3
Protein
Protein 		Agonist hCG (Human), LH (Human), LH (Rat), LH (Mouse) Peptide Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29
Gs αs Bovine bovine Gs/human Gi1 chimera, 3 DN muts 60 β1 Rat γ2 Bovine Cryo-EM 7FIH - 3.2 LSHR LHCGR LH Glycoprotein hormone A (Rhodopsin) Human - - - Chorionic gonadotropin alpha subunit
Chorionic gonadotropin beta subunit
Org43553 pubchem
Protein
Protein
Small molecule 		Agonist hCG (Human), LH (Human), LH (Rat), LH (Mouse) Peptide Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29
Gs αs Bovine mini-Gs: Gi1 N-term/AHD; G226A/A366S/L272D 91 β1 Rat γ2 Bovine Cryo-EM 7FII - 4.3 LSHR LHCGR LH Glycoprotein hormone A (Rhodopsin) Human - - - Chorionic gonadotropin alpha subunit
Chorionic gonadotropin beta subunit
Protein
Protein 		Agonist hCG (Human), LH (Human), LH (Rat), LH (Mouse) Peptide Duan J, Xu P, Cheng X, Mao C, Croll T, He X, Shi J, Luan X, Yin W, You E, Liu Q, Zhang S, Jiang H, Zhang Y, Jiang Y, Xu HE 10.1038/S41586-021-03924-2 2021-09-29
Gs αs Bovine DN bovine Gαs (DNGas): 9 stabilizing mutations 57 β1 Rat γ2 Bovine Cryo-EM 7FIM - 3.4 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human BRIL Nanobody-35 LgBiT tirzepatide pubchem gtoplig
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
Gs αs Bovine DNGs: 8 muts to stabilize complex 59 β1 Rat γ2 Bovine Cryo-EM 7FIN - 3.1 GIPR GIPR GIP Glucagon B1 (Secretin) Human BRIL Nanobody-35 - Peptide 20
Peptide Agonist gastric inhibitory polypeptide (Mouse), gastric inhibitory polypeptide (Human) Peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-02-23
Gs αs Bovine DN bovine Gαs (DNGas): 9 stabilizing mutations 60 β1 Rat γ2 Bovine Cryo-EM 7FIY - 3.4 GIPR GIPR GIP Glucagon B1 (Secretin) Human BRIL Nanobody-35 - tirzepatide pubchem gtoplig
Peptide Agonist gastric inhibitory polypeptide (Mouse), gastric inhibitory polypeptide (Human) Peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
Gq/11 αq Human miniGs/q70: Gs scaffold w/ Gq-like α5 helix 52 β1 Human γ2 Human Cryo-EM 7RMG - 3.0 NK1R TACR1 NK1 Tachykinin A (Rhodopsin) Human - Nanobody-35 - substance P (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A 10.1038/S41589-021-00890-8 2021-11-03
Gq/11 αq Human miniGs/q70: Gs body, Gq C-term α5 helix 52 β1 Human γ2 Human Cryo-EM 7RMI - 3.2 NK1R TACR1 NK1 Tachykinin A (Rhodopsin) Human - Nanobody-35 - Substance P 6-11 pubchem
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A 10.1038/S41589-021-00890-8 2021-11-03
Gq/11 αq Human MiniGq/i: Gs backbone+Gq/Gi muts; Gα-Gγ2 fusion 55 β1 Human γ2 Human Cryo-EM 7RYC - 2.9 OXYR OXTR OT Vasopressin and oxytocin A (Rhodopsin) Human - - - oxytocin (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem
Mg2+ pubchem gtoplig drugbank
Peptide
Small molecule 		Agonist
Cofactor 		vasopressin (Human), oxytocin (Human) Peptide Meyerowitz JG, Robertson MJ, Barros-Alvarez X, Panova O, Nwokonko RM, Gao Y, Skiniotis G 10.1038/S41594-022-00728-4 2022-03-09
Gi/o αi1 Rat DN Gαi1: G203A 63 β1 Bovine γ2 Bovine Cryo-EM 7S0F - 3.0 ADRB1 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey - - - LEVISOPRENALINE chembl_ligand pubchem drug_central
Small molecule Agonist - - Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY 10.1038/S41594-021-00679-2 2021-11-17
Gs αs Bovine Gi/s chimera: Gαi1(G203A)+Gs C-term(11aa) 56 β1 Bovine γ2 Bovine Cryo-EM 7S0G - 3.9 ADRB1 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey T4-Lysozyme - - LEVISOPRENALINE chembl_ligand pubchem drug_central
Small molecule Agonist - - Alegre KO, Paknejad N, Su M, Lou JS, Huang J, Jordan KD, Eng ET, Meyerson JR, Hite RK, Huang XY 10.1038/S41594-021-00679-2 2021-11-17
Gs αs Human DNGs: dominant-negative Gs protein 59 β1 Human γ2 Human Cryo-EM 7S3I - 2.5 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - - None - glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH 10.1038/S41589-021-00945-W 2022-01-05
Gq/11 αq Human mini-GαqiN: Gs body, Gq C-term α5 helix 57 β1 Human γ2 Human Cryo-EM 7S8L - 2.5 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human - - - CORTISTATIN-14 chembl_ligand pubchem
Peptide Agonist PAMP-20 (Human) Peptide Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gq/11 αq Human mini-Gs/Gq: Gs scaffold, Gq α5 for coupling 57 β1 Human γ2 Human Cryo-EM 7S8N 7S8N_refined 2.9 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human - - - (R)-ZINC-3573 pubchem gtoplig chembl_ligand
Small molecule Agonist PAMP-20 (Human) Peptide Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gq/11 αq Human mini-GαqiN: mini-Gs w/ Gq α5 helix 57 β1 Human γ2 Human Cryo-EM 7S8P 7S8P_refined 2.6 MRGX4 MRGPRX4 MRGPRX4 Orphan A (Rhodopsin) Human BRIL - - MS47134
Small molecule Agonist - - Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gq/11 αq Human mGsqiN: mini-Gs/q71 + Gαi1 N-term(1-30) 58 β1 Human γ2 Human Cryo-EM 7SR8 - 3.3 OX2R HCRTR2 OX2 Orexin A (Rhodopsin) Human - - - danavorexton pubchem gtoplig chembl_ligand pubchem drugbank
Small molecule Agonist orexin-B (Mouse), orexin-A (Human), orexin-B (Human) Peptide Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM 10.1038/S41467-022-30601-3 2022-06-08
Gq/11 αq Human miniGq: Gi2 scaffold + Gq α5 helix specificity 58 β1 Human γ2 Human Cryo-EM 7SRR 7SRR_refined 2.9 5HT2B HTR2B 5-HT2B 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist (partial) 5-hydroxytryptamine Small molecule Cao C, Barros-Alvarez X, Zhang S, Kim K, Damgen MA, Panova O, Suomivuori CM, Fay JF, Zhong X, Krumm BE, Gumpper RH, Seven AB, Robertson MJ, Krogan NJ, Huttenhain R, Nichols DE, Dror RO, Skiniotis G, Roth BL 10.1016/J.NEURON.2022.08.006 2022-09-21
Gq/11 αq Human mini-Gs/i/q chimera: G203A/A326S muts 59 β1 Rat γ2 Bovine Cryo-EM 20ZX - 3.0 LPAR5 LPAR5 LPA5 Lysophospholipid (LPA) A (Rhodopsin) Human - - - LYSOPHOSPHATIDIC ACID chembl_ligand pubchem
Small molecule Agonist LPA, N-arachidonoylglycine, farnesyl monophosphate, farnesyl diphosphate Small molecule None 10.1073/PNAS.2537482123 2026-06-17
Gs αs Human MiniGs construct 61 β1 Human γ2 Human Cryo-EM 21DU - 2.9 AGRG6 ADGRG6 ADGRG6 ADGRG B2 (Adhesion) Human - Nanobody-35 - apomorphine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule PAM - - None 10.1038/S41421-025-00866-1 2026-02-11
Gq/11 αq Human miniGsqi: mini-Gs w/ Gq/Gi C-term, Gγ2 fusion 58 β1 Rat γ2 Bovine Cryo-EM 24XY - 3.0 P2Y13 P2RY13 P2Y13 P2Y A (Rhodopsin) Human BRIL Nanobody-35 - ADP pubchem gtoplig chembl_ligand
Small molecule Agonist ADP, ATP Small molecule None 10.1016/J.BBRC.2026.153976 2026-06-10
Gq/11 αq Human MiniGq: mini-Gs scaffold, Gq α5 for specificity 57 β1 Human γ2 Mouse Cryo-EM 25IL - 3.2 MAS MAS1 MAS1 Orphan A (Rhodopsin) Human BRIL - LgBiT tag - None - - - None 10.1016/J.JMB.2026.169844 2026-05-20
Gi/o αgust Human Gα chimera: gustducin+Gαi1, α5 from gustducin 67 β3 Human γ13 Human Cryo-EM 25ST - 3.0 TA2R4 TAS2R4 TAS2R4 Taste 2 T2 (Taste 2) Human - - - L-Trp-Trp-Trp pubchem gtoplig chembl_ligand
Peptide Agonist - - - - 2026-06-24
Gi/o αgust Human Gαi1/Gαt3 chimera: α5 from gustducin(Gαt3) 67 β3 Human γ13 Human Cryo-EM 25SU - 3.3 TA2R4 TAS2R4 TAS2R4 Taste 2 T2 (Taste 2) Human - - - - None - - - - - 2026-07-15
Gi/o αt1 Bovine Transducin GαCT peptide (11-res) with K341L mut 3 - - - - X-ray 2X72 2X72_refined 3.0 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - None 10.1038/NATURE09795 2011-03-16
Gs αs Human modGαs: Gs/Gi1 chimera w/ DN muts 61 β1 Human γ2 Human Cryo-EM 8JLP - 3.2 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL - - ralmitaront pubchem gtoplig chembl_ligand
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gi/o αt1 Bovine GαCT2 peptide (transducin 340-350), K341L/C347V 3 - - - - X-ray 3PQR 3PQR_refined 2.9 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP 10.1038/NATURE09789 2011-03-09
Gs αs Bovine Nucleotide-free Gs: bovine α/γ, rat β subunits 89 β1 Rat γ2 Bovine X-ray 3SN6 - 3.2 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human T4-Lysozyme Nanobody-35 - CHEMBL1615159 chembl_ligand pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Rasmussen SG, DeVree BT, Zou Y, Kruse AC, Chung KY, Kobilka TS, Thian FS, Chae PS, Pardon E, Calinski D, Mathiesen JM, Shah ST, Lyons JA, Caffrey M, Gellman SH, Steyaert J, Skiniotis G, Weis WI, Sunahara RK, Kobilka BK 10.1038/NATURE10361 2011-07-20
Gi/o αt1 Bovine Gα C-term α5 fragment (340-350), K341L mutation 3 - - - - X-ray 4A4M 4A4M_refined 3.3 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Deupi X, Edwards P, Singhal A, Nickle B, Oprian D, Schertler G, Standfuss J 10.1073/PNAS.1114089108 2012-01-25
Gi/o αt1 Bovine GaCT2: transducin Gα C-term 11-res peptide 3 - - - - X-ray 4J4Q 4J4Q_refined 2.7 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - - None - - - Park JH, Morizumi T, Li Y, Hong JE, Pai EF, Hofmann KP, Choe HW, Ernst OP 10.1002/ANIE.201302374 2013-10-30
Gi/o αt1 Bovine GαCT peptide mimetic of transducin (Gt) 3 - - - - X-ray 4X1H 4X1H_refined 2.3 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - - None - - - Blankenship E, Vahedi-Faridi A, Lodowski DT 10.1016/J.STR.2015.09.015 2015-11-04
Gs αs Human Gs-short heterotrimer; AHD not modeled 47 β1 Human γ2 Human Cryo-EM 5UZ7 - 4.1 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - CALCITONIN SALMON chembl_ligand drug_central pubchem pubchem
Protein Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, Wootten D, Skiniotis G, Sexton PM 10.1038/NATURE22327 2017-05-03
Gi/o αt1 Bovine Transducin Gα1 C-term peptide (GαCT2, 340-350) 3 - - - - X-ray 5WKT 5WKT_refined 3.2 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - - None - - - Broecker J, Morizumi T, Ou WL, Klingel V, Kuo A, Kissick DJ, Ishchenko A, Lee MY, Xu S, Makarov O, Cherezov V, Ogata CM, Ernst OP 10.1038/NPROT.2017.135 2017-12-13
Gi/o αi1 Bovine Gαi1(bovine)/Gβ1(mouse)/Gγ2(human) heterotrimer 62 β1 Mouse γ2 Human Cryo-EM 6K42 - 4.1 ADA2B ADRA2B α2B Adrenoceptors A (Rhodopsin) Human T4-Lysozyme - - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15
Gs αs Human Gs heterotrimer 47 β1 Rat γ2 Bovine Cryo-EM 8W8X - 2.9 MC3R MC3R MC3 Melanocortin A (Rhodopsin) Human BRIL Nanobody-35 - Beta-MSH pubchem pubchem
Calcium pubchem
Small molecule
Small molecule 		Agonist
PAM 		ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide - - 2025-03-19
Gi/o αt1 Bovine Gt/Gi1 chimera: 18 Gnat1 res→Gαi1, purif 59 β1 Bovine γT1 Bovine Cryo-EM 6OYA - 3.3 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - Nanobody-35 - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Gao Y, Hu H, Ramachandran S, Erickson JW, Cerione RA, Skiniotis G 10.1016/J.MOLCEL.2019.06.007 2019-07-24
Gs αs Human DNGs: Gs/Gi1 chimera; Gs α5 tail retained 58 β1 Human γ2 Human Cryo-EM 6PB0 - 3.0 CRHR1 CRHR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - CHEMBL427807 chembl_ligand pubchem
Cholesterol pubchem drugbank
Protein
Small molecule 		Agonist
Cofactor 		corticotrophin-releasing hormone (Human), urocortin 1 (Human), urocortin 1 (Mouse), urocortin 2 (Human) Peptide Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12
Gi/o αt1 Bovine Transducin (Gnat1) C-term α5 fragment (11 res) 3 - - - - X-ray 6PEL 6PEL_refined 3.2 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - Citronellol pubchem
Small molecule Agonist - - - - 2020-06-24
Gi/o αt2 Bovine Gα C-terminal/α5 fragment (GαCT2 peptide) 3 - - - - X-ray 6PGS 6PGS_refined 2.9 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - Geraniol drugbank pubchem
Small molecule Agonist - - - - 2020-07-01
Gi/o αt2 Bovine Gα C-terminal α5 fragment (CT2 peptide) 3 - - - - X-ray 6PH7 6PH7_refined 2.9 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - nerol pubchem
Small molecule Agonist - - - - 2020-07-01
Gi/o αi1 Human Gi: human Gαi1, bovine Gβ1γ1 60 β1 Bovine γT1 Bovine Cryo-EM 6QNO - 4.4 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Tsai CJ, Marino J, Adaixo R, Pamula F, Muehle J, Maeda S, Flock T, Taylor NM, Mohammed I, Matile H, Dawson RJ, Deupi X, Stahlberg H, Schertler G 10.7554/ELIFE.46041 2019-07-10
Gi/o αi1 Rat DN rat Gαi1: S47N/G203A/E245A mutations 64 β1 Human γ2 Human Cryo-EM 6VMS - 3.8 DRD2 DRD2 D2 Dopamine A (Rhodopsin) Human T4-Lysozyme - - bromocriptine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist dopamine Small molecule Yin J, Chen KM, Clark MJ, Hijazi M, Kumari P, Bai XC, Sunahara RK, Barth P, Rosenbaum DM 10.1038/S41586-020-2379-5 2020-06-17
Gq/11 αq Human Mini-Gq/Gαi2 N-term chimera, for scFv16 binding 57 β1 Human γ2 Human Cryo-EM 6WHA - 3.4 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - CHEMBL5184791 chembl_ligand pubchem drugbank
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule Kim K, Che T, Panova O, DiBerto JF, Lyu J, Krumm BE, Wacker D, Robertson MJ, Seven AB, Nichols DE, Shoichet BK, Skiniotis G, Roth BL 10.1016/J.CELL.2020.08.024 2020-09-23
Gi/o αi1 Human DN heterotrimeric Gi protein 61 β1 Human γ2 Human Cryo-EM 6XBL - 3.9 SMO SMO SMO Oxysterol F (Frizzled) Human - - - SAG1.3 pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Agonist - - Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30
Gi/o αi1 Human Gi1 heterotrimer complex 61 β1 Human γ2 Human Cryo-EM 6XBM - 3.2 SMO SMO SMO Oxysterol F (Frizzled) Human - - - 24(S),25-Epoxycholesterol pubchem
Lipid Agonist - - Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30
Gq/11 αq Human GqiN chimera: Gq N-term→Gi1, for scFv16 63 β1 Human γ2 Human Cryo-EM 7DFL - 3.3 HRH1 HRH1 H1 Histamine A (Rhodopsin) Human - - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule Xia R, Wang N, Xu Z, Lu Y, Song J, Zhang A, Guo C, He Y 10.1038/S41467-021-22427-2 2021-03-31
Gs αs Bovine DN bovine Gs: S54N/G226A +6 more mutations 59 β1 Rat γ2 Bovine Cryo-EM 7DTY - 3.0 GIPR GIPR GIP Glucagon B1 (Secretin) Human BRIL Nanobody-35 Maltose-binding protein Gastric inhibitory polypeptide pubchem
Peptide Agonist gastric inhibitory polypeptide (Mouse), gastric inhibitory polypeptide (Human) Peptide Zhao F, Zhang C, Zhou Q, Hang K, Zou X, Chen Y, Wu F, Rao Q, Dai A, Yin W, Shen DD, Zhang Y, Xia T, Stevens RC, Xu HE, Yang D, Zhao L, Wang MW 10.7554/ELIFE.68719 2021-08-04
Gs αs Human mini-Gs: Gi1 N-term/AHD; 8 DN mutations 49 β1 Bovine γ2 Human Cryo-EM 7E14 - 2.9 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Compound 2 pubchem
orforglipron pubchem gtoplig chembl_ligand pubchem drugbank
Small molecule
Small molecule 		Ago-PAM
Agonist 		glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-021-24058-Z 2021-07-07
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S/E245A 62 β1 Human γ2 Human Cryo-EM 7E2X - 3.0 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - PtdIns4P pubchem
Cholesterol pubchem drugbank
Small molecule
Small molecule 		PAM 5-hydroxytryptamine Small molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S/E245A 62 β1 Human γ2 Human Cryo-EM 7E2Y - 3.0 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
PtdIns4P pubchem
Small molecule
Small molecule 		Agonist
PAM 		5-hydroxytryptamine Small molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14
Gi/o αi1 Human DN human Gαi1: S47N/G203A/A326S/E245A 62 β1 Human γ2 Human Cryo-EM 7E2Z - 3.1 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - aripiprazole pubchem gtoplig chembl_ligand drugbank drug_central pubchem
PtdIns4P pubchem
Small molecule
Small molecule 		Agonist (partial)
PAM 		5-hydroxytryptamine Small molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14
Gq/11 αq Human Gq chimera: N-term replaced w/ Gi1 (24aa) 62 β1 Human γ2 Human Cryo-EM 7F8W 7F8W_refined 3.1 GASR CCKBR CCK2 Cholecystokinin A (Rhodopsin) Human - - - desulfated gastrin-17 (Human) pubchem gtoplig uniprot chembl_ligand pubchem
Peptide Agonist gastrin-17 (Human), gastrin-34 (Human), CCK-33 (Mouse), gastrin-71 (Human), CCK-4 (Human), CCK-8 (Human), desulfated gastrin-17 (Human), CCK-33 (Human), desulfated gastrin-34 (Human), desulfated gastrin-71 (Human), desulfated gastrin-14 (Human), gastrin-17 (Rat), gastrin-14 (Human), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q 10.1038/S41589-021-00866-8 2021-10-13
Gq/11 αq Human Gαq chimera: αN from Gαi1, DN G203A/A326S 63 β1 Human γ2 Human Cryo-EM 7EZM - 2.9 CCKAR CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CCK-8 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Peptide Agonist gastrin-17 (Human), CCK-33 (Mouse), CCK-4 (Human), CCK-8 (Human), CCK-33 (Human), gastrin-17 (Rat), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y 10.1038/S41589-021-00841-3 2021-08-25
Gs αs Human DN human Gs: 8 stabilizing mutations 58 β1 Rat γ2 Bovine Cryo-EM 7F16 - 2.8 PTH2R PTH2R PTH2 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Tuberoinfundibular peptide of 39 residues
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), PTHrP-(1-34) (human) (Human), TIP39 (Human), PTH (Human), TIP39 (Mouse), PTH (Mouse), PTH (Rat) Peptide Wang X, Cheng X, Zhao L, Wang Y, Ye C, Zou X, Dai A, Cong Z, Chen J, Zhou Q, Xia T, Jiang H, Xu HE, Yang D, Wang MW 10.1073/PNAS.2101279118 2021-08-18
Gq/11 αq Human mini-Gs/q71/i1 chimera: G203A/A326S muts 60 β1 Rat γ2 Bovine Cryo-EM 7F2O - 2.9 BKRB2 BDKRB2 B2 Bradykinin A (Rhodopsin) Human BRIL - LgBiT bradykinin (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot drugbank
Peptide Agonist [des-Arg10]kallidin (Human), kallidin (Human), T-kinin (Human), Lys-[Hyp3]-bradykinin (Human), bradykinin (Human), [des-Arg9]bradykinin (Human), [Hyp3]bradykinin (Human) Peptide Yin YL, Ye C, Zhou F, Wang J, Yang D, Yin W, Wang MW, Xu HE, Jiang Y 10.1038/S41594-021-00645-Y 2021-10-13
Gs αs Human Gs/Gi chimera: Gαi N-term/AHD, G226A/A366S 59 β1 Human γ2 Human Cryo-EM 7F4D - 3.0 MSHR MC1R MC1 Melanocortin A (Rhodopsin) Human BRIL Nanobody-35 LgBiT Alpha-MSH pubchem
Calcium pubchem
Small molecule
Small molecule 		Agonist
PAM 		ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat) Peptide Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE 10.1038/S41422-021-00557-Y 2021-09-08
Gs αs Human miniGs: N-term & AHD from Gαi1, scFv16 59 β1 Human γ2 Human Cryo-EM 7F4F - 2.9 MSHR MC1R MC1 Melanocortin A (Rhodopsin) Human BRIL - LgBiT afamelanotide pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank drug_central pubchem
Calcium pubchem
Peptide
Small molecule 		Agonist
PAM 		ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat) Peptide Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE 10.1038/S41422-021-00557-Y 2021-09-08
Gs αs Human Gαs/Gαi chimera: G226A/A366S DN muts 59 β1 Human γ2 Human Cryo-EM 7F4H - 2.7 MSHR MC1R MC1 Melanocortin A (Rhodopsin) Human BRIL Nanobody-35 LgBiT afamelanotide pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank drug_central pubchem
Calcium pubchem
Peptide
Small molecule 		Agonist
PAM 		ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat) Peptide Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE 10.1038/S41422-021-00557-Y 2021-09-08
Gs αs Human MiniGs: Gs/Gi1 chimera, 10 stabilizing muts 59 β1 Human γ2 Human Cryo-EM 7F4I 7F4I_refined 3.1 MSHR MC1R MC1 Melanocortin A (Rhodopsin) Human BRIL Nanobody-35 LgBiT SHU9119 pubchem
Calcium pubchem
Peptide
Small molecule 		Agonist (partial)
PAM 		ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat) Peptide Ma S, Chen Y, Dai A, Yin W, Guo J, Yang D, Zhou F, Jiang Y, Wang MW, Xu HE 10.1038/S41422-021-00557-Y 2021-09-08
Gq/11 αq Human Gαq: DN mutations R183Q/Q209L 97 β1 Human γ2 Human Cryo-EM 7F6G 7F6G_refined 2.9 AGTR1 AGTR1 AT1 Angiotensin A (Rhodopsin) Human - - Maltose-binding protein (MBP) CHEMBL216061 chembl_ligand pubchem
Protein Agonist angiotensin III (Human), angiotensin A (Human), angiotensin II (Human), angiotensin IV (Human) Peptide - - 2023-03-29
Gq/11 αq Human DN Gαq: R183Q/Q209L mutations 63 β1 Human γ2 Human Cryo-EM 7F6H 7F6H_refined 2.9 BKRB2 BDKRB2 B2 Bradykinin A (Rhodopsin) Human - - Maltose-binding protein bradykinin (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot drugbank
Peptide Agonist [des-Arg10]kallidin (Human), kallidin (Human), T-kinin (Human), Lys-[Hyp3]-bradykinin (Human), bradykinin (Human), [des-Arg9]bradykinin (Human), [Hyp3]bradykinin (Human) Peptide Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H 10.1038/S41467-022-28399-1 2022-01-05
Gs αs Bovine Bovine Gs: Gαs/Gβ1/Gγ2, Gγ2 C68S mutation 51 β1 Bovine γ2 Bovine Cryo-EM 7JJO - 2.6 ADRB1 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey - Nanobody-35 - LEVISOPRENALINE chembl_ligand pubchem drug_central
Small molecule Agonist - - Su M, Zhu L, Zhang Y, Paknejad N, Dey R, Huang J, Lee MY, Williams D, Jordan KD, Eng ET, Ernst OP, Meyerson JR, Hite RK, Walz T, Liu W, Huang XY 10.1016/J.MOLCEL.2020.08.001 2020-09-02
Gs αs Human DNGas: S54N/G226A/E268A +6 more mutations 53 β1 Human γ2 Human Cryo-EM 7KI0 - 2.5 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - semaglutide pubchem gtoplig chembl_ligand pubchem chembl_ligand drugbank chembl_ligand pubchem
Protein Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D 10.1016/J.CELREP.2021.109374 2021-08-04
Gq/11 αq Human mini-Gsqi: Gαi1 αN-helix + mini-Gs/q71 64 β1 Human γ2 Human Cryo-EM 7L1U - 3.2 OX2R HCRTR2 OX2 Orexin A (Rhodopsin) Human - - - orexin-B (Human) pubchem gtoplig chembl_ligand uniprot
Protein Agonist orexin-B (Mouse), orexin-A (Human), orexin-B (Human) Peptide Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K 10.1038/S41467-021-21087-6 2021-02-10
Gq/11 αq Human mini-Gsq71/i1 chimera: αN helix, scFv16 64 β1 Human γ2 Human Cryo-EM 7L1V - 3.0 OX2R HCRTR2 OX2 Orexin A (Rhodopsin) Human - Synthetic nanobody 51 - compound 1 [PMID: 33547286] pubchem gtoplig chembl_ligand
Small molecule Agonist orexin-B (Mouse), orexin-A (Human), orexin-B (Human) Peptide Hong C, Byrne NJ, Zamlynny B, Tummala S, Xiao L, Shipman JM, Partridge AT, Minnick C, Breslin MJ, Rudd MT, Stachel SJ, Rada VL, Kern JC, Armacost KA, Hollingsworth SA, O'Brien JA, Hall DL, McDonald TP, Strickland C, Brooun A, Soisson SM, Hollenstein K 10.1038/S41467-021-21087-6 2021-02-10
Gs αs Human Human mini-Gs (miniGs_DN) 60 β1 Rat γ2 Bovine Cryo-EM 7LJC - 3.0 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - mevidalen pubchem gtoplig chembl_ligand pubchem
SKF-81297 pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		5-hydroxytryptamine, noradrenaline, dopamine Small molecule Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE 10.1038/S41422-021-00482-0 2021-03-03
Gs αs Human MiniGα_DN: DN mutation S252N 60 β1 Rat γ2 Bovine Cryo-EM 7LJD - 3.2 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - mevidalen pubchem gtoplig chembl_ligand pubchem
dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		5-hydroxytryptamine, noradrenaline, dopamine Small molecule Zhuang Y, Krumm B, Zhang H, Zhou XE, Wang Y, Huang XP, Liu Y, Cheng X, Jiang Y, Jiang H, Zhang C, Yi W, Roth BL, Zhang Y, Xu HE 10.1038/S41422-021-00482-0 2021-03-03
Gq/11 αq Human mGsqi: mini-Gs + Gq α5 helix + Gi1 αN helix 55 β1 Rat γ2 Human Cryo-EM 7MBY - 2.4 CCKAR CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CCK-8 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Peptide Agonist gastrin-17 (Human), CCK-33 (Mouse), CCK-4 (Human), CCK-8 (Human), CCK-33 (Human), gastrin-17 (Rat), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM 10.1371/JOURNAL.PBIO.3001295 2021-05-26
Gq/11 αq Human mGsqi: mini-Gs w/ Gαi1 N-term (18 res) 59 β1 Human γ2 Human Cryo-EM 7P00 - 2.7 NK1R TACR1 NK1 Tachykinin A (Rhodopsin) Human - - - substance P (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A 10.1126/SCIADV.ABK2872 2021-12-15
Gq/11 αq Human Mini-Go: Gαq α5 helix + Gαi1 N-term chimera 57 β1 Human γ2 Human Cryo-EM 7QVM - 3.3 OXYR OXTR OT Vasopressin and oxytocin A (Rhodopsin) Human - - - oxytocin (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem
Peptide Agonist vasopressin (Human), oxytocin (Human) Peptide Waltenspuhl Y, Ehrenmann J, Vacca S, Thom C, Medalia O, Pluckthun A 10.1038/S41467-022-31325-0 2022-08-10
Gq/11 αq Human Mini-Gq (Gi2-mini-Gq chimera) 60 β1 Human γ2 Human Cryo-EM 7RAN - 3.5 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - CHEMBL5399968 chembl_ligand pubchem pubchem
Small molecule Agonist (partial) tryptamine, 5-hydroxytryptamine Small molecule Kaplan AL, Confair DN, Kim K, Barros-Alvarez X, Rodriguiz RM, Yang Y, Kweon OS, Che T, McCorvy JD, Kamber DN, Phelan JP, Martins LC, Pogorelov VM, DiBerto JF, Slocum ST, Huang XP, Kumar JM, Robertson MJ, Panova O, Seven AB, Wetsel AQ, Wetsel WC, Irwin JJ, Skiniotis G, Shoichet BK, Roth BL, Ellman JA 10.1038/S41586-022-05258-Z 2022-07-06
Gq/11 α11 Human Gα11iN18: N-term(1-18) from Gαi1, scFv16 97 β1 Human γ2 Human Cryo-EM 7RKF - 4.0 US28 US28 US28 Unclassified A (Rhodopsin) strain AD169 - - - Fractalkine
Protein Agonist - - Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC 10.1126/SCIADV.ABL5442 2022-01-26
Gi/o αi1 Human Wild-type human Gi heterotrimer 61 β1 Human γ2 Human Cryo-EM 7RKM - 3.5 US28 US28 US28 Unclassified A (Rhodopsin) strain AD169 - - - Fractalkine
Protein Agonist (partial) - - Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC 10.1126/SCIADV.ABL5442 2022-01-26
Gs αs Human miniGs399: thermostabilized Gαs RAS domain 56 β1 Human γ2 Human Cryo-EM 7UTZ - 2.4 TSHR TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - TR1402 (chain B)
TR1402 (chain A)
DPPC pubchem
Protein
Protein
Lipid 		Agonist TSH (Rat), TSH (Human), TSH (Mouse) Peptide Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S/E245A 64 β1 Human γ2 Human Cryo-EM 7VKT 7VKT_refined 2.9 LT4R1 LTB4R BLT1 Leukotriene A (Rhodopsin) Human - - - LTB4 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist 20-hydroxy-LTB4, LTB4, 12R-HETE Small molecule Wang N, He X, Zhao J, Jiang H, Cheng X, Xia Y, Eric Xu H, He Y 10.1038/S41467-022-28820-9 2022-03-09
Gs αs Bovine DN bovine Gs: 9 stabilizing mutations 60 β1 Rat γ2 Bovine Cryo-EM 7VQX - 2.7 VIPR2 VIPR2 VPAC2 VIP and PACAP B1 (Secretin) Human - Nanobody-35 LgBiT PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Protein Agonist VIP (Human), GHRH (Rat), secretin (Mouse), GHRH (Mouse), PHI (Mouse), GHRH (Human), PACAP-38 (Human), secretin (Rat), secretin (Pig), PACAP-27 (Human) Protein Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW 10.1038/S41467-022-30041-Z 2022-05-18
Gq/11 αq Human MiniGs/q: Gq-mimic backbone, I372A mutation 62 β1 Human γ2 Human Cryo-EM 7VUH 7VUH_refined 3.2 GP139 GPR139 GPR139 Orphan A (Rhodopsin) Human - Nanobody-35 Endo-1
4-beta-xylanase 		JNJ-63533054 pubchem gtoplig chembl_ligand
Small molecule Agonist D-tryptophan, D-phenylalanine Small molecule Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ 10.1038/S41422-021-00591-W 2021-12-29
Gq/11 αq Human MiniGs/q: I372A mutation in α5 helix 60 β1 Human γ2 Human Cryo-EM 7VUI 7VUI_refined 3.3 GP139 GPR139 GPR139 Orphan A (Rhodopsin) Human - Nanobody-35 Endo-1
4-beta-xylanase 		JNJ-63533054 pubchem gtoplig chembl_ligand
Small molecule Agonist D-tryptophan, D-phenylalanine Small molecule Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ 10.1038/S41422-021-00591-W 2021-12-29
Gq/11 αq Human miniGs/q: Gs + Gq C-term, I372A mutation 60 β1 Human γ2 Human Cryo-EM 7VUJ 7VUJ_refined 3.8 GP139 GPR139 GPR139 Orphan A (Rhodopsin) Human - Nanobody-35 Endo-1
4-beta-xylanase 		JNJ-63533054 pubchem gtoplig chembl_ligand
Small molecule Agonist D-tryptophan, D-phenylalanine Small molecule Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ 10.1038/S41422-021-00591-W 2021-12-29
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 7VUY - 2.8 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human BRIL - - CHEMBL5665416 chembl_ligand pubchem pubchem
Small molecule Agonist PAMP-20 (Human) Peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 7VUZ 7VUZ_refined 2.9 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human - - - CHEMBL5665416 chembl_ligand pubchem pubchem
Small molecule Agonist PAMP-20 (Human) Peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gq/11 αq Human mGαs/q/iN: N-term replaced by Gαi1 59 β1 Human γ2 Human Cryo-EM 7W56 - 2.9 NMUR1 NMUR1 NMU1 Neuromedin U A (Rhodopsin) Human BRIL - LgBiT Neuromedin-S
Peptide Agonist neuromedin U-25 (Human), neuromedin S-36 (Mouse), neuromedin S-36 (Rat), neuromedin U-23 (Mouse), neuromedin S-33 (Human), neuromedin U-23 (Rat) Peptide You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y 10.1038/S41467-022-29683-W 2022-04-20
Gq/11 αq Human mGαs/q/iN: Gαi1 N-term, Gαq α5 helix 59 β1 Human γ2 Human Cryo-EM 7W57 - 3.2 NMUR2 NMUR2 NMU2 Neuromedin U A (Rhodopsin) Human BRIL - - Neuromedin-S
Peptide Agonist neuromedin U-25 (Human), neuromedin S-36 (Mouse), neuromedin S-36 (Rat), neuromedin S-33 (Human), neuromedin U-23 (Rat) Peptide You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y 10.1038/S41467-022-29683-W 2022-04-20
Gi/o αo Human Go heterotrimer used for complex formation 59 β1 Human γ2 Human Cryo-EM 7W7E - 3.4 ADA2A ADRA2A α2A Adrenoceptors A (Rhodopsin) Human - - - CHEMBL5517987 chembl_ligand pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P 10.1126/SCIENCE.ABN7065 2022-09-28
Gs αs Bovine DN Gs heterotrimer: Gα 9 muts incl A366S 60 β1 Rat γ2 Bovine Cryo-EM 7WBJ - 3.4 VIPR2 VIPR2 VPAC2 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Protein Agonist VIP (Human), GHRH (Rat), secretin (Mouse), GHRH (Mouse), PHI (Mouse), GHRH (Human), PACAP-38 (Human), secretin (Rat), secretin (Pig), PACAP-27 (Human) Protein Xu Y, Feng W, Zhou Q, Liang A, Li J, Dai A, Zhao F, Yan J, Chen CW, Li H, Zhao LH, Xia T, Jiang Y, Xu HE, Yang D, Wang MW 10.1038/S41467-022-30041-Z 2022-05-18
Gq/11 αq Human Gs/Gi1 backbone chimera w/ Gq α5 (per paper) 60 β1 Human γ2 Human Cryo-EM 7WKD - 3.0 TRFR TRHR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human - - - TRH (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem pubchem
Peptide Agonist TRH (Human) Peptide Xu Y, Cai H, You C, He X, Yuan Q, Jiang H, Cheng X, Jiang Y, Xu HE 10.1038/S41422-022-00641-X 2022-06-15
Gq/11 αq Human Gq chimera: mini-Gαs scaffold, Gαi1 N-term 60 β1 Rat γ2 Bovine Cryo-EM 7WQ4 7WQ4_refined 2.6 GALR2 GALR2 GAL2 Galanin A (Rhodopsin) Human - Nanobody-35 - galanin(1-13)amide gtoplig pubchem
Peptide Agonist galanin-like peptide (Human), galanin (Human), galanin-like peptide (Rat), galanin-like peptide (Mouse), spexin-1 (Human) Protein Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y 10.1038/S41467-022-29072-3 2022-04-20
Gs αs Human DN miniGαs: G49D/E50N/A249D+ muts, ΔAHD 54 β1 Human γ2 Human Cryo-EM 7WU3 - 3.1 AGRF1 ADGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - LPC 16:0
Lipid PAM - - Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gi/o αi1 Human MiniGi1: ΔAHD + 8 stabilizing mutations 58 β1 Human γ2 Human Cryo-EM 7WU5 - 3.0 AGRF1 ADGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - - - LPC 16:0
Lipid Allosteric agonist - - Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gs αs Human Human mini-Gs; Gi1 N-term chimera, Nb35/scFv16 58 β1 Human γ2 Human Cryo-EM 7WUI - 3.1 AGRG2 Adgrg2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 mCherry IP15
Peptide Agonist - - Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27
Gq/11 αq Human Mini-Gαq construct 60 β1 Human γ2 Human Cryo-EM 7WXU - 2.9 AGRF1 ADGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - - - - - - Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y 10.1038/S41467-022-33173-4 2022-09-28
Gq/11 αq Human Mini-Gαq subunit 59 β1 Human γ2 Human Cryo-EM 7WY5 - 2.8 AGRL3 Adgrl3 ADGRL3 ADGRL B2 (Adhesion) Mouse - Nanobody-35 - - - - - - Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y 10.1016/J.MOLCEL.2022.10.009 2022-10-26
Gq/11 αq Human Mini-Gαq, NanoBiT tether + ScFv16 stabilized 57 β1 Bovine γ2 Bovine Cryo-EM 7X1T - 3.3 TRFR TRHR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human - - - taltirelin pubchem gtoplig chembl_ligand drug_central
Small molecule Agonist TRH (Human) Peptide Yang F, Zhang H, Meng X, Li Y, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41422-022-00646-6 2022-08-31
Gs αs Human Mini-Gs399: truncated/mutated, receptor-fused 58 β1 Human γ2 Human Cryo-EM 7X2C 7X2C_refined 3.2 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - fenoldopam pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand pubchem gtoplig pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S 10.1038/S41467-022-30929-W 2022-06-29
Gs αs Human DNGs: DN Gs based on mini-Gs G112 59 β1 Rat γ2 Human Cryo-EM 7X8R - 2.6 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL2158411 chembl_ligand pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW 10.1073/PNAS.2200155119 2022-06-29
Gs αs Human G112 (DNGαs, mini-Gs); Gβ-HiBiT fusion 60 β1 Rat γ2 Human Cryo-EM 7X8S 7X8S_refined 3.1 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL2158488 chembl_ligand pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cong Z, Zhou Q, Li Y, Chen LN, Zhang ZC, Liang A, Liu Q, Wu X, Dai A, Xia T, Wu W, Zhang Y, Yang D, Wang MW 10.1073/PNAS.2200155119 2022-06-29
Gq/11 αq Human mGαqiN: mini-Gs + Gq α5 + Gi1 N-term 60 β1 Human γ2 Human Cryo-EM 7XBD 7XBD_refined 3.1 GALR2 GALR2 GAL2 Galanin A (Rhodopsin) Human BRIL - - galanin(1-13)amide gtoplig pubchem
Peptide Agonist galanin-like peptide (Human), galanin (Human), galanin-like peptide (Rat), galanin-like peptide (Mouse), spexin-1 (Human) Protein Heo Y, Ishimoto N, Jeon YE, Yun JH, Ohki M, Anraku Y, Sasaki M, Kita S, Fukuhara H, Ikuta T, Kawakami K, Inoue A, Maenaka K, Tame JRH, Lee W, Park SY 10.1371/JOURNAL.PBIO.3001714 2022-07-13
Gi/o αgust Human mini-Gs/gust: C-term α5 from gustducin 63 β1 Human γ2 Human Cryo-EM 7XP4 - 3.0 T2R46 TAS2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - Nanobody-35 Endoglucanase H - None - - - Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T 10.1126/SCIENCE.ABO1633 2022-10-12
Gi/o αgust Human miniGs/gust: α5 helix from gustducin 63 β1 Human γ2 Human Cryo-EM 7XP5 - 3.1 T2R46 TAS2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - Nanobody-35 Endoglucanase H - None - - - - - 2022-10-12
Gi/o αgust Human mini-Gs/gustducin: α5 helix from gustducin 63 β1 Human γ2 Human Cryo-EM 7XP6 - 3.0 T2R46 TAS2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - Nanobody-35 Endoglucanase H strychnine pubchem gtoplig chembl_ligand drug_central drugbank
Small molecule Agonist - - Xu W, Wu L, Liu S, Liu X, Cao X, Zhou C, Zhang J, Fu Y, Guo Y, Wu Y, Tan Q, Wang L, Liu J, Jiang L, Fan Z, Pei Y, Yu J, Cheng J, Zhao S, Hao X, Liu ZJ, Hua T 10.1126/SCIENCE.ABO1633 2022-10-12
Gs αs Human Engineered mini-Gs: deletions + stabilizing muts 59 β1 Human γ2 Human Cryo-EM 7XV3 7XV3_refined 2.8 GP174 GPR174 GPR174 Orphan A (Rhodopsin) Human - Nanobody-35 - LysoPS(18:0)
Small molecule Agonist lysophosphatidylserine Lipid Liang J, Inoue A, Ikuta T, Xia R, Wang N, Kawakami K, Xu Z, Qian Y, Zhu X, Zhang A, Guo C, Huang Z, He Y 10.1038/S41467-023-36575-0 2023-02-15
Gs αs Human DN mini-Gs: G226A/A366S/L272D mutations 59 β1 Human γ2 Human Cryo-EM 7XW6 - 2.8 TSHR TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - M22 antibody (chain Y)
M22 antibody (chain L)
ML-109 pubchem
Protein
Protein
Small molecule 		Agonist TSH (Rat), TSH (Human), TSH (Mouse) Peptide Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE 10.1038/S41586-022-05173-3 2022-08-17
Gq/11 αq Human GαsqiN chimera; Gq specificity determinant 58 β1 Rat γ2 Bovine Cryo-EM 7XW9 - 2.7 TRFR TRHR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human BRIL - - TRH (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem pubchem
Peptide Agonist TRH (Human) Peptide - - 2022-12-28
Gq/11 αq Human Engineered Gαq protein (G324) 59 β1 Rat γ2 Bovine Cryo-EM 7XWO 7XWO_refined 2.7 NK2R TACR2 NK2 Tachykinin A (Rhodopsin) Human BRIL - - neurokinin A (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide - - 2023-05-31
Gq/11 α11 Human Gα11/Gαi1 chimeric Gα, stabilized w/ scFv16 63 β1 Human γ2 Human Cryo-EM 7XXH 7XXH_refined 2.9 P2RY1 P2RY1 P2Y1 P2Y A (Rhodopsin) Human - - - 2MeSADP pubchem gtoplig chembl_ligand
Small molecule Agonist ADP, ATP Small molecule - - 2023-06-07
Gi/o αi1 Human DN Gi: G203A/A326S 62 β1 Mouse γ2 Mouse Cryo-EM 7Y15 7Y15_refined 2.9 MRGRD MRGPRD MRGPRD Orphan A (Rhodopsin) Human BRIL - - - None - β-alanine Small molecule Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A 10.1038/S42003-022-03668-3 2022-07-20
Gq/11 αq Human Mini-Gαs/q: Gs scaffold, Gq-coupling specificity 60 β1 Human γ2 Human Cryo-EM 7YDM - 2.9 AGRE5 ADGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - Nanobody-35 - - - - - - Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
Gq/11 αq Human Gα chimera: Gs+Gi1 N-term, DN muts, mimics Gq 62 β1 Human γ2 Human Cryo-EM 7YFC - 3.0 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human - Nanobody-35 - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule Im D, Kishikawa JI, Shiimura Y, Hisano H, Ito A, Fujita-Fujiharu Y, Sugita Y, Noda T, Kato T, Asada H, Iwata S 10.1038/S41467-023-42260-Z 2023-10-25
Gq/11 αq Human miniGqiN: mini-Gs + Gαi1 N-term35, G203A/A326S 62 β1 Human γ2 Human Cryo-EM 7YFD - 3.1 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human - Nanobody-35 - imetit pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule Im D, Kishikawa JI, Shiimura Y, Hisano H, Ito A, Fujita-Fujiharu Y, Sugita Y, Noda T, Kato T, Asada H, Iwata S 10.1038/S41467-023-42260-Z 2023-10-25
Gi/o αi2 Human DN Gαi2: S47N/G204A/E246A/A327S 58 β1 Bovine γ2 Bovine Cryo-EM 7YJ4 - 3.2 RL3R2 RXFP4 RXFP4 Relaxin family peptide A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		INSL5 (chain A)
INSL5 (chain B)
Peptide
Peptide 		Agonist relaxin-3 (B chain) (Human), relaxin-3 (Human), INSL5 (Human) Peptide Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW 10.1038/S41467-023-36182-Z 2023-03-01
Gs αs Bovine WT bovine Gs, Gγ C68S mutation 51 β1 Bovine γ2 Bovine Cryo-EM 8DCR - 2.6 ADRB1 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey T4-Lysozyme Nanobody-35 - DOBUTAMINE pubchem
Small molecule Agonist (partial) - - Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY 10.1038/S41467-022-31823-1 2022-07-27
Gs αs Bovine Bovine Gs heterotrimer, nucleotide-free 51 β1 Bovine γ2 Bovine Cryo-EM 8DCS - 2.5 ADRB1 ADRB1 β1 Adrenoceptors A (Rhodopsin) Wild turkey T4-Lysozyme Nanobody-35 - 4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile pubchem drugbank
Small molecule Agonist (partial) - - Su M, Paknejad N, Zhu L, Wang J, Do HN, Miao Y, Liu W, Hite RK, Huang XY 10.1038/S41467-022-31823-1 2022-07-27
Gq/11 αq Human Mini-GalphaqiN: Gq/Gi2 chimera 57 β1 Human γ2 Human Cryo-EM 8DPF - 2.8 5HT2C HTR2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - - - lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist 5-hydroxytryptamine Small molecule Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24
Gq/11 αq Human Mini-GaqiN: Gαi2/Gαq chimera, Gαq α5 helix 57 β1 Human γ2 Human Cryo-EM 8DPG - 3.6 5HT2C HTR2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - - - psilocin pubchem gtoplig chembl_ligand
Small molecule Agonist (partial) 5-hydroxytryptamine Small molecule Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24
Gq/11 αq Human mini-GαqiN: Gi2-mini-Gq chimeric Gα protein 57 β1 Human γ2 Human Cryo-EM 8DPH - 3.2 5HT2C HTR2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - - - lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist 5-hydroxytryptamine Small molecule Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24
Gq/11 αq Human Mini-GαqiN: Gi2-miniGq chimera 57 β1 Human γ2 Human Cryo-EM 8DPI - 3.4 5HT2C HTR2C 5-HT2C 5-Hydroxytryptamine A (Rhodopsin) Human - - - lorcaserin pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist 5-hydroxytryptamine Small molecule Gumpper RH, Fay JF, Roth BL 10.1016/J.CELREP.2022.111211 2022-08-24
Gq/11 αq Human miniGq: mini-Gs backbone + Gq α5 helix 57 β1 Human γ2 Human Cryo-EM 8E9W - 2.7 ACM3 CHRM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - CHEMBL73538 chembl_ligand pubchem
Small molecule Agonist acetylcholine Small molecule Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30
Gq/11 αq Human miniGq: mini-Gs scaffold + Gαq C-term α5 helix 56 β1 Human γ2 Human Cryo-EM 8E9Y - 2.8 ACM3 CHRM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - Clozapine N-oxide pubchem
Small molecule Agonist acetylcholine Small molecule Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30
Gq/11 αq Human miniGq: Gs/Gq chimera, Gq specificity determinants 57 β1 Human γ2 Human Cryo-EM 8E9Z - 2.7 ACM3 CHRM3 M3 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - iperoxo pubchem gtoplig chembl_ligand
Small molecule Agonist acetylcholine Small molecule Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30
Gi/o αi1 Human DN Gαi1: G203A/A326S 61 β1 Rat γ2 Bovine Cryo-EM 8EFQ - 3.3 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - DAMGO pubchem gtoplig chembl_ligand pubchem
MONOETHANOLAMINE chembl_ligand pubchem drugbank
Peptide
Small molecule 		Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
Gq/11 αq Human mGsqiN: mini-Gs scaffold + Gs/Gq/Gi elements 59 β1 Human γ2 Human Cryo-EM 8EIT - 2.8 FFAR1 FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human T4-Lysozyme - - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Small molecule Agonist oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid Small molecule Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM 10.1073/PNAS.2219569120 2023-05-24
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 8F2B - 2.0 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- pramlintide analogue San45
N-hexadecanoyl-L-glutamic acid pubchem
Peptide
Small molecule 		Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02
Gi/o αi1 Human Gai1_4M (labeled Gs): S47N/G203A/E245A/A326S 64 β1 Rat γ2 Bovine Cryo-EM 8F7Q - 3.2 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - Beta-endorphin pubchem
Peptide Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE 10.1016/J.CELL.2022.12.026 2022-12-14
Gi/o αi1 Human Gαi1_4M: S47N/G203A/E245A/A326S mutations 63 β1 Rat γ2 Bovine Cryo-EM 8F7R - 3.3 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - endomorphin-1 (Human) pubchem gtoplig chembl_ligand
Peptide Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE 10.1016/J.CELL.2022.12.026 2022-12-14
Gq/11 αq Human MiniGsq71: Gαs backbone, Gαq α5 helix 57 β1 Human γ2 Human Cryo-EM 8FMZ - 2.6 NTR1 Ntsr1 NTS1 Neurotensin A (Rhodopsin) Rat - - - NTS8–13 pubchem
Peptide Agonist neurotensin (Human), neuromedin N (Mouse) Peptide Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
Gi/o αi1 Mouse DNGai1: dominant-negative Gα subunit 64 β1 Human γ2 Human Cryo-EM 8FX5 - 2.5 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - xanomeline pubchem gtoplig chembl_ligand drug_central drugbank pubchem
xanomeline pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule
Small molecule 		Agonist
PAM 		acetylcholine Small molecule Burger WAC, Pham V, Vuckovic Z, Powers AS, Mobbs JI, Laloudakis Y, Glukhova A, Wootten D, Tobin AB, Sexton PM, Paul SM, Felder CC, Danev R, Dror RO, Christopoulos A, Valant C, Thal DM 10.1038/S41467-023-41199-5 2023-09-13
Gq/11 αq Human miniGs/q chimera: Gαq α5 specificity residues 52 β1 Human γ2 Human Cryo-EM 8G2Y - 3.4 AGRF1 ADGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - - None - - - Jones DTD, Dates AN, Rawson SD, Burruss MM, Lipper CH, Blacklow SC 10.1038/S41467-023-38083-7 2023-05-10
Gi/o αi1 Human Gi heterotrimer 62 β1 Human γ2 Human Cryo-EM 8G94 8G94_refined 3.2 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - - Early activation antigen CD69
Protein Allosteric agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Chen H, Qin Y, Chou M, Cyster JG, Li X 10.7554/ELIFE.88204 2023-04-19
G12/13 α13 Human Gα13/iN: N-term(1-18) replaced by Gαi1 60 β1 Human γ2 Human Cryo-EM 8H8J 8H8J_refined 3.2 GPR35 GPR35 GPR35 Orphan A (Rhodopsin) Human BRIL - - lodoxamide pubchem gtoplig chembl_ligand drug_central drugbank
Calcium pubchem
Small molecule
Small molecule 		Agonist
PAM 		kynurenic acid, 2-oleoyl-LPA Small molecule Duan J, Liu Q, Yuan Q, Ji Y, Zhu S, Tan Y, He X, Xu Y, Shi J, Cheng X, Jiang H, Eric Xu H, Jiang Y 10.1038/S41421-022-00499-8 2023-02-08
Gs αs Bovine mDNGs: Gs/Gi chimera, G226A/A366S mutations 60 β1 Rat γ2 Bovine Cryo-EM 8HAF - 3.3 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTHrP-(1-36) (Human) pubchem gtoplig uniprot
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21
Gs αs Bovine DNGαs (bovine): G226A/A366S, Δ254-263, Gi AHD 60 β1 Rat γ2 Bovine Cryo-EM 8HAO - 3.8 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - teriparatide pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21
Gq/11 αq Human mini-Gq: Gi2 N-term; Gβ1-HiBiT fusion 57 β1 Human γ2 Human Cryo-EM 8HCQ 8HCQ_refined 3.0 EDNRA EDNRA ETA Endothelin A (Rhodopsin) Human - - LgBiT
HiBiT 		endothelin-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Protein Agonist endothelin-2 (Mouse), endothelin-2 (Human), endothelin-1 (Human), endothelin-3 (Human) Protein - - 2023-03-22
Gq/11 αq Human MiniGαq: N-term(1-35) from Gαi2, for scFv16 61 β1 Human γ2 Human Cryo-EM 8HCX 8HCX_refined 3.5 EDNRB EDNRB ETB Endothelin A (Rhodopsin) Human - - LgBiT (Oplophorus-luciferin 2-monooxygenase)
HiBiT peptide 		endothelin-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Protein Agonist endothelin-2 (Mouse), endothelin-2 (Human), endothelin-1 (Human), endothelin-3 (Human) Protein - - 2023-03-22
Gs αs Human Modified miniGs (engineered gnas2_human fragment) 60 β1 Human γ2 Human Cryo-EM 8HDP - 3.2 AA2BR ADORA2B A2B Adenosine A (Rhodopsin) Human - Nanobody-35 - adenosine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist adenosine Small molecule Cai H, Xu Y, Guo S, He X, Sun J, Li X, Li C, Yin W, Cheng X, Jiang H, Xu HE, Xie X, Jiang Y 10.1038/S41421-022-00503-1 2023-01-18
Gq/11 αq Human mini-Gαs/q71: Gαi1 N-term(1-18) + AHD 60 β1 Human γ2 Human Cryo-EM 8HJ5 8HJ5_refined 3.0 MRGX1 MRGPRX1 MRGPRX1 Orphan A (Rhodopsin) Human BRIL Nanobody-35 LgBiT
HiBiT 		compound 16 [PMID: 31498617] pubchem gtoplig chembl_ligand
Small molecule Agonist bovine adrenal medulla peptide 8-22 (Human) Peptide - - 2023-05-31
Gs αs Bovine Engineered mini-Gs (Cricetulus griseus) 58 β1 Human γ2 Human Cryo-EM 8I2G - 2.8 FSHR FSHR FSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Follitropin (FSH) (chain X)
Follitropin (FSH) (chain Y)
Cpd-21f pubchem
Protein
Protein
Small molecule 		Agonist FSH (Human), FSH (Rat), FSH (Mouse) Peptide Duan J, Xu P, Zhang H, Luan X, Yang J, He X, Mao C, Shen DD, Ji Y, Cheng X, Jiang H, Jiang Y, Zhang S, Zhang Y, Xu HE 10.1038/S41467-023-36170-3 2023-03-29
Gq/11 αq Human Mini-Gq: Gs/Gq chimera, Gq α5 helix specificity 58 β1 Human γ2 Human Cryo-EM 8I9A - 3.6 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - - EP54
Peptide Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gq/11 αq Human mGαs/q/iN: Gαi1 N-term, Gq specificity res 60 β1 Human γ2 Human Cryo-EM 8IBV 8IBV_refined 3.2 MTLR MLNR motilin Motilin A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		motilin (Human) pubchem gtoplig chembl_ligand uniprot uniprot
Protein Agonist motilin (Human) Protein You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y 10.1126/SCIADV.ADE9020 2023-04-12
Gq/11 αq Human miniGs/q70iN: Gs+Gαi N-term+Gαq α5, fused to FP 54 β1 Human γ2 Human Cryo-EM 8IQ4 8IQ4_refined 2.7 PF2R PTGFR FP Prostanoid A (Rhodopsin) Human - Nanobody-35 - Carboprost tromethamine pubchem drugbank pubchem chembl_ligand pubchem chembl_ligand pubchem
Small molecule Agonist PGF2α, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Lv X, Gao K, Nie J, Zhang X, Zhang S, Ren Y, Sun X, Li Q, Huang J, Liu L, Zhang X, Zhang W, Liu X 10.1038/S41467-023-43922-8 2024-01-31
Gq/11 αq Human MiniGs/q70iN: Gi1 N-term + 7 α5 muts to Gq 54 β1 Human γ2 Human Cryo-EM 8IQ6 8IQ6_refined 3.4 PF2R PTGFR FP Prostanoid A (Rhodopsin) Human - Nanobody-35 - latanoprost (free acid form) pubchem gtoplig chembl_ligand
Small molecule Agonist PGF2α, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Lv X, Gao K, Nie J, Zhang X, Zhang S, Ren Y, Sun X, Li Q, Huang J, Liu L, Zhang X, Zhang W, Liu X 10.1038/S41467-023-43922-8 2024-01-31
Gi/o αi1 Human DNGs: Gαi1 αN/α5 helices + Gαs Ras domain 61 β1 Human γ2 Human Cryo-EM 8IRU - 3.2 DRD4 DRD4 D4 Dopamine A (Rhodopsin) Human BRIL - - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Agonist
PAM 		dopamine Small molecule Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-21
Gq/11 αq Human mGαs/q/iN: Gs scaffold, Gi1 N-term, Gq α5 60 β1 Human γ2 Human Cryo-EM 8IUK - 2.7 PF2R PTGFR FP Prostanoid A (Rhodopsin) Human BRIL Nanobody-35 - PGF2α pubchem gtoplig chembl_ligand drug_central pubchem drugbank drugbank
Small molecule Agonist PGF2α, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Wu C, Xu Y, He Q, Li D, Duan J, Li C, You C, Chen H, Fan W, Jiang Y, Eric Xu H 10.1038/S41467-023-38411-X 2023-07-12
Gq/11 αq Human mGαs/q/iN: Gαi1 N-term, Gαq α5(348-359) 60 β1 Human γ2 Human Cryo-EM 8IUL - 2.8 PF2R PTGFR FP Prostanoid A (Rhodopsin) Human BRIL - - latanoprost (free acid form) pubchem gtoplig chembl_ligand
Small molecule Agonist PGF2α, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Wu C, Xu Y, He Q, Li D, Duan J, Li C, You C, Chen H, Fan W, Jiang Y, Eric Xu H 10.1038/S41467-023-38411-X 2023-07-12
Gq/11 αq Human mGαs/q/iN: Gαi1 N-term, Gαq α5(348-359) 60 β1 Human γ2 Human Cryo-EM 8IUM - 3.1 PF2R PTGFR FP Prostanoid A (Rhodopsin) Human BRIL Nanobody-35 - tafluprost acid pubchem gtoplig
Small molecule Agonist PGF2α, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Wu C, Xu Y, He Q, Li D, Duan J, Li C, You C, Chen H, Fan W, Jiang Y, Eric Xu H 10.1038/S41467-023-38411-X 2023-07-12
Gs αs Human mini-Gs: N-term & linker from Gi1, scFv16 59 β1 Human γ2 Human Cryo-EM 8IW9 - 3.1 TAAR9 Taar9 TAAR9 Orphan A (Rhodopsin) Mouse BRIL Nanobody-35 - Cadaverine pubchem drugbank
Small molecule Agonist - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gi/o αi1 Human Gi1 heterotrimer (Gαi1, Gβ1, Gγ2) 63 β1 Human γ2 Human Cryo-EM 8IZ4 - 2.9 GPR34 GPR34 GPR34 Orphan A (Rhodopsin) Human - - - [(2R)-2-oxidanyl-3-phosphonooxy-propyl] octadecanoate pubchem
L-serine pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank pubchem drugbank
Lipid
Small molecule 		Agonist lysophosphatidylserine Lipid - - 2024-04-10
Gs αs Human Mini-Gs (DN_miniGαs): muts + AHD deletion 60 β1 Human γ2 Human Cryo-EM 8IZB - 3.1 GP174 GPR174 GPR174 Orphan A (Rhodopsin) Human - Nanobody-35 BN (Beta-2-AR fragment)
LgBiT 		L-serine pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank pubchem drugbank
LYSOPHOSPHATIDIC ACID chembl_ligand pubchem
Small molecule
Small molecule 		Agonist lysophosphatidylserine Lipid Liu G, Li X, Wang Y, Zhang X, Gong W 10.1371/JOURNAL.PBIO.3002387 2023-11-01
Gq/11 αq Human mini-Gs/q7/i1: DN G203A/A326S muts 59 β1 Rat γ2 Bovine Cryo-EM 8JBH 8JBH_refined 2.9 NK3R TACR3 NK3 Tachykinin A (Rhodopsin) Human BRIL - LgBiT substance P (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist substance P (Human), neurokinin B (Human), neurokinin A (Human) Peptide - - 2024-02-07
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 8JD3 - 3.3 GRM2 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - - - L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
Small molecule
Small molecule 		Agonist
PAM 		L-glutamic acid Small molecule Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B 10.1038/S41422-023-00830-2 2023-06-21
Gi/o αi1 Human DNGαi1 (labeled Gs): S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8JD5 - 3.6 GRM2 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - - - L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
ADX88178 pubchem gtoplig chembl_ligand
Small molecule
Small molecule
Small molecule 		Agonist
PAM
PAM 		L-glutamic acid Small molecule Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B 10.1038/S41422-023-00830-2 2023-06-21
Gq/11 αq Human mini-Gs/Gq71/i1: G203A/A326S muts 60 β1 Human γ2 Human Cryo-EM 8JGF 8JGF_refined 2.7 MRGX1 MRGPRX1 MRGPRX1 Orphan A (Rhodopsin) Human BRIL - - bovine adrenal medulla peptide 8-22 (Human) pubchem gtoplig chembl_ligand uniprot
Peptide Agonist bovine adrenal medulla peptide 8-22 (Human) Peptide Guo L, Zhang Y, Fang G, Tie L, Zhuang Y, Xue C, Liu Q, Zhang M, Zhu K, You C, Xu P, Yuan Q, Zhang C, Liu L, Rong N, Peng S, Liu Y, Wang C, Luo X, Lv Z, Kang D, Yu X, Zhang C, Jiang Y, Dong X, Zhou J, Liu Z, Yang F, Eric Xu H, Sun JP 10.1038/S41467-023-40705-Z 2024-01-10
Gs αs Human Mini-Gs/Gi1 chimera (dual UniProt IDs) 62 β1 Rat γ2 Bovine Cryo-EM 8JIP 8JIP_refined 2.9 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - N-hexadecanoyl-L-glutamic acid pubchem
COTADUTIDE chembl_ligand drugbank pubchem
Small molecule
Protein 		Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z 10.1073/PNAS.2303696120 2023-09-06
Gs αs Human mini-Gs: Gs/Gi1 chimera, Gs-family α5 tail 58 β1 Rat γ2 Bovine Cryo-EM 8JIR 8JIR_refined 2.6 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - N-hexadecanoyl-L-glutamic acid pubchem
SAR425899 pubchem
Small molecule
Peptide 		Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z 10.1073/PNAS.2303696120 2023-09-06
Gs αs Human modGαs: Gs/Gi1 chimera for stabilization 59 β1 Human γ2 Human Cryo-EM 8JLJ - 3.1 TAAR1 Taar1 TA1 Trace amine A (Rhodopsin) Mouse BRIL - - CHEMBL1182312 chembl_ligand pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine Small molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gs αs Human mini-Gs: human Gs/Gi1 chimera (modGαs) 59 β1 Human γ2 Human Cryo-EM 8JLK - 3.2 TAAR1 Taar1 TA1 Trace amine A (Rhodopsin) Mouse BRIL - - ulotaront pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine Small molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gs αs Human modGαs chimera: Gs + Gi1 segments, scFv16 61 β1 Human γ2 Human Cryo-EM 8JLN - 3.2 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL - - CHEMBL1182312 chembl_ligand pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gs αs Human modGαs chimera: human Gαs + Gαi1 58 β1 Human γ2 Human Cryo-EM 8JLQ - 2.8 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL - - fenoldopam pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand pubchem gtoplig pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gs αs Human Mini-Gs: Gs/Gi chimera (human GNAS/GNAI1) 59 β1 Human γ2 Human Cryo-EM 8JLR - 3.0 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL - - A77636
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gs αs Human modGαs chimera: Gs + Gi1 sequence 59 β1 Human γ2 Mouse Cryo-EM 8JSO 8JSO_refined 3.4 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL - - dexamfetamine pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gq/11 αq Human MiniGq: DN miniGs skeleton + Gαi1 N-term helix 62 β1 Human γ2 Human Cryo-EM 8JSR 8JSR_refined 2.9 GHSR GHSR ghrelin Ghrelin A (Rhodopsin) Human - Nanobody-35 NLuc fragment anamorelin pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist [des-Gln14]ghrelin (Mouse), liver enriched antimicrobial peptide 2 (Human), ghrelin (Mouse), [des-Gln14]ghrelin (Human), ghrelin (Human) Peptide Shiimura Y, Im D, Tany R, Asada H, Kise R, Kurumiya E, Wakasugi-Masuho H, Yasuda S, Matsui K, Kishikawa JI, Kato T, Murata T, Kojima M, Iwata S, Masuho I 10.1038/S41594-024-01481-6 2025-01-22
Gi/o αgust Human miniGgus: Gαi1 N15 + 7 stabilizing muts, scFv16 61 β1 Human γ2 Human Cryo-EM 8RQL - 3.0 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - - flufenamic acid pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist - - Peri L, Matzov D, Huxley DR, Rainish A, Fierro F, Sapir L, Pfeiffer T, Waterloo L, Hubner H, Peleg Y, Gmeiner P, McCormick PJ, Weikert D, Niv MY, Shalev-Benami M 10.1038/S41467-024-54157-6 2024-11-27
Gi/o αi1 Human DN Gαi1: G203A/A326S 66 β1 Human γ2 Human Cryo-EM 8K3Z - 2.8 CXCR4 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human - - - CXCL12
Small molecule Agonist CXCL12ε (Human), CXCL12 (Mouse), CXCL12δ (Human), CXCL12α (Human), CXCL12β (Human), CXCL12φ (Human), CXCL12γ (Human) Peptide - - 2024-07-17
Gq/11 αq Human mini-Gαq: Gs body, Gq α5 for MRGPRX4 57 β1 Human γ2 Human Cryo-EM 8K4S 8K4S_refined 2.9 MRGX4 MRGPRX4 MRGPRX4 Orphan A (Rhodopsin) Human BRIL - Green fluorescent protein (GFP) DCA-3P pubchem
Small molecule Agonist - - Yang J, Zhao T, Fan J, Zou H, Lan G, Guo F, Shi Y, Ke H, Yu H, Yue Z, Wang X, Bai Y, Li S, Liu Y, Wang X, Chen Y, Li Y, Lei X 10.1016/J.CELL.2024.10.001 2024-11-06
Gq/11 αq Human miniGs/q chimera: Gs with Gq α5 helix specificity 62 β1 Human γ2 Human Cryo-EM 8K8J - 2.9 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human BRIL Nanobody-35 LgBiT FENOFIBRATE chembl_ligand pubchem drugbank drug_central
Small molecule Agonist (partial) anandamide, 2-arachidonoylglycerol Small molecule Wang T, Tang W, Zhao Z, Zhao R, Lv Z, Guo X, Gu Q, Liu B, Lv H, Chen J, Zhang K, Li F, Wang J 10.1002/ADVS.202306311 2024-02-14
Gi/o αi3 Rhesus macaque WT macaque Gαi3, human Gβ1/Gγ2 63 β1 Human γ2 Human Cryo-EM 8K9K - 3.0 OPRM OPRM1 μ Opioid A (Rhodopsin) Human BRIL - - DAMGO pubchem gtoplig chembl_ligand pubchem
Peptide Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Kaneko S, Imai S, Uchikubo-Kamo T, Hisano T, Asao N, Shirouzu M, Shimada I 10.1038/S41467-024-47792-6 2024-05-29
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8PJK - 2.4 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - ST171 pubchem
Phosphatidylinositol-4-phosphate
Small molecule
Small molecule 		Agonist (partial)
PAM 		5-hydroxytryptamine Small molecule - - 2024-05-29
Gq/11 αq Human Gαq chimera: Gαi1 N-term swap, SmBiT fusion 61 β1 Human γ2 Human Cryo-EM 8SZG - 3.6 CASR CASR CaS Calcium-sensing C (Glutamate) Human - - LgBiT
HiBiT 		spermine pubchem gtoplig chembl_ligand drugbank
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule
Small molecule
Small molecule
Small molecule 		Ago-PAM
Agonist
Agonist
PAM 		D-tryptophan, Mg2+, spermine, Ca2+ Small molecule He F, Wu CG, Gao Y, Rahman SN, Zaoralova M, Papasergi-Scott MM, Gu TJ, Robertson MJ, Seven AB, Li L, Mathiesen JM, Skiniotis G 10.1038/S41586-024-07055-2 2024-02-07
Gi/o αi3 Human Wild-type human Gi3 heterotrimer 63 β1 Human γ2 Human Cryo-EM 8SZH - 3.1 CASR CASR CaS Calcium-sensing C (Glutamate) Human - - - spermine pubchem gtoplig chembl_ligand drugbank
Calcium pubchem
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule
Small molecule
Small molecule
Small molecule 		Ago-PAM
Agonist
Agonist
PAM 		D-tryptophan, Mg2+, spermine, Ca2+ Small molecule He F, Wu CG, Gao Y, Rahman SN, Zaoralova M, Papasergi-Scott MM, Gu TJ, Robertson MJ, Seven AB, Li L, Mathiesen JM, Skiniotis G 10.1038/S41586-024-07055-2 2024-02-07
Gi/o αi3 Human DN Gαi3 63 β1 Human γ2 Human Cryo-EM 8SZI - 3.5 CASR CASR CaS Calcium-sensing C (Glutamate) Human - - - Calcium pubchem
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule
Small molecule
Small molecule 		Agonist D-tryptophan, Mg2+, spermine, Ca2+ Small molecule He F, Wu CG, Gao Y, Rahman SN, Zaoralova M, Papasergi-Scott MM, Gu TJ, Robertson MJ, Seven AB, Li L, Mathiesen JM, Skiniotis G 10.1038/S41586-024-07055-2 2024-02-07
Gq/11 αq Human MiniGq: N-term(1-35) replaced by Gαi 59 β1 Human γ2 Human Cryo-EM 8T3O - 3.1 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - TUG-891 pubchem gtoplig chembl_ligand
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Zhang X, Guseinov AA, Jenkins L, Li K, Tikhonova IG, Milligan G, Zhang C 10.1126/SCIADV.ADJ2384 2024-01-17
Gq/11 αq Human MiniGq: N-term(1-35) from Gαi1 59 β1 Human γ2 Human Cryo-EM 8T3Q 8T3Q_refined 3.1 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Zhang X, Guseinov AA, Jenkins L, Li K, Tikhonova IG, Milligan G, Zhang C 10.1126/SCIADV.ADJ2384 2024-01-24
Gq/11 αq Human MiniGq: N-term Gαi, rest Gαq 59 β1 Human γ2 Human Cryo-EM 8T3S - 3.1 FFAR2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - - - butyric acid pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem chembl_ligand pubchem
Small molecule Agonist butyric acid, propanoic acid, trans-2-methylcrotonic acid, acetic acid Small molecule Zhang X, Guseinov AA, Jenkins L, Li K, Tikhonova IG, Milligan G, Zhang C 10.1126/SCIADV.ADJ2384 2024-01-24
Gq/11 αq Human MiniGq: N-term(1-35) Gαi1, rest Gαq 59 β1 Human γ2 Human Cryo-EM 8T3V - 3.4 FFAR1 FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human - - - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Small molecule Agonist oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid Small molecule Zhang X, Guseinov AA, Jenkins L, Li K, Tikhonova IG, Milligan G, Zhang C 10.1126/SCIADV.ADJ2384 2024-01-24
Gs αs Human Gs/Gi1 DN chimera (G226A/A366S), receptor-fused 56 β1 Human γ2 Human Cryo-EM 8TB0 8TB0_refined 3.5 GPR61 GPR61 GPR61 Orphan A (Rhodopsin) Human - - - - None - - - - - 2023-10-04
Gq/11 αq Human Mini-GαqiN: Gαi2/Gαq/Gαs chimera 55 β1 Human γ2 Human Cryo-EM 8THK - 2.6 ADA1A ADRA1A α1A Adrenoceptors A (Rhodopsin) Human T4-Lysozyme - - CHEMBL133451 chembl_ligand pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY 10.1038/S41467-023-40524-2 2023-08-16
Gq/11 αq Human Mini-GαqiN chimera: Gαq/Gαi/Gαs segments 55 β1 Human γ2 Human Cryo-EM 8THL - 3.1 ADA1A ADRA1A α1A Adrenoceptors A (Rhodopsin) Human T4-Lysozyme - - (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Su M, Wang J, Xiang G, Do HN, Levitz J, Miao Y, Huang XY 10.1038/S41467-023-40524-2 2023-08-16
Gs αs Rat DN Gs: G226A/A366S + 5 more muts; α-γ fusion 60 β1 Human γ2 Human Cryo-EM 8UHB 8UHB_refined 3.4 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 Beta-2 adrenergic receptor (N-terminal fragment) CHEMBL3684869 chembl_ligand pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Zilberg G, Parpounas AK, Warren AL, Yang S, Wacker D 10.1038/S41467-023-44601-4 2024-01-10
Gi/o αi1 Human DN Gαi1: G203A/A326S, reduces nucl. binding 61 β1 Rat γ2 Bovine Cryo-EM 7T6T 7T6T_refined 3.2 FPR1 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - - - fMLFII
Peptide Agonist spinorphin (Human), cathepsin G (Rat), fMet-Leu-Phe-Ile-Ile, annexin I-(2-26) (Human), mitochondrial peptde fMMYALF, mitochondrial peptide fMFADRW, fMet-Leu-Phe, annexin I (Rat), annexin I (Mouse), cathepsin G (Mouse), cathepsin G (Human), annexin I (Human) Peptide Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C 10.1038/S41467-022-28586-0 2022-03-30
Gi/o αi1 Human DN human Gαi1: G203A/A326S, low GDP affinity 62 β1 Rat γ2 Bovine Cryo-EM 7T6U - 2.9 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - - - CGEN-855A
Peptide Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C 10.1038/S41467-022-28586-0 2022-03-30
Gs αs Human MiniGs399: thermostable, only α5 fragment modeled 56 β1 Human γ2 Human Cryo-EM 7T9I - 2.9 TSHR TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Thyrotropin subunit beta (TSH subunit beta)
Glycoprotein hormones alpha chain (TSH subunit alpha)
Protein
Protein 		Agonist TSH (Rat), TSH (Human), TSH (Mouse) Peptide Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03
Gi/o αi1 Mouse DN Gαi1: G203A 62 β1 Bovine γ2 Bovine Cryo-EM 7TD0 - 2.8 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - LPA pubchem
Lipid Agonist LPA Small molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi1 Mouse DN mouse Gαi1: G203A; Gγ2 C68S mutation 62 β1 Bovine γ2 Bovine Cryo-EM 7TD1 - 3.1 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - LPA pubchem
Lipid Agonist LPA Small molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi1 Mouse DN Gαi1: G203A 62 β1 Bovine γ2 Bovine Cryo-EM 7TD2 - 3.1 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - LPA pubchem
Lipid Agonist LPA Small molecule Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi1 Mouse DN Gαi1: G203A 63 β1 Bovine γ2 Bovine Cryo-EM 7TD3 - 3.0 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - - sphingosine 1-phosphate pubchem gtoplig chembl_ligand
Lipid Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gi/o αi1 Mouse Mouse Gαi1 DN mutant: G203A 63 β1 Bovine γ2 Bovine Cryo-EM 7TD4 - 2.6 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - - siponimod pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Liu S, Paknejad N, Zhu L, Kihara Y, Ray M, Chun J, Liu W, Hite RK, Huang XY 10.1038/S41467-022-28417-2 2022-02-09
Gq/11 α11 Human Gα11/Gαi1 chimera: N-term swap, DN muts 62 β1 Rat γ Rat Cryo-EM 7TRY - 3.7 CRHR2 CRHR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - - - CHEMBL427807 chembl_ligand pubchem
Protein Agonist urocortin 2 (Rat), urocortin 3 (Human), corticotrophin-releasing hormone (Human), urocortin 2 (Human), urocortin 1 (Human), urocortin 1 (Mouse) Peptide Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE 10.1038/S41467-022-33851-3 2022-11-09
Gi/o αo Human DNGαo: Gαs template, N-term/AHD from Gαi1 63 β1 Rat γ2 Mouse Cryo-EM 7TS0 7TS0_refined 2.8 CRHR2 CRHR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - - - CHEMBL427807 chembl_ligand pubchem
Protein Agonist urocortin 2 (Rat), urocortin 3 (Human), corticotrophin-releasing hormone (Human), urocortin 2 (Human), urocortin 1 (Human), urocortin 1 (Mouse) Peptide Zhao LH, Lin J, Ji SY, Zhou XE, Mao C, Shen DD, He X, Xiao P, Sun J, Melcher K, Zhang Y, Yu X, Xu HE 10.1038/S41467-022-33851-3 2022-11-09
Gs αs Human DNGs: 8 muts incl S54N/G226A/E268A/I285T 53 β1 Rat γ2 Bovine Cryo-EM 7V35 7V35_refined 3.4 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 20
Peptide Agonist glucagon (Human) Protein Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
Gq/11 αq Human Gαq/i chimera: N-term swap, DN R183Q/Q209L 98 β1 Human γ2 Human Cryo-EM 7W3Z - 3.0 GRPR GRPR BB2 Bombesin A (Rhodopsin) Human - - Maltodextrin-binding protein
LgBiT
HiBiT 		Gastrin Releasing Peptide (GRP)
Peptide Agonist neuromedin B (Human), GRP-(18-27) (Mouse), neuromedin C (Human), gastrin releasing peptide(14-27) (human) (Human), gastrin-releasing peptide (Human), GRP-(18-27) (Human) Protein Peng S, Zhan Y, Zhang D, Ren L, Chen A, Chen ZF, Zhang H 10.1073/PNAS.2216230120 2023-02-22
Gq/11 αq Human Gαq/Gαi chimera: N-term swap, R183Q/Q209L 79 β1 Human γ2 Human Cryo-EM 7W40 7W40_refined 3.0 GRPR GRPR BB2 Bombesin A (Rhodopsin) Human - - Maltose-binding protein (MBP)
LgBiT (NanoBiT) 		Bombesin (6-14) [D-Phe6, beta-Ala11, Phe13, Nle14] Bn (6-14)
Peptide Agonist neuromedin B (Human), GRP-(18-27) (Mouse), neuromedin C (Human), gastrin releasing peptide(14-27) (human) (Human), gastrin-releasing peptide (Human), GRP-(18-27) (Human) Protein - - 2023-02-22
Gq/11 αq Human mGαs/q/iN: Gαi1 N-term (scFv16), Gαq α5 54 β1 Human γ2 Human Cryo-EM 7W53 - 3.2 NMUR1 NMUR1 NMU1 Neuromedin U A (Rhodopsin) Human BRIL - LgBiT CHEMBL3315349 chembl_ligand pubchem
Protein Agonist neuromedin U-25 (Human), neuromedin S-36 (Mouse), neuromedin S-36 (Rat), neuromedin U-23 (Mouse), neuromedin S-33 (Human), neuromedin U-23 (Rat) Peptide You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y 10.1038/S41467-022-29683-W 2022-04-20
Gq/11 αq Human mGαs/q/iN: Gαi1 N-term, Gαq specificity 60 β1 Human γ2 Human Cryo-EM 7W55 - 2.8 NMUR2 NMUR2 NMU2 Neuromedin U A (Rhodopsin) Human BRIL - - CHEMBL3315349 chembl_ligand pubchem
Protein Agonist neuromedin U-25 (Human), neuromedin S-36 (Mouse), neuromedin S-36 (Rat), neuromedin S-33 (Human), neuromedin U-23 (Rat) Peptide You C, Zhang Y, Xu P, Huang S, Yin W, Eric Xu H, Jiang Y 10.1038/S41467-022-29683-W 2022-04-20
G12/13 α13 Human Mini-Gα13: Gαi2 N-term for scFv16; Gγ2 fusion 58 β1 Human γ2 Human Cryo-EM 9GE2 - 2.5 GPR55 GPR55 GPR55 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - - Folding Reporter GFP CID2440433 pubchem gtoplig chembl_ligand
Small molecule Agonist N-palmitoylethanolamine, lysophosphatidylinositol, anandamide, 2-arachidonoylglycerolphosphoinositol, 2-arachidonoylglycerol Small molecule - - 2025-03-05
Gi/o αi2 Human Gαi2 heterotrimer (paper says Gαi1) 63 β1 Human γ2 Human Cryo-EM 7WV9 - 3.4 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - CP55940 pubchem gtoplig chembl_ligand
ZCZ011 pubchem
Small molecule
Small molecule 		Agonist
PAM 		anandamide, 2-arachidonoylglycerol Small molecule Yang X, Wang X, Xu Z, Wu C, Zhou Y, Wang Y, Lin G, Li K, Wu M, Xia A, Liu J, Cheng L, Zou J, Yan W, Shao Z, Yang S 10.1038/S41589-022-01038-Y 2022-06-15
Gi/o αi2 Human DN Gαi2: S47N/G204A/A327S/E246A 63 β1 Human γ2 Human Cryo-EM 7WVY 7WVY_refined 3.0 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - Aβ42 pubchem
Peptide Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B 10.1038/S41467-022-29361-X 2022-04-13
Gq/11 αq Human Mini-Gαq protein 57 β1 Bovine γ2 Bovine Cryo-EM 7X1U 7X1U_refined 3.2 TRFR TRHR TRH1 Thyrotropin-releasing hormone A (Rhodopsin) Human - - - TRH (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem pubchem
Peptide Agonist TRH (Human) Peptide Yang F, Zhang H, Meng X, Li Y, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41422-022-00646-6 2022-08-31
Gi/o αi1 Human DN human Gαi1: S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 7XBW 7XBW_refined 2.8 CX3C1 CX3CR1 CX3CR1 Chemokine A (Rhodopsin) Human - - - Cholesterol pubchem drugbank
Small molecule PAM CX3CL1 (Mouse), CX3CL1 (Rat), CX3CL1 (Human) Peptide Lu M, Zhao W, Han S, Lin X, Xu T, Tan Q, Wang M, Yi C, Chu X, Yang W, Zhu Y, Wu B, Zhao Q 10.1126/SCIADV.ABN8048 2022-07-13
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 7XBX - 3.4 CX3C1 CX3CR1 CX3CR1 Chemokine A (Rhodopsin) Human - - - Cholesterol pubchem drugbank
Small molecule PAM CX3CL1 (Mouse), CX3CL1 (Rat), CX3CL1 (Human) Peptide - - 2022-07-13
Gq/11 αq Human Thermostable miniGq: αN from Gαi, for scFv16 58 β1 Human γ2 Human Cryo-EM 7XJK 7XJK_refined 3.3 GALR2 GALR2 GAL2 Galanin A (Rhodopsin) Human - - - galanin(1-13)amide gtoplig pubchem
Peptide Agonist galanin-like peptide (Human), galanin (Human), galanin-like peptide (Rat), galanin-like peptide (Mouse), spexin-1 (Human) Protein Jiang W, Zheng S 10.1073/PNAS.2121465119 2022-06-29
Gq/11 αq Human Mini-Gq: αN helix from Gαi, for scFv16 binding 58 β1 Human γ2 Human Cryo-EM 7XJL 7XJL_refined 3.5 GALR2 GALR2 GAL2 Galanin A (Rhodopsin) Human - - - Spexin pubchem
Small molecule Agonist galanin-like peptide (Human), galanin (Human), galanin-like peptide (Rat), galanin-like peptide (Mouse), spexin-1 (Human) Protein Jiang W, Zheng S 10.1073/PNAS.2121465119 2022-06-29
Gq/11 αq Human Gαq chimera: αN helix from Gi for scFv16 61 β1 Human γ2 Human Cryo-EM 7XOW 7XOW_refined 3.1 GASR CCKBR CCK2 Cholecystokinin A (Rhodopsin) Human - - - desulfated gastrin-17 (Human) pubchem gtoplig uniprot chembl_ligand pubchem
Peptide Agonist gastrin-17 (Human), gastrin-34 (Human), CCK-33 (Mouse), gastrin-71 (Human), CCK-4 (Human), CCK-8 (Human), desulfated gastrin-17 (Human), CCK-33 (Human), desulfated gastrin-34 (Human), desulfated gastrin-71 (Human), desulfated gastrin-14 (Human), gastrin-17 (Rat), gastrin-14 (Human), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM 10.1038/S41421-022-00420-3 2022-07-20
Gq/11 αq Human Mini-Gq: N-term replaced by Gαi1, for scFv16 60 β1 Human γ2 Human Cryo-EM 7Y26 7Y26_refined 3.3 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - - octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Chen S, Teng X, Zheng S 10.1038/S41589-022-01130-3 2022-10-19
Gq/11 αq Human Mini-Gq: N-term replaced by Gαi1, for scFv16 60 β1 Human γ2 Human Cryo-EM 7Y27 7Y27_refined 3.5 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - - SOMATOSTATIN chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Chen S, Teng X, Zheng S 10.1038/S41589-022-01130-3 2022-10-19
Gq/11 αq Human miniGsq: miniGs scaffold, Gq α5 helix 46 - - - - Cryo-EM 7YM8 7YM8_refined 2.9 ADA1A ADRA1A α1A Adrenoceptors A (Rhodopsin) Human mT4-Lysozyme - - oxymetazoline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Nanobody 29 (Nb29)
Small molecule
Protein 		Agonist (partial)
PAM 		(-)-noradrenaline, (-)-adrenaline Small molecule Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X 10.1038/S41467-023-39310-X 2023-07-05
Gq/11 αq Human MiniGsq: Gs core, C-term 15 res(α5) from Gq 51 - - - - Cryo-EM 7YMH 7YMH_refined 3.5 ADA1A ADRA1A α1A Adrenoceptors A (Rhodopsin) Human minimal T4-Lysozyme (mT4L) - - (-)-noradrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
Nb29
Small molecule
Protein 		Agonist
PAM 		(-)-noradrenaline, (-)-adrenaline Small molecule Toyoda Y, Zhu A, Kong F, Shan S, Zhao J, Wang N, Sun X, Zhang L, Yan C, Kobilka BK, Liu X 10.1038/S41467-023-39310-X 2023-07-05
Gq/11 αq Human mini-GαqiN: Gs backbone mimics Gq specificity 57 β1 Human γ2 Human Cryo-EM 8DWC - 2.9 MRGX1 MRGPRX1 MRGPRX1 Orphan A (Rhodopsin) Human - - - bovine adrenal medulla peptide 8-22 (Human) pubchem gtoplig chembl_ligand uniprot
Peptide Agonist bovine adrenal medulla peptide 8-22 (Human) Peptide - - 2022-11-02
Gq/11 αq Human Mini-Gq (mini-GqiN): Gs/Gq chimera heterotrimer 57 β1 Human γ2 Human Cryo-EM 8DWG - 2.7 MRGX1 MRGPRX1 MRGPRX1 Orphan A (Rhodopsin) Human - - - bovine adrenal medulla peptide 8-22 (Human) pubchem gtoplig chembl_ligand uniprot
CHEMBL5177388 chembl_ligand pubchem
Peptide
Small molecule 		Agonist
PAM 		bovine adrenal medulla peptide 8-22 (Human) Peptide Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL 10.1038/S41589-022-01173-6 2022-11-02
Gq/11 αq Human mini-Gs/Gq chimera: Gq α5 tail for coupling 57 β1 Human γ2 Human Cryo-EM 8DWH 8DWH_refined 3.3 MRGX1 MRGPRX1 MRGPRX1 Orphan A (Rhodopsin) Human - - - compound 16 [PMID: 31498617] pubchem gtoplig chembl_ligand
Small molecule Agonist bovine adrenal medulla peptide 8-22 (Human) Peptide Liu Y, Cao C, Huang XP, Gumpper RH, Rachman MM, Shih SL, Krumm BE, Zhang S, Shoichet BK, Fay JF, Roth BL 10.1038/S41589-022-01173-6 2022-11-02
Gi/o αgust Human Gustducin/Gi2 chimera, DN muts (7 total) 58 β1 Human γ2 Human Cryo-EM 8DZR - 2.6 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - CHEMBL277863 chembl_ligand pubchem
Small molecule Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03
Gq/11 αq Human mGsqiN: Gs backbone w/ Gq+Gi residues 60 β1 Human γ2 Human Cryo-EM 8EJC - 3.0 FFAR1 FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human T4-Lysozyme - - fasiglifam pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist (partial) oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid Small molecule Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM 10.1073/PNAS.2219569120 2023-05-24
Gq/11 αq Human mGsqiN: mini-G chimera mimicking Gq coupling 60 β1 Human γ2 Human Cryo-EM 8EJK - 3.4 FFAR1 FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human T4-Lysozyme - - fasiglifam pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist (partial) oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid Small molecule Kumari P, Inoue A, Chapman K, Lian P, Rosenbaum DM 10.1073/PNAS.2219569120 2023-05-24
Gs αs Human DNGs: short isoform (Gnas2) 58 β1 Human γ2 Human Cryo-EM 8F0J - 2.0 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - San45
N-hexadecanoyl-L-glutamic acid pubchem
Peptide
Small molecule 		Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02
Gq/11 αq Human Gαiq chimera: Gαi1 body, Gαq C-term α5 61 β1 Human γ2 Human Cryo-EM 8G59 8G59_refined 2.6 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - TUG-891 pubchem gtoplig chembl_ligand
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-08
Gs αs Human miniGs: Gs/Gi chimera, 8+2 DN mutations 59 β1 Human γ2 Human Cryo-EM 8GY7 - 3.3 ACTHR MC2R MC2 Melanocortin A (Rhodopsin) Human BRIL - MRAP1 ACTH (Corticotropin)
Calcium pubchem
Peptide
Small molecule 		Agonist
Cofactor 		ACTH (Human), ACTH (Mouse) Peptide Luo P, Feng W, Ma S, Dai A, Wu K, Chen X, Yuan Q, Cai X, Yang D, Wang MW, Eric Xu H, Jiang Y 10.1038/S41422-022-00751-6 2023-01-11
Gq/11 αq Human Gs/Gi1 chimera; engineered Gq-mimetic 57 β1 Human γ2 Human Cryo-EM 8H0P - 3.2 NMBR NMBR BB1 Bombesin A (Rhodopsin) Human - - - NMB30
Peptide Agonist neuromedin B (Human), gastrin-releasing peptide (Mouse), GRP-(18-27) (Mouse), gastrin-releasing peptide (Pig), gastrin-releasing peptide (Human), gastrin releasing peptide(14-27) (human) (Human), GRP-(18-27) (Human) Protein Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W 10.1038/S41422-022-00743-6 2023-08-09
Gq/11 αq Human Gs/Gi chimera w/ Gq C-term, for scFv16 56 β1 Human γ2 Human Cryo-EM 8H0Q - 3.3 GRPR GRPR BB2 Bombesin A (Rhodopsin) Human - - - GRP(14-27) pubchem
Peptide Agonist neuromedin B (Human), GRP-(18-27) (Mouse), neuromedin C (Human), gastrin releasing peptide(14-27) (human) (Human), gastrin-releasing peptide (Human), GRP-(18-27) (Human) Protein Li C, Xu Y, Liu H, Cai H, Jiang Y, Xu HE, Yin W 10.1038/S41422-022-00743-6 2023-08-09
Gq/11 αq Human MiniGsq: Gq α5(αH5) in miniGs body 60 β1 Human γ2 Human Cryo-EM 8H4K - 3.1 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - Nanobody-35 - GW9508 pubchem gtoplig chembl_ligand
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21
Gq/11 αq Human MiniGsq: Gs body with Gq α5 helix 60 β1 Human γ2 Human Cryo-EM 8H4L - 3.1 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - Nanobody-35 - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21
Gs αs Human Gα short isoform, C3S mutation 40 β1 Human γ2 Human Cryo-EM 8HTI - 3.0 O52E4 OR52E4 OR52E4 Olfactory family 52 O1 (Olfactory/extra-nasal 1) Human - Nanobody-35 - OCTANOIC ACID chembl_ligand pubchem pubchem drugbank drug_central
Small molecule Agonist - - Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ 10.1038/S41467-023-43983-9 2023-12-20
Gq/11 αq Human Gαq chimera: αN helix→Gαi, scFv16 61 β1 Human γ2 Human Cryo-EM 8IA7 8IA7_refined 3.1 GASR CCKBR CCK2 Cholecystokinin A (Rhodopsin) Human - - - CCK-8 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Peptide Agonist gastrin-17 (Human), gastrin-34 (Human), CCK-33 (Mouse), gastrin-71 (Human), CCK-4 (Human), CCK-8 (Human), desulfated gastrin-17 (Human), CCK-33 (Human), desulfated gastrin-34 (Human), desulfated gastrin-71 (Human), desulfated gastrin-14 (Human), gastrin-17 (Rat), gastrin-14 (Human), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM 10.1038/S41421-022-00420-3 2023-12-06
Gq/11 αq Human mGαs/q/iN: Gαi1 N-term, Gαq α5 helix 60 β1 Human γ2 Human Cryo-EM 8IBU 8IBU_refined 3.5 MTLR MLNR motilin Motilin A (Rhodopsin) Human BRIL - - erythromycin pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist motilin (Human) Protein You C, Zhang Y, Xu Y, Xu P, Li Z, Li H, Huang S, Chen Z, Li J, Xu HE, Jiang Y 10.1126/SCIADV.ADE9020 2023-04-12
Gs αs Bovine DN Gs: 8 muts S54N/G226A/E268A...I285T 59 β1 Rat γ2 Bovine Cryo-EM 8ITL - 3.2 GIPR GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - - None - gastric inhibitory polypeptide (Mouse), gastric inhibitory polypeptide (Human) Peptide Zhao F, Hang K, Zhou Q, Shao L, Li H, Li W, Lin S, Dai A, Cai X, Liu Y, Xu Y, Feng W, Yang D, Wang MW 10.1073/PNAS.2306145120 2023-10-18
Gs αs Bovine DN bovine Gαs (8 muts); Gβ1 C-term SmBiT 59 β1 Rat γ2 Bovine Cryo-EM 8ITM - 3.1 GIPR GIPR GIP Glucagon B1 (Secretin) Human BRIL Nanobody-35 - - None - gastric inhibitory polypeptide (Mouse), gastric inhibitory polypeptide (Human) Peptide Zhao F, Hang K, Zhou Q, Shao L, Li H, Li W, Lin S, Dai A, Cai X, Liu Y, Xu Y, Feng W, Yang D, Wang MW 10.1073/PNAS.2306145120 2023-10-18
Gs αolf Human Mini-Golf: Gαi1 N-term + Gαolf body/α5 helix 59 β1 Human γ2 Human Cryo-EM 8IW1 - 3.4 TAAR9 Taar9 TAAR9 Orphan A (Rhodopsin) Mouse BRIL - - - - - - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gq/11 αq Human Mini-Gq: Gs scaffold + Gq α5 helix chimera 60 β1 Human γ2 Human Cryo-EM 8J9N - 3.5 FZD1 FZD1 FZD1 WNT F (Frizzled) Human - Nanobody-35 - - None - Wnt-1 (Human), Wnt-3a (Human), Wnt-5a (Human), Wnt-7b (Human), Wnt-2 (Human) Peptide Zhang Z, Lin X, Wei L, Wu Y, Xu L, Wu L, Wei X, Zhao S, Zhu X, Xu F 10.1038/S41421-023-00627-Y 2024-01-17
Gq/11 αq Human Gα chimera: Gs/q71+Gαi1 N-term/AHD, DN muts 59 β1 Rat γ2 Bovine Cryo-EM 8JBF - 3.0 NK3R TACR3 NK3 Tachykinin A (Rhodopsin) Human BRIL - - senktide pubchem gtoplig chembl_ligand chembl_ligand pubchem pubchem
Peptide Agonist substance P (Human), neurokinin B (Human), neurokinin A (Human) Peptide Sun W, Yang F, Zhang H, Yuan Q, Ling S, Wang Y, Lv P, Li Z, Luo Y, Liu D, Yin W, Shi P, Xu HE, Tian C 10.1038/S41421-023-00564-W 2024-02-28
Gq/11 αq Human mini-Gαs/q71: Gαi1 N-term, Gαq C-term 59 β1 Rat γ2 Bovine Cryo-EM 8JBG 8JBG_refined 2.8 NK3R TACR3 NK3 Tachykinin A (Rhodopsin) Human BRIL - LgBiT neurokinin B (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot uniprot
Peptide Agonist substance P (Human), neurokinin B (Human), neurokinin A (Human) Peptide - - 2024-02-07
Gs αs Human Mini-Gs (XLas isoform) 60 β1 Human γ2 Human Cryo-EM 8JHB - 3.3 FZD6 FZD6 FZD6 WNT F (Frizzled) Human BRIL Nanobody-35 - - None - Wnt-3a (Human), Wnt-5a (Human), Wnt-4 (Human) Peptide Zhang Z, Lin X, Wei L, Wu Y, Xu L, Wu L, Wei X, Zhao S, Zhu X, Xu F 10.1038/S41421-023-00627-Y 2024-01-17
Gs αs Human Mini-Gs protein 60 β1 Human γ2 Human Cryo-EM 8JHI - 3.2 FZD3 FZD3 FZD3 WNT F (Frizzled) Human - Nanobody-35 - - None - - - - - 2024-01-17
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Rat γ2 Bovine Cryo-EM 8JIT - 2.9 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - N-hexadecanoyl-L-glutamic acid pubchem
COTADUTIDE chembl_ligand drugbank pubchem
Small molecule
Protein 		Agonist glucagon (Human) Protein Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z 10.1073/PNAS.2303696120 2023-09-06
Gq/11 αq Human Gαq/i1 chimera: N-term swap for expression 88 - - - - Cryo-EM 8JPB - 3.1 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human BRIL GRK2 LgBiT
HiBiT
GRK2 		SBI-553 pubchem gtoplig chembl_ligand
NTS8–13 pubchem
Small molecule
Peptide 		Ago-PAM
Agonist 		large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE 10.1038/S41586-023-06395-9 2023-08-09
Gq/11 αq Human Gαq chimera: N-term→Gαi1, GDP-AlF4 stabilized 88 - - - - Cryo-EM 8JPC - 3.1 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human BRIL GRK2 LgBiT
HiBiT
GRK2 		SBI-553 pubchem gtoplig chembl_ligand
NTS8–13 pubchem
Small molecule
Peptide 		Ago-PAM
Agonist 		large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE 10.1038/S41586-023-06395-9 2023-08-09
Gq/11 αq Human MiniGs/q: Gs scaffold, α5 from Gq 61 β1 Human γ2 Human Cryo-EM 8JPP - 3.2 SUCR1 SUCNR1 succinate Succinate A (Rhodopsin) Human BRIL - Oplophorus-luciferin 2-monooxygenase catalytic subunit succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank
Small molecule Agonist succinic acid Small molecule Wang T, Tang W, Zhu X, Lv Z, Chen J, Li Y, Sun X, Lv H, Gu Q, Li F, Wang J 10.1038/S41422-024-00968-7 2024-05-22
Gs αs Bovine DNGs: 9 muts+A366S; Gβ C-term SmBiT 59 β1 Rat γ2 Bovine Cryo-EM 8WA3 8WA3_refined 2.9 GIPR GIPR GIP Glucagon B1 (Secretin) Human BRIL Nanobody-35 - - None - gastric inhibitory polypeptide (Mouse), gastric inhibitory polypeptide (Human) Peptide Cong Z, Zhao F, Li Y, Luo G, Mai Y, Chen X, Chen Y, Lin S, Cai X, Zhou Q, Yang D, Wang MW 10.1038/S41421-024-00649-0 2024-03-06
Gq/11 αq Human modGaq: mini-Gs, Gαi1 N-term, Gαq α5 58 β1 Human γ2 Human Cryo-EM 8WC9 - 3.2 TAAR1 Taar1 TA1 Trace amine A (Rhodopsin) Mouse - - - CHEMBL476516 chembl_ligand pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine Small molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human Gs: DN mutations G226A/A366S 58 β1 Human γ2 Human Cryo-EM 8WW2 - 2.8 GPR3 GPR3 GPR3 Orphan A (Rhodopsin) Human - Nanobody-35 - oleic acid pubchem gtoplig chembl_ligand drug_central pubchem drugbank
Small molecule Agonist sphingosine 1-phosphate Lipid Xiong Y, Xu Z, Li X, Wang Y, Zhao J, Wang N, Duan Y, Xia R, Han Z, Qian Y, Liang J, Zhang A, Guo C, Inoue A, Xia Y, Chen Z, He Y 10.1038/S41422-024-00932-5 2024-02-14
Gs αs Bovine Gs protein with thermostabilizing mutations 58 β1 Rat γ2 Bovine Cryo-EM 8X9S - 3.5 AGRD1 ADGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - - - dihydrotestosterone pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist dihydrotestosterone Small molecule Yang Z, Ping YQ, Wang MW, Zhang C, Zhou SH, Xi YT, Zhu KK, Ding W, Zhang QY, Song ZC, Zhao RJ, He ZL, Wang MX, Qi L, Ullmann C, Ricken A, Schoneberg T, Gan ZJ, Yu X, Xiao P, Yi F, Liebscher I, Sun JP 10.1016/J.CELL.2025.01.006 2025-02-12
Gi/o αi1 Bovine DN bovine Gαi: G203A/A326S; Gβ-HiBiT fusion 61 β1 Rat γ2 Bovine Cryo-EM 8X17 8X17_refined 3.2 AA3R ADORA3 A3 Adenosine A (Rhodopsin) Human BRIL - LgBiT Cl-IB-MECA pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist adenosine Small molecule Cai H, Guo S, Xu Y, Sun J, Li J, Xia Z, Jiang Y, Xie X, Xu HE 10.1038/S41467-024-47207-6 2024-04-24
Gi/o αi1 Human mini-Gs/i143: Gi1 N-term(1-18) + GαAH domain 62 β1 Human γ2 Human Cryo-EM 8X8L 8X8L_refined 2.7 SSR5 SSTR5 SST5 Somatostatin A (Rhodopsin) Human - - - Cortistatin
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide - - 2024-06-12
Gi/o αt1 Bovine eGt: bovine Gt αN → human Gi1, fused to Gγ, Nb35 59 β1 Rat γ2 Bovine Cryo-EM 8XGR - 3.2 EDNRB EDNRB ETB Endothelin A (Rhodopsin) Human - Nanobody-35 - endothelin-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Protein Agonist endothelin-2 (Mouse), endothelin-2 (Human), endothelin-1 (Human), endothelin-3 (Human) Protein - - 2024-04-03
Gq/11 αq Human Gαq chimera: N-term(18)→Gi1 for scFv16 64 β1 Human γ2 Human Cryo-EM 8XGS - 3.0 KISSR KISS1R kisspeptin Kisspeptin A (Rhodopsin) Human - - - Metastin (KP54) pubchem
Peptide Agonist kisspeptin-10 (Mouse), kisspeptin-52 (Mouse), kisspeptin-13 (Human), kisspeptin-14 (Human), kisspeptin-54 (Human), kisspeptin-10 (Human), kisspeptin-52 (Rat) Peptide Wu Z, Chen G, Qiu C, Yan X, Xu L, Jiang S, Xu J, Han R, Shi T, Liu Y, Gao W, Wang Q, Li J, Ye F, Pan X, Zhang Z, Ning P, Zhang B, Chen J, Du Y 10.1126/SCIADV.ADN7771 2024-10-30
Gi/o αi1 Human mini-Gs/i43: αN & α5 helices from Gαi1 62 β1 Human γ2 Human Cryo-EM 8XIO - 2.7 SSR1 SSTR1 SST1 Somatostatin A (Rhodopsin) Human - Nanobody-35 - L-797591 pubchem
Small molecule Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide - - 2024-07-03
Gi/o αi1 Human mini-Gs/i43: N-term & AHD/α5 from Gαi1 62 β1 Human γ2 Human Cryo-EM 8XIP - 3.3 SSR1 SSTR1 SST1 Somatostatin A (Rhodopsin) Human - Nanobody-35 - pasireotide pubchem gtoplig drugbank chembl_ligand drug_central
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide - - 2024-07-03
Gq/11 αq Human Gαs/Gαi1 chimera, likely w/ Gq α5 for coupling 59 β1 Human γ2 Human Cryo-EM 8XOI 8XOI_refined 3.2 GPER1 GPER1 GPER Estrogen (G protein-coupled) A (Rhodopsin) Human - - - - None - 17β-estradiol Small molecule Liu H, Guo S, Dai A, Xu P, Li X, Huang S, He X, Wu K, Zhang X, Yang D, Xie X, Xu HE 10.1038/S41422-024-00963-Y 2024-04-10
Gq/11 αq Human mini-Gs/q chimera: Gi1 N-term/AHD, Gq body 61 β1 Rat γ2 Bovine Cryo-EM 8XOR 8XOR_refined 3.0 PAR1 F2R PAR1 Proteinase-activated A (Rhodopsin) Human - - LgBiT - - - thrombin (Human), thrombin (Rat), thrombin (Mouse) Peptide - - 2024-09-18
Gi/o αi1 Human DN Gαi1: G203A/A326S, Gβ1-SmBit fusion 64 β1 Human γ2 Human Cryo-EM 8XQS - 3.3 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - Exo-alpha-sialidase (NanI)
LgBiT 		Cholesterol pubchem drugbank
flufenamic acid pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule
Small molecule 		Agonist
Allosteric agonist 		- - Hu X, Ao W, Gao M, Wu L, Pei Y, Liu S, Wu Y, Zhao F, Sun Q, Liu J, Jiang L, Wang X, Li Y, Tan Q, Cheng J, Yang F, Yang C, Sun J, Hua T, Liu ZJ 10.1038/S41586-024-07569-9 2024-07-10
Gi/o αgust Human Gustducin/GNAI1 N-term chimera+V265I, scFv16 63 β1 Human γ2 Human Cryo-EM 8XQP - 3.3 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - NanI sialidase
LgBiT
HiBiT 		Cholesterol pubchem drugbank
aristolochic acid pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
Allosteric agonist 		- - Hu X, Ao W, Gao M, Wu L, Pei Y, Liu S, Wu Y, Zhao F, Sun Q, Liu J, Jiang L, Wang X, Li Y, Tan Q, Cheng J, Yang F, Yang C, Sun J, Hua T, Liu ZJ 10.1038/S41586-024-07569-9 2024-07-10
Gq/11 αq Human MiniGs/q: Gq-mimicking α5 fragment only 60 β1 Human γ2 Human Cryo-EM 8XVH 8XVH_refined 3.3 EDNRB EDNRB ETB Endothelin A (Rhodopsin) Human Sialidase H
BRIL 		Nanobody-35 - endothelin-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Protein Agonist endothelin-2 (Mouse), endothelin-2 (Human), endothelin-1 (Human), endothelin-3 (Human) Protein Hou J, Liu S, Zhang X, Tu G, Wu L, Zhang Y, Yang H, Li X, Liu J, Jiang L, Tan Q, Bai F, Liu Z, Miao C, Hua T, Luo Z 10.1038/S41421-024-00705-9 2024-08-28
Gi/o αi1 Human Fusion: human Gαi1 fused to bovine Gγ2 (linker) 60 β1 Bovine γ2 Human Cryo-EM 8YH0 - 2.9 AA3R ADORA3 A3 Adenosine A (Rhodopsin) Sheep - - LgBiT
eGFP 		NECA pubchem gtoplig chembl_ligand
Small molecule Agonist - - Oshima HS, Ogawa A, Sano FK, Akasaka H, Kawakami T, Iwama A, Okamoto HH, Nagiri C, Wei FY, Shihoya W, Nureki O 10.1038/S41467-024-53473-1 2024-11-06
Gi/o αi3 Human DN Gi3: S47N/G203A/E245A/A326S 63 β1 Rat γ2 Bovine Cryo-EM 8YK0 - 2.4 GP156 GPR156 GPR156 Orphan C (Glutamate) Human - - - - None - - - Ma X, Chen LN, Liao M, Zhang L, Xi K, Guo J, Shen C, Shen DD, Cai P, Shen Q, Qi J, Zhang H, Zang SK, Dong YJ, Miao L, Qin J, Ji SY, Li Y, Liu J, Mao C, Zhang Y, Chai R 10.1038/S41467-024-54681-5 2025-02-05
Gq/11 αq Human MiniGq (miniGαq50) construct 64 β1 Human γ2 Human Cryo-EM 8YN2 - 2.7 HRH1 HRH1 H1 Histamine A (Rhodopsin) Human - - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W 10.1038/S41467-024-52585-Y 2024-10-09
Gq/11 αq Human Gi2-mini-Gq chimera, stabilizes active state 58 β1 Human γ2 Human Cryo-EM 8UWL - 2.8 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - lisuride pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (partial) tryptamine, 5-hydroxytryptamine Small molecule Lyu J, Kapolka N, Gumpper R, Alon A, Wang L, Jain MK, Barros-Alvarez X, Sakamoto K, Kim Y, DiBerto J, Kim K, Glenn IS, Tummino TA, Huang S, Irwin JJ, Tarkhanova OO, Moroz Y, Skiniotis G, Kruse AC, Shoichet BK, Roth BL 10.1126/SCIENCE.ADN6354 2024-05-29
Gs αs Human Mini-Gs399 construct 56 β1 Human γ2 Human Cryo-EM 8UXV - 3.2 O51G2 OR51G2 OR51G2 Olfactory family 51 O1 (Olfactory/extra-nasal 1) Human - Nanobody-35 - - None - - - de March CA, Ma N, Billesbolle CB, Tewari J, Llinas Del Torrent C, van der Velden WJC, Ojiro I, Takayama I, Faust B, Li L, Vaidehi N, Manglik A, Matsunami H 10.1038/S41586-024-08126-0 2024-10-30
Gs αs Human Mini-Gs399 construct 56 β1 Human γ2 Human Cryo-EM 8UXY - 3.3 OR1F1 OR1F1 OR1F1 Olfactory family 1 O2 (Olfactory/extra-nasal 2) Human - Nanobody-35 - Levomenthol pubchem drugbank
Small molecule Agonist - - de March CA, Ma N, Billesbolle CB, Tewari J, Llinas Del Torrent C, van der Velden WJC, Ojiro I, Takayama I, Faust B, Li L, Vaidehi N, Manglik A, Matsunami H 10.1038/S41586-024-08126-0 2024-10-30
Gs αs Human miniGs399: engineered truncated Gs protein 55 β1 Human γ2 Human Cryo-EM 8UY0 - 3.2 OR2T2 OR2T2 OR2T2 Olfactory family 2 O2 (Olfactory/extra-nasal 2) Human - Nanobody-35 - S-carvone pubchem
Small molecule Agonist - - de March CA, Ma N, Billesbolle CB, Tewari J, Llinas Del Torrent C, van der Velden WJC, Ojiro I, Takayama I, Faust B, Li L, Vaidehi N, Manglik A, Matsunami H 10.1038/S41586-024-08126-0 2024-10-30
Gs αs Human Mini-Gs399, fused to receptor during expression 55 β1 Human γ2 Human Cryo-EM 8UYQ - 3.5 OR4D5 OR4D5 OR4D5 Olfactory family 4 O2 (Olfactory/extra-nasal 2) Human - Nanobody-35 - 2-methylthiazoline pubchem
Small molecule Agonist - - de March CA, Ma N, Billesbolle CB, Tewari J, Llinas Del Torrent C, van der Velden WJC, Ojiro I, Takayama I, Faust B, Li L, Vaidehi N, Manglik A, Matsunami H 10.1038/S41586-024-08126-0 2024-10-30
Gq/11 αq Human mini-GaqiN: Gq backbone + Gi2 N-term, scFv16 57 β1 Human γ2 Human Cryo-EM 8V6U 8V6U_refined 3.0 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - Z7757 pubchem
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule Lyu J, Kapolka N, Gumpper R, Alon A, Wang L, Jain MK, Barros-Alvarez X, Sakamoto K, Kim Y, DiBerto J, Kim K, Glenn IS, Tummino TA, Huang S, Irwin JJ, Tarkhanova OO, Moroz Y, Skiniotis G, Kruse AC, Shoichet BK, Roth BL 10.1126/SCIENCE.ADN6354 2024-05-29
Gi/o αi1 Human DN Gαi1 (Gαi1DN), complex stabilizer 63 β1 Human γ2 Human Cryo-EM 8VVG - 3.3 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - GB18 pubchem
Small molecule Inverse agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2025-01-15
Gi/o αgust Human Gustducin/Gαi2 chimera, 8 stabilizing muts 63 β1 Human γ2 Human Cryo-EM 8VY9 - 2.9 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human BRIL - LgBiT compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Ago-PAM
Agonist 		- - - - 2024-04-03
Gs αs Human Gs/Gi1 chimera: Gs α5, Gi1 body for scFv16 60 β1 Human γ2 Human Cryo-EM 8W8R - 3.3 GP101 GPR101 GPR101 Orphan A (Rhodopsin) Human - - - AA-14 pubchem
Small molecule Allosteric agonist - - Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP 10.1038/S41589-023-01456-6 2024-01-03
Gs αs Human mini-Gs: N-term→Gαi1(1-18), scFv16 59 β1 Human γ2 Human Cryo-EM 8WCA - 3.5 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human - - - β-phenylethylamine pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gq/11 αq Human modGαq: miniGs scaffold, Gαi1 N-term, Gαq α5 57 β1 Human γ2 Human Cryo-EM 8WCB - 3.1 TAAR1 Taar1 TA1 Trace amine A (Rhodopsin) Mouse BRIL - - Cyclohexylammonium Ion pubchem drugbank pubchem drugbank
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine Small molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human G112: Gi1 N-term chimera; 9 DN mutations 59 β1 Rat γ2 Bovine Cryo-EM 8WG8 8WG8_refined 2.7 GLR GCGR glucagon Glucagon B1 (Secretin) Human - - - Unknown peptide (Chain X)
Peptide Unknown glucagon (Human) Protein Cong Z, Zhao F, Li Y, Luo G, Mai Y, Chen X, Chen Y, Lin S, Cai X, Zhou Q, Yang D, Wang MW 10.1038/S41421-024-00649-0 2024-03-06
Gi/o αi3 Human DN Gi3: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8WGB - 3.7 GRM4 GRM4 mGlu4 Metabotropic glutamate C (Glutamate) Human T4-Lysozyme - HiBiT
LgBiT 		L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
VU0155041 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		L-serine-O-phosphate, L-glutamic acid Small molecule Huang W, Jin N, Guo J, Shen C, Xu C, Xi K, Bonhomme L, Quast RB, Shen DD, Qin J, Liu YR, Song Y, Gao Y, Margeat E, Rondard P, Pin JP, Zhang Y, Liu J 10.1038/S41467-024-54744-7 2024-10-30
Gq/11 αq Human MiniGs/q: Gs scaffold with Gq-specific tail 62 β1 Human γ2 Human Cryo-EM 8WJX - 3.2 P2RY1 P2RY1 P2Y1 P2Y A (Rhodopsin) Human BRIL Nanobody-35 Gaussia luciferase (NanoLuc) ADP pubchem gtoplig chembl_ligand
Small molecule Agonist ADP, ATP Small molecule - - 2024-10-02
Gq/11 αq Human Gi2-miniGq chimera: Gq C-term on Gi2 scaffold 58 β1 Human γ2 Human Cryo-EM 8WPU - 3.1 CASR CASR CaS Calcium-sensing C (Glutamate) Human - - LgBiT D-tryptophan pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand drugbank drug_central
Calcium pubchem
cinacalcet pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule
Small molecule
Small molecule 		Agonist D-tryptophan, Mg2+, spermine, Ca2+ Small molecule Ling S, Meng X, Zhang Y, Xia Z, Zhou Y, Yang F, Shi P, Shi C, Tian C 10.1038/S41422-023-00892-2 2023-11-22
Gi/o αi1 Human DNGai: DN Gαi1, 4 mutations 63 β1 Human γ2 Human Cryo-EM 8WRB - 2.9 GPR34 GPR34 GPR34 Orphan A (Rhodopsin) Human - - - LYSOPHOSPHATIDIC ACID chembl_ligand pubchem
L-serine pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank pubchem drugbank
Small molecule
Small molecule 		Agonist lysophosphatidylserine Lipid Liu G, Li X, Wang Y, Zhang X, Gong W 10.1371/JOURNAL.PBIO.3002387 2023-11-08
Gq/11 αq Human Mini-Gq: Gs Ras domain, Gi1 N-term, Gq α5 helix 59 β1 Human γ2 Human Cryo-EM 8WST 8WST_refined 2.4 MCHR2 MCHR2 MCH2 Melanin-concentrating hormone A (Rhodopsin) Human - Nanobody-35 - melanin-concentrating hormone (Human) pubchem gtoplig uniprot uniprot uniprot
Peptide Agonist melanin-concentrating hormone (Human) Peptide He Q, Yuan Q, Shan H, Wu C, Gu Y, Wu K, Hu W, Zhang Y, He X, Xu HE, Zhao LH 10.1038/S41421-024-00679-8 2024-06-19
Gq/11 αq Human Gαq (paper); metadata: Gs/Gi backbone chimera 59 β1 Human γ2 Human Cryo-EM 8XOJ 8XOJ_refined 3.1 GPER1 GPER1 GPER Estrogen (G protein-coupled) A (Rhodopsin) Human - - - - None - 17β-estradiol Small molecule Liu H, Guo S, Dai A, Xu P, Li X, Huang S, He X, Wu K, Zhang X, Yang D, Xie X, Xu HE 10.1038/S41422-024-00963-Y 2024-04-10
Gi/o αi1 Human Standard Gi1 heterotrimer complex 63 β1 Human γ2 Human Cryo-EM 8WWH 8WWH_refined 2.8 MCHR1 MCHR1 MCH1 Melanin-concentrating hormone A (Rhodopsin) Human - - Fusion protein 1
Fusion protein 2 		- None - melanin-concentrating hormone (Human) Peptide - - 2024-11-13
Gq/11 αq Human GαsqiN: mini-Gs, Gαi1 N-term, for scFv16 60 β1 Rat γ2 Bovine Cryo-EM 8WZ2 8WZ2_refined 2.7 QRFPR QRFPR QRFP QRFP A (Rhodopsin) Human BRIL - - 26RFa pubchem
Peptide Agonist QRFP43 (43RFa) (Human), QRFP43 (Rat), QRFP26 (26RFa) (Human) Peptide Jin S, Guo S, Xu Y, Li X, Wu C, He X, Pan B, Xin W, Zhang H, Hu W, Yin Y, Zhang T, Wu K, Yuan Q, Xu HE, Xie X, Jiang Y 10.1038/S41421-024-00670-3 2024-06-19
Gi/o αi1 Bovine DN bovine Gi: G203A/A326S mutations 61 β1 Rat γ2 Bovine Cryo-EM 8X16 8X16_refined 3.3 AA3R ADORA3 A3 Adenosine A (Rhodopsin) Human BRIL - - piclidenoson pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank
Small molecule Agonist adenosine Small molecule Cai H, Guo S, Xu Y, Sun J, Li J, Xia Z, Jiang Y, Xie X, Xu HE 10.1038/S41467-024-47207-6 2024-04-24
Gi/o αi1 Human mini-Gs/i43 chimera; Gβ1-SmBiT fusion 62 β1 Human γ2 Human Cryo-EM 8X8N 8X8N_refined 2.9 SSR5 SSTR5 SST5 Somatostatin A (Rhodopsin) Human - - - octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide - - 2024-06-12
Gs αs Bovine Human Gs, thermostabilized; bovine/rat subunits 58 β1 Rat γ2 Bovine Cryo-EM 8X9T - 2.8 AGRD1 ADGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - - - AP503 pubchem
Small molecule Agonist dihydrotestosterone Small molecule Yang Z, Ping YQ, Wang MW, Zhang C, Zhou SH, Xi YT, Zhu KK, Ding W, Zhang QY, Song ZC, Zhao RJ, He ZL, Wang MX, Qi L, Ullmann C, Ricken A, Schoneberg T, Gan ZJ, Yu X, Xiao P, Yi F, Liebscher I, Sun JP 10.1016/J.CELL.2025.01.006 2025-02-12
Gs αs Human mini-Gs (human); rat Gβ1, bovine Gγ2 58 β1 Rat γ2 Bovine Cryo-EM 8X9U - 2.9 AGRD1 ADGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - - - Metenolone drugbank pubchem
Small molecule Agonist (partial) dihydrotestosterone Small molecule - - 2025-02-12
Gq/11 αq Human Gαq chimera: N-term(18)→Gαi1, scFv16 64 β1 Human γ2 Human Cryo-EM 8XGO - 2.7 KISSR KISS1R kisspeptin Kisspeptin A (Rhodopsin) Human BRIL - LgBiT
SmBiT 		TAK448
Peptide Agonist kisspeptin-10 (Mouse), kisspeptin-52 (Mouse), kisspeptin-13 (Human), kisspeptin-14 (Human), kisspeptin-54 (Human), kisspeptin-10 (Human), kisspeptin-52 (Rat) Peptide Wu Z, Chen G, Qiu C, Yan X, Xu L, Jiang S, Xu J, Han R, Shi T, Liu Y, Gao W, Wang Q, Li J, Ye F, Pan X, Zhang Z, Ning P, Zhang B, Chen J, Du Y 10.1126/SCIADV.ADN7771 2024-10-30
Gi/o αi1 Human mini-Gs w/ Gαi1 αN & α5 helices 62 β1 Human γ2 Human Cryo-EM 8XIQ - 2.7 SSR3 SSTR3 SST3 Somatostatin A (Rhodopsin) Human - Nanobody-35 - L-796,778 pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide - - 2024-07-03
Gi/o αi1 Human mini-Gs/i43: N-term/AHD/α5 from Gαi1 62 β1 Human γ2 Human Cryo-EM 8XIR - 2.5 SSR3 SSTR3 SST3 Somatostatin A (Rhodopsin) Human - Nanobody-35 - pasireotide pubchem gtoplig drugbank chembl_ligand drug_central
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide - - 2024-07-03
Gq/11 αq Human mini-Gs/i1/Gq chimera: Gi1 N-term, scFv16 58 β1 Human γ2 Human Cryo-EM 8XJK 8XJK_refined 2.6 PF2R PTGFR FP Prostanoid A (Rhodopsin) Human - - LgBiT
beta-2 adrenergic receptor N-terminal fragment (BN) 		cloprostenol pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist PGF2α, PGE2, PGD2, PGI2, thromboxane A2 Small molecule - - 2024-02-28
Gq/11 αq Human MiniGq: Gs skeleton, Gi1 N-term, Gq muts 58 β1 Human γ2 Human Cryo-EM 8XJL 8XJL_refined 2.8 PF2R PTGFR FP Prostanoid A (Rhodopsin) Human - - LgBiT
BN (beta-2 adrenergic receptor N-terminus fragment) 		PGF2α pubchem gtoplig chembl_ligand drug_central pubchem drugbank drugbank
Small molecule Agonist PGF2α, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Li X, Zhang X, Wen X, Zhang D, Qu C, Miao X, Zhang W, Zhang R, Liu G, Xiao P, Sun JP, Gong W 10.1016/J.CELREP.2024.113893 2024-02-28
Gq/11 αq Human Gαq/Gαi1 chimera for scFv16, keeps Gq spec 59 β1 Human γ2 Human Cryo-EM 8XOH 8XOH_refined 3.2 GPER1 GPER1 GPER Estrogen (G protein-coupled) A (Rhodopsin) Human - - - - None - 17β-estradiol Small molecule Liu H, Guo S, Dai A, Xu P, Li X, Huang S, He X, Wu K, Zhang X, Yang D, Xie X, Xu HE 10.1038/S41422-024-00963-Y 2024-04-10
Gq/11 αq Human MiniGq: Gs+Gi1 N-term, Gq specificity 58 β1 Human γ2 Human Cryo-EM 8XJM 8XJM_refined 2.9 PF2R PTGFR FP Prostanoid A (Rhodopsin) Human - - LgBiT and BN Fusion latanoprost (free acid form) pubchem gtoplig chembl_ligand
Small molecule Agonist PGF2α, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Li X, Zhang X, Wen X, Zhang D, Qu C, Miao X, Zhang W, Zhang R, Liu G, Xiao P, Sun JP, Gong W 10.1016/J.CELREP.2024.113893 2024-02-28
Gq/11 αq Human MiniGq: Gs skeleton, Gi1 N-term, DN muts 58 β1 Human γ2 Human Cryo-EM 8XJN 8XJN_refined 3.1 TA2R TBXA2R TP Prostanoid A (Rhodopsin) Human - - LgBiT
b2 adrenergic receptor N-terminal fragment (BN) 		cloprostenol pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist PGF2α, PGH2, PGE2, PGD2, PGI2, thromboxane A2 Small molecule - - 2024-02-28
Gq/11 αq Human MiniGq (miniGqiN): Gs skeleton, Gi1 N-term, DN 58 β1 Human γ2 Human Cryo-EM 8XJO 8XJO_refined 3.1 TA2R TBXA2R TP Prostanoid A (Rhodopsin) Human - - LgBiT
BN (beta-2 adrenergic receptor N-terminal fragment) 		U46619 pubchem gtoplig chembl_ligand
Small molecule Agonist PGF2α, PGH2, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Li X, Zhang X, Wen X, Zhang D, Qu C, Miao X, Zhang W, Zhang R, Liu G, Xiao P, Sun JP, Gong W 10.1016/J.CELREP.2024.113893 2024-02-28
Gq/11 αq Human WT human Gq heterotrimer (Gαq/Gβ1/Gγ2) 59 β1 Human γ2 Human Cryo-EM 8XOF 8XOF_refined 2.6 GPER1 GPER1 GPER Estrogen (G protein-coupled) A (Rhodopsin) Human - Nanobody-35 - Lys05 pubchem
Small molecule Agonist 17β-estradiol Small molecule - - 2024-04-10
Gq/11 αq Human Gs/Gi1 chimeric scaffold, likely for Gq scFv16 use 59 β1 Human γ2 Human Cryo-EM 8XOG - 2.9 GPER1 GPER1 GPER Estrogen (G protein-coupled) A (Rhodopsin) Human - - - - None - 17β-estradiol Small molecule Liu H, Guo S, Dai A, Xu P, Li X, Huang S, He X, Wu K, Zhang X, Yang D, Xie X, Xu HE 10.1038/S41422-024-00963-Y 2024-04-10
Gi/o αgust Human miniGs/gust: Gαs body, gustducin α5(329-354) 63 β1 Human γ2 Human Cryo-EM 8XQL - 3.0 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - Nanobody-35 NanI sialidase
LgBiT
HiBiT 		Cholesterol pubchem drugbank
aristolochic acid pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
Allosteric agonist 		- - Hu X, Ao W, Gao M, Wu L, Pei Y, Liu S, Wu Y, Zhao F, Sun Q, Liu J, Jiang L, Wang X, Li Y, Tan Q, Cheng J, Yang F, Yang C, Sun J, Hua T, Liu ZJ 10.1038/S41586-024-07569-9 2024-07-10
Gi/o αi1 Human DN Gαi1: G203A/A326S; Gβ-SmBiT fusion 64 β1 Human γ2 Human Cryo-EM 8XQN - 3.1 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - NanI sialidase
LgBiT
HiBiT 		Cholesterol pubchem drugbank
aristolochic acid pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
Allosteric agonist 		- - Hu X, Ao W, Gao M, Wu L, Pei Y, Liu S, Wu Y, Zhao F, Sun Q, Liu J, Jiang L, Wang X, Li Y, Tan Q, Cheng J, Yang F, Yang C, Sun J, Hua T, Liu ZJ 10.1038/S41586-024-07569-9 2024-07-10
Gi/o αi1 Human DN Gs: G203A/A326S; Gβ-SmBiT fusion 64 β1 Human γ2 Human Cryo-EM 8XQO - 2.8 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - NanI sialidase (catalytic domain)
LgBiT
HiBiT 		Cholesterol pubchem drugbank
aristolochic acid pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
Allosteric agonist 		- - Hu X, Ao W, Gao M, Wu L, Pei Y, Liu S, Wu Y, Zhao F, Sun Q, Liu J, Jiang L, Wang X, Li Y, Tan Q, Cheng J, Yang F, Yang C, Sun J, Hua T, Liu ZJ 10.1038/S41586-024-07569-9 2024-07-10
Gi/o αgust Human miniGs/gust chimera: Gs body, gustducin α5 63 β1 Human γ2 Human Cryo-EM 8XQR - 3.2 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - Nanobody-35 NanI sialidase
LgBiT
HiBiT 		flufenamic acid pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Allosteric agonist - - Hu X, Ao W, Gao M, Wu L, Pei Y, Liu S, Wu Y, Zhao F, Sun Q, Liu J, Jiang L, Wang X, Li Y, Tan Q, Cheng J, Yang F, Yang C, Sun J, Hua T, Liu ZJ 10.1038/S41586-024-07569-9 2024-07-10
Gi/o αi1 Human DN G protein: G203A/A326S mutations 64 β1 Human γ2 Human Cryo-EM 8XQT - 2.9 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - NanI sialidase
LgBiT
HiBiT 		Cholesterol pubchem drugbank
Small molecule Agonist - - Hu X, Ao W, Gao M, Wu L, Pei Y, Liu S, Wu Y, Zhao F, Sun Q, Liu J, Jiang L, Wang X, Li Y, Tan Q, Cheng J, Yang F, Yang C, Sun J, Hua T, Liu ZJ 10.1038/S41586-024-07569-9 2024-07-10
Gq/11 αq Human MiniGs/q: Gs backbone, Gq α5 helix 60 β1 Human γ2 Human Cryo-EM 8XVE 8XVE_refined 3.0 EDNRB EDNRB ETB Endothelin A (Rhodopsin) Human Sialidase H Nanobody-35 - BQ 3020 pubchem gtoplig
Peptide Agonist endothelin-2 (Mouse), endothelin-2 (Human), endothelin-1 (Human), endothelin-3 (Human) Protein Hou J, Liu S, Zhang X, Tu G, Wu L, Zhang Y, Yang H, Li X, Liu J, Jiang L, Tan Q, Bai F, Liu Z, Miao C, Hua T, Luo Z 10.1038/S41421-024-00705-9 2024-08-28
Gq/11 αq Human MiniGαs/q: Gs α with Gq-derived α5 helix 60 β1 Human γ2 Human Cryo-EM 8XVI 8XVI_refined 3.3 EDNRA EDNRA ETA Endothelin A (Rhodopsin) Human BRIL Nanobody-35 Endoglucanase H endothelin-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Protein Agonist endothelin-2 (Mouse), endothelin-2 (Human), endothelin-1 (Human), endothelin-3 (Human) Protein Hou J, Liu S, Zhang X, Tu G, Wu L, Zhang Y, Yang H, Li X, Liu J, Jiang L, Tan Q, Bai F, Liu Z, Miao C, Hua T, Luo Z 10.1038/S41421-024-00705-9 2024-08-28
Gi/o αi1 Human DN Gi1 heterotrimer: Gαi1 4 muts; rat Gβ1/Gγ2 64 β1 Human γ2 Human Cryo-EM 8XXU - 2.5 PD2R2 PTGDR2 DP2 Prostanoid A (Rhodopsin) Human BRIL - LgBiT - None - PGF2α, Δ12-PGJ2, PGE2, PGD2, PGI2, PGD3, thromboxane A2 Small molecule - - 2024-12-04
Gq/11 αq Human mini-Gs/q71: N-term/AHD from human Gαi1 60 β1 Human γ2 Human Cryo-EM 8Y52 8Y52_refined 2.9 BRS3 BRS3 BB3 Bombesin A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		BA1
Peptide Agonist - - Li C, Xu Y, Su W, He X, Li J, Li X, Xu HE, Yin W 10.1016/J.CELREP.2024.114511 2024-09-11
Gq/11 αq Human Mini-Gs/q71: Gi1 N-term/AHD, DN G203A/A326S 60 β1 Human γ2 Human Cryo-EM 8Y53 8Y53_refined 2.9 BRS3 BRS3 BB3 Bombesin A (Rhodopsin) Human BRIL Nanobody-35 - MK-5046 pubchem gtoplig chembl_ligand
Small molecule Agonist - - - - 2024-09-11
Gq/11 αq Mouse - 61 β1 Rat γ2 Bovine Cryo-EM 8YFS - 2.8 A0A9L0JPP9 - MRGPRE Orphan A (Rhodopsin) Donkey - - - (E)-3-(2-methoxyphenyl)prop-2-enal pubchem
Small molecule Agonist - - - - 2025-03-05
Gi/o αi1 Human Gαi1-Gγ2 fusion (GSAGSAGSA linker); rat Gβ1 60 β1 Bovine γ2 Human Cryo-EM 8YH2 - 3.3 AA3R ADORA3 A3 Adenosine A (Rhodopsin) Sheep - - GFP
Hemagglutinin (HA) tag 		adenosine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist - - Oshima HS, Ogawa A, Sano FK, Akasaka H, Kawakami T, Iwama A, Okamoto HH, Nagiri C, Wei FY, Shihoya W, Nureki O 10.1038/S41467-024-53473-1 2024-11-06
Gi/o αi1 Bovine Gαi1 fused to C-term of bovine Gγ2 60 β1 Bovine γ2 Human Cryo-EM 8YH3 - 3.4 AA3R ADORA3 A3 Adenosine A (Rhodopsin) Sheep - - GFP
Hemagglutinin 		CHEMBL383144 chembl_ligand pubchem
Small molecule Agonist - - Oshima HS, Ogawa A, Sano FK, Akasaka H, Kawakami T, Iwama A, Okamoto HH, Nagiri C, Wei FY, Shihoya W, Nureki O 10.1038/S41467-024-53473-1 2024-11-06
Gi/o αi1 Bovine Fusion-G: Gαi1-Gγ2 fusion (human/human/rat Gβ1) 60 β1 Bovine γ2 Human Cryo-EM 8YH5 - 3.7 AA3R ADORA3 A3 Adenosine A (Rhodopsin) Sheep - - GFP
Hemagglutinin 		Riboprine pubchem drugbank
Small molecule Agonist - - Oshima HS, Ogawa A, Sano FK, Akasaka H, Kawakami T, Iwama A, Okamoto HH, Nagiri C, Wei FY, Shihoya W, Nureki O 10.1038/S41467-024-53473-1 2024-11-06
Gi/o αi1 Bovine Gαi1(bovine)-Gγ2 fusion; Gβ1(rat)-HiBiT tag 60 β1 Bovine γ2 Human Cryo-EM 8YH6 - 3.6 AA3R ADORA3 A3 Adenosine A (Rhodopsin) Sheep - - HA-signal peptide
LgBiT
eGFP 		Cl-IB-MECA pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist - - Oshima HS, Ogawa A, Sano FK, Akasaka H, Kawakami T, Iwama A, Okamoto HH, Nagiri C, Wei FY, Shihoya W, Nureki O 10.1038/S41467-024-53473-1 2024-11-06
Gi/o αgust Human Gαg/i chimera: Gαi1 N-term, V265I, SmBit 61 β1 Human γ2 Human Cryo-EM 8YKY - 3.0 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - NanI sialidase
LgBiT 		Cholesterol pubchem drugbank
compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
Allosteric agonist 		- - - - 2024-07-10
Gs αs Human Gs heterotrimer (mini-Gs) for stabilization 59 β1 Bovine γ Greater horseshoe bat Cryo-EM 8YKD - 2.9 AGRG2 Adgrg2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - PRASTERONE chembl_ligand pubchem drugbank
Small molecule Agonist - - Zheng Y, Jiang D, Lu Y, Zhang C, Huang SM, Lin H, Zhang D, Guo S, Han J, Chen J, He Y, Zhang M, Gao Y, Guo Y, Wei R, Xia M, Qin Y, Liu Z, Yang F, Ge S, Yi F, Yu X, Lin H, Xiao P, Sun JP, Feng S 10.1038/S41589-025-01896-2 2025-08-13
Gq/11 αq Human mini-GαqiN: Gs/Gq chimera for stabilization 57 β1 Human γ2 Human Cryo-EM 8YRG 8YRG_refined 3.1 MRGX4 MRGPRX4 MRGPRX4 Orphan A (Rhodopsin) Human BRIL - - Fospropofol pubchem drugbank
Small molecule Agonist - - - - 2024-05-22
Gq/11 αq Human mini-G chimera of Gαo and Gαq 57 β1 Human γ2 Human Cryo-EM 8YRQ - 2.8 PAR4 F2RL3 PAR4 Proteinase-activated A (Rhodopsin) Human - - Maltose/maltodextrin-binding periplasmic protein - - - cathepsin G (Rat), thrombin (Human), cathepsin G (Mouse), thrombin (Mouse), cathepsin G (Human), thrombin (Rat) Peptide - - 2026-06-10
Gi/o αi1 Human DNGnai1: DN Gαi1 w/ stabilizing muts 64 β1 Human γ2 Human Cryo-EM 8YUU - 2.7 HRH3 HRH3 H3 Histamine A (Rhodopsin) Human - - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule Shen Q, Tang X, Wen X, Cheng S, Xiao P, Zang SK, Shen DD, Jiang L, Zheng Y, Zhang H, Xu H, Mao C, Zhang M, Hu W, Sun JP, Zhang Y, Chen Z 10.1002/ADVS.202310120 2024-06-05
Gs αs Human Mini-Gs (mGs) protein 59 β1 Human γ2 Human Cryo-EM 8YY8 - 3.2 FZD7 FZD7 FZD7 WNT F (Frizzled) Human - Nanobody-35 - - None - - - Xu L, Chen B, Schihada H, Wright SC, Turku A, Wu Y, Han GW, Kowalski-Jahn M, Kozielewicz P, Bowin CF, Zhang X, Li C, Bouvier M, Schulte G, Xu F 10.1038/S41422-021-00525-6 2024-04-24
Gq/11 αq Human mini-Gαs/q71: Gαi1 N-term/AHD, for scFv16 59 β1 Human γ2 Human Cryo-EM 8ZPT 8ZPT_refined 3.0 PRLHR PRLHR PrRP Prolactin-releasing peptide A (Rhodopsin) Human - - - PrRP20 pubchem
Peptide Agonist PrRP-20 (Human), PrRP-20 (Rat), neuropeptide Y (Human), PTHrP (Human), PrRP-31 (Rat), PrRP-31 (Human) Peptide Li Y, Yuan Q, He X, Zhang Y, You C, Wu C, Li J, Xu HE, Zhao LH 10.1038/S41421-024-00724-6 2024-09-25
Gs αs Human DN Gs: site-directed muts, reduce nucl. affinity 56 β1 Rat γ2 Bovine Cryo-EM 8Z9O - 2.4 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 - - None - - - Chen LN, Zhou H, Xi K, Cheng S, Liu Y, Fu Y, Ma X, Xu P, Ji SY, Wang WW, Shen DD, Zhang H, Shen Q, Chai R, Zhang M, Yang L, Han F, Mao C, Cai X, Zhang Y 10.1016/J.MOLCEL.2025.02.030 2025-07-16
Gi/o αi1 Human DN G protein, site-directed mutations 64 β1 Rat γ2 Bovine Cryo-EM 8Z9P - 2.5 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - - - - None - - - Chen LN, Zhou H, Xi K, Cheng S, Liu Y, Fu Y, Ma X, Xu P, Ji SY, Wang WW, Shen DD, Zhang H, Shen Q, Chai R, Zhang M, Yang L, Han F, Mao C, Cai X, Zhang Y 10.1016/J.MOLCEL.2025.02.030 2025-07-09
Gi/o αi1 Human DN Gαi1 (G203A/A326S); Gβ1-HiBit, Gγ2 60 β1 Rat γ Rat Cryo-EM 8ZBE 8ZBE_refined 3.2 SSR5 SSTR5 SST5 Somatostatin A (Rhodopsin) Human - - HA-Flag-beta2AR(1-24) fusion
LgBiT
HiBiT 		octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Li YG, Meng XY, Yang X, Ling SL, Shi P, Tian CL, Yang F 10.1038/S41401-024-01314-8 2024-07-10
Gq/11 αq Human Gαq/i1 chimera: DN G208A/A331S, Gβ1-HiBiT 63 β1 Human γ2 Human Cryo-EM 8ZJD - 3.1 KISSR KISS1R kisspeptin Kisspeptin A (Rhodopsin) Human - - LgBiT
HiBiT 		kisspeptin-10 (Human) pubchem gtoplig chembl_ligand
Peptide Agonist kisspeptin-10 (Mouse), kisspeptin-52 (Mouse), kisspeptin-13 (Human), kisspeptin-14 (Human), kisspeptin-54 (Human), kisspeptin-10 (Human), kisspeptin-52 (Rat) Peptide - - 2024-07-03
Gq/11 αq Human Gαq/i1: Gi1 αN, DN G208A/A331S, Gβ1-HiBiT 63 β1 Human γ2 Human Cryo-EM 8ZJE - 3.1 KISSR KISS1R kisspeptin Kisspeptin A (Rhodopsin) Human - - - TAK-448 pubchem gtoplig chembl_ligand drugbank
Peptide Agonist kisspeptin-10 (Mouse), kisspeptin-52 (Mouse), kisspeptin-13 (Human), kisspeptin-14 (Human), kisspeptin-54 (Human), kisspeptin-10 (Human), kisspeptin-52 (Rat) Peptide - - 2024-07-03
Gq/11 αq Human miniGs/q: Gs base + Gq α5 helix, truncated AHD 59 β1 Human γ2 Human Cryo-EM 8ZMD - 3.3 PAR2 F2RL1 PAR2 Proteinase-activated A (Rhodopsin) Human - - LgBiT
HiBiT 		- - - - - Zhu X, Xia R, Zhang A, Guo C, Xu Z, He Y 10.1038/S41421-025-00851-8 2025-05-28
Gi/o αi1 Human mini-Gs/i143: Gs + Gi1 N-term/AHD, scFv16 57 β1 Human γ2 Human Cryo-EM 8ZPS 8ZPS_refined 3.0 PRLHR PRLHR PrRP Prolactin-releasing peptide A (Rhodopsin) Human - - - PrRP20 pubchem
Peptide Agonist PrRP-20 (Human), PrRP-20 (Rat), neuropeptide Y (Human), PTHrP (Human), PrRP-31 (Rat), PrRP-31 (Human) Peptide Li Y, Yuan Q, He X, Zhang Y, You C, Wu C, Li J, Xu HE, Zhao LH 10.1038/S41421-024-00724-6 2024-09-25
Gq/11 αq Human mini-GαqiN: Gi2 N-term, for scFv16 60 β1 Human γ2 Human Cryo-EM 9ARY - 3.3 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule Gumpper RH, Jain MK, Kim K, Sun R, Sun N, Xu Z, DiBerto JF, Krumm BE, Kapolka NJ, Kaniskan HU, Nichols DE, Jin J, Fay JF, Roth BL 10.1038/S41467-025-57956-7 2025-04-02
Gq/11 αq Human Mini-Gq (mini-GaqiN): Gi2/Gq chimera 60 β1 Human γ2 Human Cryo-EM 9AS0 - 3.4 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - 2-bromo-LSD pubchem gtoplig chembl_ligand
Small molecule Agonist (partial) tryptamine, 5-hydroxytryptamine Small molecule - - 2025-04-02
Gq/11 αq Human mini-GαqiN: engineered for Gq coupling 59 β1 Human γ2 Human Cryo-EM 9AS8 - 2.5 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - psilocin pubchem gtoplig chembl_ligand
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule Gumpper RH, Jain MK, Kim K, Sun R, Sun N, Xu Z, DiBerto JF, Krumm BE, Kapolka NJ, Kaniskan HU, Nichols DE, Jin J, Fay JF, Roth BL 10.1038/S41467-025-57956-7 2025-04-02
Gq/11 αq Human Gi2-miniGq chimera, for scFv16 stabilization 59 β1 Human γ2 Human Cryo-EM 9ASA - 3.1 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - RS130-180 pubchem
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule - - 2025-04-02
Gq/11 αq Human miniGis/q: Gs skeleton w/ Gq H5 substitutions 60 β1 Human γ2 Human Cryo-EM 9ASB - 3.4 CASR CASR CaS Calcium-sensing C (Glutamate) Human - - - Calcium pubchem
CYCLOMETHYLTRYPTOPHAN pubchem
tecalcet pubchem gtoplig chembl_ligand
Small molecule
Small molecule
Small molecule 		Agonist D-tryptophan, Mg2+, spermine, Ca2+ Small molecule - - 2024-04-17
Gs αs Human miniGαis: Gαi1 N-term; H5=Gs; thermostab muts 57 β1 Human γ2 Human Cryo-EM 9AVG - 3.6 CASR CASR CaS Calcium-sensing C (Glutamate) Human - - - Calcium pubchem
CYCLOMETHYLTRYPTOPHAN pubchem
tecalcet pubchem gtoplig chembl_ligand
Small molecule
Small molecule
Small molecule 		Agonist D-tryptophan, Mg2+, spermine, Ca2+ Small molecule - - 2024-04-17
Gq/11 αq Human miniGisq: Gαi1 N-term, Gαq C-term H5 helix 59 β1 Human γ2 Human Cryo-EM 9AXF - 3.5 CASR CASR CaS Calcium-sensing C (Glutamate) Human - Nanobody-35 - Calcium pubchem
CYCLOMETHYLTRYPTOPHAN pubchem
tecalcet pubchem gtoplig chembl_ligand
Small molecule
Small molecule
Small molecule 		Agonist D-tryptophan, Mg2+, spermine, Ca2+ Small molecule Zuo H, Park J, Frangaj A, Ye J, Lu G, Manning JJ, Asher WB, Lu Z, Hu GB, Wang L, Mendez J, Eng E, Zhang Z, Lin X, Grassucci R, Hendrickson WA, Clarke OB, Javitch JA, Conigrave AD, Fan QR 10.1038/S41586-024-07331-1 2024-04-17
Gi/o αi1 Human MiniGαi1: Gi1 N-term on Gs skeleton, scFv16 60 β1 Human γ2 Human Cryo-EM 9AYF - 3.6 CASR CASR CaS Calcium-sensing C (Glutamate) Human - - - CYCLOMETHYLTRYPTOPHAN pubchem
Calcium pubchem
tecalcet pubchem gtoplig chembl_ligand
Small molecule
Small molecule
Small molecule 		Agonist D-tryptophan, Mg2+, spermine, Ca2+ Small molecule Zuo H, Park J, Frangaj A, Ye J, Lu G, Manning JJ, Asher WB, Lu Z, Hu GB, Wang L, Mendez J, Eng E, Zhang Z, Lin X, Grassucci R, Hendrickson WA, Clarke OB, Javitch JA, Conigrave AD, Fan QR 10.1038/S41586-024-07331-1 2024-04-17
Gq/11 αq Human GαqiN: Gαq w/ Gi N-term (35aa) for scFv16 62 β1 Human γ2 Human Cryo-EM 9B5Y - 3.5 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - - LargeBit
HiBiT 		Long-acting parathyroid hormone analog pubchem
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Zhang X, Lee JY, Pacheco J, Sutkeviciute I, Anitha AK, Liu H, Singh S, Ventura C, Savransky S, Khatri A, Zhang C, Bahar I, Vilardaga JP 10.1073/PNAS.2426178122 2025-03-19
Gq/11 αq Human miniGsq: miniGs body, Gαq α5 determinants 52 β1 Human γ2 Human Cryo-EM 9BI6 9BI6_refined 2.9 GPR68 GPR68 GPR68 Proton A (Rhodopsin) Human - Nanobody-35 - - None - - - Howard MK, Hoppe N, Huang XP, Mitrovic D, Billesbolle CB, Macdonald CB, Mehrotra E, Rockefeller Grimes P, Trinidad DD, Delemotte L, English JG, Coyote-Maestas W, Manglik A 10.1016/J.CELL.2024.11.036 2025-01-15
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 9BP3 - 2.2 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- cagrilintide pubchem gtoplig drugbank
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide - - 2025-04-23
Gi/o αi1 Rat DN rat Gαi1: G203A mutation 60 β1 Bovine γ2 Bovine Cryo-EM 9CBL - 2.8 ADA2A ADRA2A α2A Adrenoceptors A (Rhodopsin) Human T4-Lysozyme - - (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Lou JS, Su M, Wang J, Do HN, Miao Y, Huang XY 10.1038/S12276-024-01296-X 2024-09-11
Gq/11 αq Human mGαi/s/q: Gαq C-term(15) + Gαi N-term(35) 58 β1 Human γ2 Human Cryo-EM 9CM3 - 3.1 FFAR2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - - - CHEMBL5965059 chembl_ligand pubchem
CHEMBL4176503 chembl_ligand pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		butyric acid, propanoic acid, trans-2-methylcrotonic acid, acetic acid Small molecule - - 2025-06-25
Gq/11 αq Human GqiN: Gαq w/ Gs/Gi N-term, for scFv16 60 β1 Human γ2 Human Cryo-EM 9D0A - 3.1 PAR2 F2RL1 PAR2 Proteinase-activated A (Rhodopsin) Human - - - - - - - - Lyu Z, Lyu X, Malyutin AG, Xia G, Carney D, Alves VM, Falk M, Arora N, Zou H, McGrath AP, Kang Y 10.1038/S41467-025-59138-X 2025-05-07
Gq/11 αq Human GqiN: N-term replaced by Gαi (1-28 res) 60 β1 Human γ2 Human Cryo-EM 9E7R - 3.2 PAR2 F2RL1 PAR2 Proteinase-activated A (Rhodopsin) Human - - - GB88 pubchem
Small molecule Agonist (partial) - - - - 2025-05-07
Gi/o αi1 Human mini-Gs/i148: Gs backbone + Gi1 α5 helix 59 β1 Human γ2 Human Cryo-EM 9EBI - 3.6 AA3R ADORA3 A3 Adenosine A (Rhodopsin) Human - Nanobody-35 - piclidenoson pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank
Small molecule Agonist adenosine Small molecule Zhang L, Mobbs JI, Bennetts FM, Venugopal H, Nguyen ATN, Christopoulos A, van der Es D, Heitman LH, May LT, Glukhova A, Thal DM 10.1038/S41467-025-62872-X 2025-08-20
Gq/11 αq Human miniGs skeleton: Gi1 N-term, Gq body 59 β1 Human γ2 Human Cryo-EM 9M1R - 2.7 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human BRIL Nanobody-35 - α-ketoglutaric acid pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist α-ketoglutaric acid Small molecule None 10.1038/S44318-026-00823-Y 2026-06-17
Gs αs Human DN Gs protein 59 β1 Human γ2 Human Cryo-EM 9EBQ - 3.2 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 2 (GLP-1 (ACPC18))
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cary BP, Hager MV, Mariam Z, Morris RK, Belousoff MJ, Deganutti G, Sexton PM, Wootten D, Gellman SH 10.1073/PNAS.2407574122 2025-03-26
Gq/11 αq Human mini-GαsqiN: mini-Gαs + Gαq interface + Gαi αN 64 β1 Rat γ2 Human Cryo-EM 9EJZ - 2.1 ACM5 CHRM5 M5 Acetylcholine (muscarinic) A (Rhodopsin) Human - Nanobody-35 - VU6007678 pubchem gtoplig
acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		acetylcholine Small molecule - - 2025-08-13
Gq/11 αq Human Mini-GαsqiN: Gs backbone, Gq interface, Gi αN 59 β1 Rat γ2 Human Cryo-EM 9EK0 - 2.8 ACM5 CHRM5 M5 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - iperoxo pubchem gtoplig chembl_ligand
Small molecule Agonist acetylcholine Small molecule Burger WAC, Mobbs JI, Rana B, Wang J, Joshi K, Gentry PR, Yeasmin M, Venugopal H, Bender AM, Lindsley CW, Miao Y, Christopoulos A, Valant C, Thal DM 10.1038/S41467-025-62212-Z 2025-10-08
Gq/11 αq Human Mini-Gs/q/i: Gs scaffold, α5 Gq, N-term Gi2 59 β1 Human γ2 Human Cryo-EM 9GG5 - 3.3 TA2R TBXA2R TP Prostanoid A (Rhodopsin) Human - - - U46619 pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Agonist
PAM 		PGF2α, PGH2, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Krawinski P, Matzov D, Ryder A, Lal K, Karlov DS, Chalhoub G, Mulvaney EP, Kinsella BT, McCormick PJ, Caffrey M, Tikhonova IG, Shalev-Benami M 10.1038/S41467-026-69844-9 2025-08-27
Gq/11 αq Human Mini-Gαs/q: Gq α5, N-term(1-36) from Gαi2 58 β1 Human γ2 Human Cryo-EM 9GGG - 3.3 TA2R TBXA2R TP Prostanoid A (Rhodopsin) Human - - - I-BOP pubchem gtoplig chembl_ligand
Small molecule Agonist PGF2α, PGH2, PGE2, PGD2, PGI2, thromboxane A2 Small molecule - - 2025-08-27
Gs αs Human dnGs: N54S/A226G/A268E +5 more substitutions 56 β1 Human γ2 Human Cryo-EM 9GL2 - 3.2 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - Befiradol pubchem chembl_ligand pubchem
Phosphatidylinositol-4-phosphate
Small molecule
Small molecule 		Agonist
PAM 		5-hydroxytryptamine Small molecule Ullrich A, Schneider J, Braz JM, Neu E, Staffen N, Stanek M, Blahova J, Hove T, Albert T, Allikalt A, Lober S, Bhardwaj K, Rodriguez-Rosado S, Fink E, Rasmussen T, Hubner H, Inoue A, Shoichet BK, Basbaum AI, Bottcher B, Weikert D, Gmeiner P 10.1126/SCIADV.ADV9267 2025-07-02
Gi/o αgust Human miniGs/gust chimera w/ Gα-gust α5 helix 64 β1 Human γ2 Human Cryo-EM 9IIX - 2.9 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - - compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
Allosteric agonist 		- - - - 2024-07-24
Gs αs Bovine miniGs-iN: Gs core, Gi1 N-term, for scFv16 57 β1 Rat γ2 Bovine Cryo-EM 9IJD - 2.8 ADRB3 ADRB3 β3 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - (S)-carazolol pubchem drugbank
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline, (±)-adrenaline Small molecule Zheng S, Zhang S, Dai S, Chen K, Gao K, Sun X, Lin B, Liu X 10.1002/CPLU.202400288 2024-08-21
Gs αs Bovine MiniGsαiN: Gi1 N-term helix, for Nb35 binding 57 β1 Rat γ2 Bovine Cryo-EM 9IJE 9IJE_refined 2.3 ADRB3 ADRB3 β3 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline, (±)-adrenaline Small molecule Zheng S, Zhang S, Dai S, Chen K, Gao K, Sun X, Lin B, Liu X 10.1002/CPLU.202400288 2024-08-21
Gi/o αi1 Human Wild-type human Gi heterotrimer 64 β1 Human γ2 Human Cryo-EM 9IQT 9IQT_refined 2.9 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Liu Y, Zhou Z, Guan F, Han Z, Zhu C, Ye S, Yu X, Qiao A 10.1016/J.JMB.2024.168795 2024-10-02
Gs αs Human Human Gs, engineered for thermal stability 58 β1 Human γ2 Human Cryo-EM 9IV2 - 3.5 AGRD1 ADGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - - - dihydrotestosterone pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist dihydrotestosterone Small molecule Yang Z, Ping YQ, Wang MW, Zhang C, Zhou SH, Xi YT, Zhu KK, Ding W, Zhang QY, Song ZC, Zhao RJ, He ZL, Wang MX, Qi L, Ullmann C, Ricken A, Schoneberg T, Gan ZJ, Yu X, Xiao P, Yi F, Liebscher I, Sun JP 10.1016/J.CELL.2025.01.006 2025-02-12
Gq/11 αq Human Mini-Gαs/q71: Gs/Gq scaffold, Gαi1 N-term 60 β1 Human γ2 Human Cryo-EM 9IXX - 3.2 CLTR2 CYSLTR2 CysLT2 Leukotriene A (Rhodopsin) Human BRIL - NanoBiT (LargeBit/SmBiT) LTD4 pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank
Small molecule Agonist LTC4, LTE4, LTD4 Small molecule Jiang M, Xu Y, Luan X, Wu K, Li Z, Xu HE, Zhang S, Jiang Y, Yin W 10.1073/PNAS.2417148122 2025-04-02
Gi/o αi1 Human Gαi1 (4 DN muts); Gβ1 C-term HiBiT tag 64 β1 Human γ2 Human Cryo-EM 9IYB - 2.8 PD2R2 PTGDR2 DP2 Prostanoid A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		PGD2 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist PGF2α, Δ12-PGJ2, PGE2, PGD2, PGI2, PGD3, thromboxane A2 Small molecule - - 2024-12-04
Gq/11 αq Human mini-Gs scaffold w/ Gq α5 & interface res 57 β1 Human γ2 Mouse Cryo-EM 9IZG - 3.0 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human BRIL - LgBiT tag LPA pubchem
Lipid Agonist LPA Small molecule - - 2025-01-01
Gs αs Human Mini-Gs (mini-GasIN): αN from Gαi1, scFv16 60 β1 Human γ2 Human Cryo-EM 9J31 - 3.1 GPR4 gpr4 GPR4 Proton A (Rhodopsin) Zebrafish BRIL - LgBiT
HiBiT 		- None - - - Ma Y, Wang Y, Tang M, Weng Y, Chen Y, Xu Y, An S, Wu Y, Zhao S, Xu H, Li D, Liu M, Lu W, Ru H, Song G 10.1038/S41467-025-55901-2 2025-01-22
Gs αs Human mini-Gαs(teleost)+Gαi1 N-term; Gβ1-HiBiT 59 β1 Human γ2 Human Cryo-EM 9JCO - 2.4 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 - Lysophosphatidylcholine (LPC) pubchem
Small molecule PAM - - - - 2025-07-09
Gq/11 αq Human Gαq: N-term(1-18) from Gαi1, for stabilizer 62 β1 Human γ2 Human Cryo-EM 9JCP - 2.6 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 - Lysophosphatidylcholine (LPC) pubchem
Small molecule PAM - - - - 2025-07-09
Gq/11 αq Human gi2-miniGq: mini-Gαs + Gαi N-term + Gαq α5 helix 58 β1 Human γ2 Human Cryo-EM 9JFK - 3.2 UR2R UTS2R UT Urotensin A (Rhodopsin) Human BRIL Nanobody-35 - P5U
Peptide Agonist urotensin II-related peptide (Human), urotensin-II (Human) Peptide Gao T, You C, Cao Y, Xu X, Yuan Q, Shen S, Xu HE, Duan J 10.1016/J.JBC.2025.110794 2025-12-03
Gs αs Human MiniGαs399: 8 mutations, AHD→linker 59 β1 Human γ2 Human Cryo-EM 9JFT - 3.3 GPR65 GPR65 GPR65 Proton A (Rhodopsin) Human BRIL Nanobody-35 - - None - - - Yue X, Peng L, Liu S, Zhang B, Zhang X, Chang H, Pei Y, Li X, Liu J, Shui W, Wu L, Xu H, Liu ZJ, Hua T 10.1038/S41422-025-01092-W 2025-08-13
Gq/11 αq Human miniGs/q: miniGs backbone, Gq specificity 60 β1 Human γ2 Human Cryo-EM 9JFV - 2.7 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - - - - None - - - Yue X, Peng L, Liu S, Zhang B, Zhang X, Chang H, Pei Y, Li X, Liu J, Shui W, Wu L, Xu H, Liu ZJ, Hua T 10.1038/S41422-025-01092-W 2025-04-23
Gq/11 αq Human MiniGq(s/q71): Gs backbone, Gq α5, Gi1 N-term 57 β1 Rat γ2 Bovine Cryo-EM 9JR2 - 2.8 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - - - Parathyroid hormone
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide - - 2024-10-16
Gq/11 αq Human mGαsq: Gαi1 scaffold, ΔAHD, stabilizing muts 61 β1 Human γ2 Human Cryo-EM 9JH6 - 2.9 CLTR2 CYSLTR2 CysLT2 Leukotriene A (Rhodopsin) Human BRIL Nanobody-35 - Cer(d18:0/20:0) pubchem
Small molecule Agonist LTC4, LTE4, LTD4 Small molecule - - 2025-04-30
G12/13 α13 Human MiniG13: 7 stabilizing muts, AHD→linker 57 β1 Human γ2 Human Cryo-EM 9JHP - 3.4 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - - Endoglucanase H - None - - - Yue X, Peng L, Liu S, Zhang B, Zhang X, Chang H, Pei Y, Li X, Liu J, Shui W, Wu L, Xu H, Liu ZJ, Hua T 10.1038/S41422-025-01092-W 2025-04-23
Gq/11 αq Human Mini-Gsq: Gq on Gs scaffold, Gi1 N-term 61 β1 Human γ2 Human Cryo-EM 9JMC - 2.6 MTLR MLNR motilin Motilin A (Rhodopsin) Human BRIL - - DS-3801b free base pubchem gtoplig chembl_ligand
Small molecule Agonist motilin (Human) Protein - - 2025-05-28
Gq/11 αq Human mini-Gs: Gαi1 N-term (scFv16), Gαq α5 mimic 61 β1 Human γ2 Human Cryo-EM 9JMD - 2.7 MTLR MLNR motilin Motilin A (Rhodopsin) Human BRIL - - azithromycin pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist motilin (Human) Protein You C, Jiang M, Gao T, Zhu Z, He X, Xu Y, Gao Y, Jiang Y, Xu HE 10.1016/J.CELREP.2025.115329 2025-05-28
Gq/11 αq Human miniGq: miniGs+Gi1 N-term+Gq contact residues 57 β1 Rat γ2 Bovine Cryo-EM 9JR3 - 2.8 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - - - Parathyroid hormone
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide - - 2024-10-16
Gs αs Human modGαs: Gi1 N-term chimera; DN G226A/A366S 60 β1 Human γ2 Human Cryo-EM 9JVG - 2.8 GPR4 Gpr4 GPR4 Proton A (Rhodopsin) Mouse BRIL - - - None - - - Wen X, Shang P, Chen H, Guo L, Rong N, Jiang X, Li X, Liu J, Yang G, Zhang J, Zhu K, Meng Q, He X, Wang Z, Liu Z, Cheng H, Zheng Y, Zhang B, Pang J, Liu Z, Xiao P, Chen Y, Liu L, Luo F, Yu X, Yi F, Zhang P, Yang F, Deng C, Sun JP 10.1016/J.CELL.2024.12.001 2025-02-26
Gi/o αgust Human miniGs/gust chimera: Gs body + gustducin α5 helix 63 β1 Human γ2 Human Cryo-EM 9KPD - 2.8 T2R16 TAS2R16 TAS2R16 Taste 2 T2 (Taste 2) Human Sialidase NanA Nanobody-35 - salicin pubchem gtoplig
Small molecule Agonist - - Wang X, Zhou C, Ao W, Wu L, Wu Y, Xu W, Liu S, Tan Q, Wang L, Zhao F, Liu J, Pei Y, Zhao S, Hua T 10.1016/J.CELREP.2025.115604 2025-04-02
Gi/o αo Human Mini-Go: AHD deleted, N-term ScFv16 sequence 59 β1 Human γ2 Human Cryo-EM 9KZK - 3.5 C3AR C3ar1 C3a Complement peptide A (Rhodopsin) Mouse - - Muscarinic acetylcholine receptor M4 N-terminal region mouse C3a anaphylatoxin
Protein Agonist - - Mishra S, Yadav MK, Dalal A, Ganguly M, Yadav R, Sawada K, Tiwari D, Roy N, Banerjee N, Fung JN, Marallag J, Cui CS, Li XX, Lee JD, Dsouza CA, Saha S, Sarma P, Rawat G, Zhu H, Khant HA, Clark RJ, Sano FK, Banerjee R, Woodruff TM, Nureki O, Gati C, Shukla AK 10.1101/2025.05.26.656101 2025-11-26
Gi/o αi1 Human DNGαi: S47N/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 9L42 - 2.9 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human - - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule Chen A, Su C, Zhang Z, Zhang H 10.3390/PH18030292 2025-10-22
Gs αs Bovine Gs heterotrimer stabilized by NB35 53 β1 Rat γ2 Bovine Cryo-EM 9L84 - 3.2 ADRB1 ADRB1 β1 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - ATAZANAVIR chembl_ligand pubchem drugbank
(-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		(-)-noradrenaline, noradrenaline, (-)-adrenaline Small molecule He G, Sun Q, Xu X, Kong F, Zhang S, Ye K, Sun X, Lin B, Chen X, Yan C, Liu X 10.1016/J.CELL.2025.12.023 2025-12-31
Gs αs Bovine Gs heterotrimer: bovine Gα, rat Gβ, bovine Gγ 58 β1 Rat γ2 Bovine Cryo-EM 9L8L - 3.2 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - ATAZANAVIR chembl_ligand pubchem drugbank
CHEMBL1615159 chembl_ligand pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		(-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule He G, Sun Q, Xu X, Kong F, Zhang S, Ye K, Sun X, Lin B, Chen X, Yan C, Liu X 10.1016/J.CELL.2025.12.023 2025-12-31
Gs αolf Human Gα_olf chimera: N-term→Gαi1(1-18), scFv16 61 β1 Human γ2 Human Cryo-EM 9LDW - 2.6 O6C76 OR6C76 OR6C76 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human - - - alpha-Hexylcinnamaldehyde pubchem
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Agonist
PAM 		- - - - 2026-01-28
Gs αolf Human Mini-Gαolf/Gαi1 N-term chimera, scFv16 binding 61 β1 Human γ2 Human Cryo-EM 9LDX - 2.8 O6C76 OR6C76 OR6C76 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human - - - Benzophenone pubchem drugbank
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Agonist
PAM 		- - Wang T, Wu Y, Wang L, Li S, Zhao F, Wu L, Liu Y, Qin J, Tan Q, Liu J, Zeng L, Chen Y, Gao S, Shui W, Zhao S, Hua T, Liu ZJ 10.1016/J.CELL.2025.12.017 2026-01-28
Gs αs Human Mini-Gs: N-term (1-25) from Gαi1, for scFv16 60 β1 Human γ2 Human Cryo-EM 9LDZ - 3.2 O6C76 OR6C76 OR6C76 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human BRIL - - ethyl (2R,3S)-3-methyl-3-phenyl-oxirane-2-carboxylate pubchem
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Agonist
PAM 		- - - - 2026-01-28
Gs αolf Human Mini-Golf/Gαi1 chimera (N-term, AHD), scFv16 61 β1 Human γ2 Human Cryo-EM 9LE0 - 2.5 OR6A2 OR6A2 OR6A2 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human BRIL - - Octanal pubchem
Small molecule Agonist - - Wang T, Wu Y, Wang L, Li S, Zhao F, Wu L, Liu Y, Qin J, Tan Q, Liu J, Zeng L, Chen Y, Gao S, Shui W, Zhao S, Hua T, Liu ZJ 10.1016/J.CELL.2025.12.017 2026-01-28
Gq/11 αq Human modGαq: Gαi1 N-term segments, stability muts 60 β1 Human γ2 Human Cryo-EM 9LL9 - 2.8 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human b562RIL - LgBiT
HiBiT 		(R)-DOI pubchem gtoplig chembl_ligand
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule - - 2026-01-14
Gq/11 αq Human ModGαq chimera: Gαq/Gαi1/Gαs segments 60 β1 Human γ2 Human Cryo-EM 9LLA - 3.3 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human b562RIL - LgBiT Ariadne pubchem
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule - - 2026-01-14
Gq/11 αq Human modGαq: GNAQ + stabilizing GNAS2/GNAI1 segs 60 β1 Human γ2 Human Cryo-EM 9LLB - 3.0 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		DOI-NBOMe pubchem
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule - - 2026-01-14
Gs αs Human Gs heterotrimer, short Gαs isoform 57 β1 Human γ2 Human Cryo-EM 9LLJ - 2.6 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 LgBiT Agonist-positive allosteric GEM targeting TM5/6/7
dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
GEM targeting TM3/4/5
GEM targeting TM1/2/4
Protein
Small molecule
Protein
Protein 		Ago-PAM
Agonist
Unknown
Unknown 		5-hydroxytryptamine, noradrenaline, dopamine Small molecule - - 2026-03-04
Gq/11 αq Human Gs-mini-Gq chimera: Gs w/ Gq α5 (LQMNLREYNLV) 57 β1 Human γ2 Human Cryo-EM 9LRS - 2.8 MRGX4 MRGPRX4 MRGPRX4 Orphan A (Rhodopsin) Human BRIL - - PSB-18061 pubchem
Small molecule Agonist - - - - 2026-02-04
Gs αs Human miniGs: truncated/mutated Gs-short (P63092) 49 β1 Human γ2 Human Cryo-EM 9LWC - 2.9 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - (-)-adrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule - - 2026-02-18
Gq/11 αq Human mini-Gs/q71: Gαi1 N-term/AHD; G203A/A326S 57 β1 Rat γ2 Bovine Cryo-EM 9LWP - 2.9 BRS3 BRS3 BB3 Bombesin A (Rhodopsin) Human - - LgBiT
HiBiT 		- None - - - Li J, Li C, Zhou Q, Han W, Fang M, Xu Y, Mai Y, Zhang Y, Cui J, Xu HE, Zhang Y, Yin W, Wang MW 10.1016/J.APSB.2025.06.025 2025-07-16
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 9M0J - 2.9 BRS3 BRS3 BB3 Bombesin A (Rhodopsin) Human - Nanobody-35 - oridonin pubchem
Small molecule Agonist - - - - 2026-03-04
Gq/11 αq Human Gαq/Gαi1 chimera (miniGαs skeleton, N-term swap) 59 β1 Human γ2 Human Cryo-EM 9M1U - 2.6 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human BRIL Nanobody-35 - succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank
Small molecule Agonist α-ketoglutaric acid Small molecule None 10.1038/S44318-026-00823-Y 2026-06-17
Gq/11 αq Human Mini-Gs/q: Gs α with C-term Gq residues 62 β1 Human γ2 Human Cryo-EM 9M42 - 3.2 GP139 GPR139 GPR139 Orphan A (Rhodopsin) Human - Nanobody-35 Endo-1
4-beta-xylanase 		Compound 1.1(S) pubchem
Small molecule Agonist D-tryptophan, D-phenylalanine Small molecule - - 2026-01-21
Gi/o αi1 Bovine DN Gαi1: G203A/A326S; Gβ1-HiBiT, NanoBiT tether 64 β1 Rat γ2 Bovine Cryo-EM 9M54 - 3.2 NPFF2 NPFFR2 NPFF2 Neuropeptide FF/neuropeptide AF A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		Neuropeptide VF pubchem
Peptide Agonist QRFP43 (43RFa) (Human), neuropeptide AF (Rat), neuropeptide AF (Human), RFRP-3 (Human), neuropeptide SF (Human), PrRP-31 (Human), neuropeptide AF (Mouse), neuropeptide FF (Human), RFRP-1 (Human) Peptide Li X, Zhang H, Hu W, Wu K, Li S, Jin S, Yin Y, Yuan Q, Xu HE, Pan B, Jiang Y 10.1016/J.CELREP.2025.116160 2025-07-23
Gi/o αz Human Gα-Gγ fusion protein (GSAGSAGSA linker) 34 β1 Human γ2 Human Cryo-EM 9MD1 - 3.0 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - buspirone pubchem gtoplig chembl_ligand drugbank drug_central pubchem
PtdIns4P pubchem
Small molecule
Small molecule 		Agonist
PAM 		5-hydroxytryptamine Small molecule Warren AL, Zilberg G, Abbassi A, Abraham A, Yang S, Wacker D 10.1126/SCIADV.ADU9851 2025-08-13
Gs αs Human Gs heterotrimer 59 β1 Human γ2 Human Cryo-EM 9MXU - 2.5 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - Glucagon pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein - - 2026-04-22
Gi/o αi1 Human mGsI: Gαi1-based mini-G, stabilizes complex 59 β1 Rat γ2 Human Cryo-EM 9N29 - 2.6 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - Nanobody-35 - diphenhydramine pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank drugbank pubchem pubchem pubchem pubchem
Small molecule Agonist acetylcholine Small molecule Devenish SO, Patel SD, Ussingkaer LV, Almeida Silva LF, Goff O, Richardson A, Mobbs JI, Venugopal H, Thal DM, Kullmann DM 10.1038/S41392-026-02865-4 2026-07-15
Gi/o αgust Human MiniGs/gust: α5→gustducin(GNAT3), receptor fused 62 β1 Human γ2 Human Cryo-EM 9O38 - 3.0 TS1R2 TAS1R2 TAS1R2 Taste 1 C (Glutamate) Human - Nanobody-35 - - None - - - Juen Z, Lu Z, Yu R, Chang AN, Wang B, Fitzpatrick AWP, Zuker CS 10.1016/J.CELL.2025.04.021 2025-05-14
Gi/o αi1 Human Wild-type Gi1 heterotrimer 91 β1 Human γ2 Human Cryo-EM 9ODG - 4.3 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - - None - - - Robertson MJ, Modak A, Papasergi-Scott MM, Hu M, Peroto MC, Varga BR, Majumdar S, Kalathur R, Blanchard SC, Skiniotis G 10.1038/S41586-025-10056-4 2026-03-04
Gi/o αi1 Human WT Gi heterotrimer, no antibody fragments used 99 β1 Human γ2 Human Cryo-EM 9ODJ - 3.0 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - Mitragynine pseudoindoxyl
Small molecule Agonist (partial) - - Robertson MJ, Modak A, Papasergi-Scott MM, Hu M, Peroto MC, Varga BR, Majumdar S, Kalathur R, Blanchard SC, Skiniotis G 10.1038/S41586-025-10056-4 2026-01-07
Gi/o αgust Human DN gustducin (Gnat3) protein 63 β1 Human γ2 Human Cryo-EM 9OXB - 3.0 T2R43 TAS2R43 TAS2R43 Taste 2 T2 (Taste 2) Human BRIL - - aristolochic acid pubchem gtoplig chembl_ligand
Small molecule Agonist - - Kim Y, Gumpper RH, Zhuang Y, Dror RO, Roth BL 10.1038/S41594-026-01776-W 2026-04-22
Gi/o αi1 Human WT Gi1 heterotrimer, GTP-bound, closed AHD 97 β1 Human γ2 Human Cryo-EM 9P85 - 3.0 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gq/11 αq Human Mini-Gs/q v70: Gs backbone, Gq-mutated, ΔAHD 63 β1 Human γ2 Human Cryo-EM 9QXL - 3.1 AGRL4 ADGRL4 ADGRL4 ADGRL B2 (Adhesion) Human - - Green fluorescent protein - None - - - Chen Q, Gusach A, Diamante A, Patel JC, Edwards PC, Tate CG, Favara DM 10.1038/S41467-025-67629-0 2026-01-14
Gq/11 αq Human mini-Gαs: N-term from Gαi1, for scFv16 60 β1 Human γ2 Human Cryo-EM 9U4Y - 2.7 Q90WJ2 gnrhr.L GnRH1 Gonadotrophin-releasing hormone A (Rhodopsin) African clawed frog - - - CHEMBL266314 chembl_ligand pubchem pubchem drugbank pubchem chembl_ligand pubchem
Peptide Agonist - - Shen S, He X, Liu H, Hu W, Xu HE, Duan J 10.1073/PNAS.2500112122 2025-06-11
Gq/11 αq Human miniGq: truncated Gαq, a5 tail LQMNLREYNLV 59 β1 Human γ2 Human Cryo-EM 9UAM - 3.3 CLTR2 CYSLTR2 CysLT2 Leukotriene A (Rhodopsin) Human - - Oplophorus-luciferin 2-monooxygenase catalytic subunit
Beta-2 adrenergic receptor 		LTC4 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist LTC4, LTE4, LTD4 Small molecule - - 2026-03-18
Gq/11 αq Human miniGq: truncated/mutated Gαq, α5=Gnaq 59 β1 Human γ2 Human Cryo-EM 9UAN - 3.5 CLTR2 CYSLTR2 CysLT2 Leukotriene A (Rhodopsin) Human - - Beta-2 adrenergic receptor
Oplophorus-luciferin 2-monooxygenase catalytic subunit 		LTD4 pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank
Small molecule Agonist LTC4, LTE4, LTD4 Small molecule - - 2026-03-18
Gq/11 α11 Human Gna11 C-term α5 fragment (residues 335-359) 7 - - - - Cryo-EM 9UAP - 3.6 ACM1 CHRM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human - - De novo designed fusion protein - None - acetylcholine Small molecule Zhang X, Gao K, Nie J, Meng H, Sun X, Zhao J, Liu X 10.1073/PNAS.2508879122 2025-10-29
Gq/11 αq Human mini-Gs/Gq chimera: Gq C-term determinants 57 β1 Human γ2 Human Cryo-EM 9V81 - 2.6 MRGX4 MRGPRX4 MRGPRX4 Orphan A (Rhodopsin) Human BRIL - - HEP-50768 gtoplig pubchem
Small molecule Inverse agonist - - - - 2026-05-06
Gs αs Bovine mDN-Gαs: Gs/Gi1 chimera; Δloop +8 stab muts 60 β1 Human γ2 Human Cryo-EM 9UWM - 3.1 CALCR CALCR CT Calcitonin B1 (Secretin) Human - - - cagrilintide pubchem gtoplig drugbank
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Gu YM, Yuan QN, Li X, He Q, Xu HE, Zhao LH 10.1038/S41401-025-01635-2 2026-05-27
Gq/11 αq Human mini-Gαs/Gαq chimera; G203A/A326S muts 59 β1 Human γ2 Human Cryo-EM 9V0X - 2.7 PRLHR PRLHR PrRP Prolactin-releasing peptide A (Rhodopsin) Human - - - GUB08248
KUT [2-(2-[2-(2-[2-(Octadecandioyl-gamma-Glu)amino]ethoxy)ethoxy]acetylamino)ethoxy]ethoxy)acetyl] pubchem
Peptide
Small molecule 		Agonist PrRP-20 (Human), PrRP-20 (Rat), neuropeptide Y (Human), PTHrP (Human), PrRP-31 (Rat), PrRP-31 (Human) Peptide Li X, Li S, Shan H, Yuan QN, He XH, He Q, Zhang M, Li Y, Hu W, Wu K, Xu HE, Zhao LH 10.1038/S41401-025-01741-1 2026-02-04
Gi/o αi1 Human mini-Gαs+Gαi determinants; G203A/A326S 57 β1 Human γ2 Human Cryo-EM 9V1H - 2.9 NPFF2 NPFFR2 NPFF2 Neuropeptide FF/neuropeptide AF A (Rhodopsin) Human - - - GUB08248
Peptide Agonist QRFP43 (43RFa) (Human), neuropeptide AF (Rat), neuropeptide AF (Human), RFRP-3 (Human), neuropeptide SF (Human), PrRP-31 (Human), neuropeptide AF (Mouse), neuropeptide FF (Human), RFRP-1 (Human) Peptide Li X, Li S, Shan H, Yuan QN, He XH, He Q, Zhang M, Li Y, Hu W, Wu K, Xu HE, Zhao LH 10.1038/S41401-025-01741-1 2026-02-04
Gq/11 αq Human Gαq chimera: Gs skeleton+Gi1 N-term, scFv16/NB35 59 β1 Human γ2 Human Cryo-EM 9V2N - 2.6 GHSR GHSR ghrelin Ghrelin A (Rhodopsin) Human BRIL Nanobody-35 - macimorelin pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist [des-Gln14]ghrelin (Mouse), liver enriched antimicrobial peptide 2 (Human), ghrelin (Mouse), [des-Gln14]ghrelin (Human), ghrelin (Human) Peptide - - 2025-07-02
Gq/11 αq Human MiniGq50 construct 64 β1 Human γ2 Human Cryo-EM 8YN4 - 3.0 HRH2 HRH2 H2 Histamine A (Rhodopsin) Human - - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W 10.1038/S41467-024-52585-Y 2024-10-09
Gq/11 αq Human Gαq/i1 chimera: Gi1 backbone+Gq α5, DN muts 63 β1 Human γ2 Human Cryo-EM 8YYW - 3.2 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human - - - α-ketoglutaric acid pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist α-ketoglutaric acid Small molecule Liu A, Liu Y, Long Y, Ye RD 10.1038/S41467-025-67101-Z 2025-04-09
Gq/11 αq Human Gi1(1-326)+Gq tail(332-359); G203A/A326S 63 β1 Human γ2 Human Cryo-EM 8YYX - 2.8 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human - - - LTE4 pubchem gtoplig chembl_ligand
Small molecule Allosteric agonist α-ketoglutaric acid Small molecule - - 2025-04-09
Gq/11 αq Human Engineered Gαq (mini-Gq-like) construct 61 β1 Human γ2 Human Cryo-EM 8Z3M - 2.9 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - - - - None - - - - - 2025-04-23
Gs αs Human modGαs; α5 tail is Gs-family type 60 β1 Human γ2 Human Cryo-EM 8ZFA - 3.0 GPR4 gpr4 GPR4 Proton A (Rhodopsin) Western clawed frog BRIL - - - None - - - Wen X, Shang P, Chen H, Guo L, Rong N, Jiang X, Li X, Liu J, Yang G, Zhang J, Zhu K, Meng Q, He X, Wang Z, Liu Z, Cheng H, Zheng Y, Zhang B, Pang J, Liu Z, Xiao P, Chen Y, Liu L, Luo F, Yu X, Yi F, Zhang P, Yang F, Deng C, Sun JP 10.1016/J.CELL.2024.12.001 2025-02-26
Gq/11 αq Human Mini-Gs (mini-Gsqi): Gαi1 N-term, Gαq α5 helix 57 β1 Rat γ2 Bovine Cryo-EM 8ZH8 - 3.2 QRFPR QRFPR QRFP QRFP A (Rhodopsin) Human - Nanobody-35 - QRFP26
Peptide Agonist QRFP43 (43RFa) (Human), QRFP43 (Rat), QRFP26 (26RFa) (Human) Peptide Iwama A, Kise R, Akasaka H, Sano FK, Oshima HS, Inoue A, Shihoya W, Nureki O 10.1038/S41467-024-49030-5 2024-07-03
Gq/11 αq Human Mini-GαqiN: Gi2 scaffold, Gq α5 helix 60 β1 Human γ2 Human Cryo-EM 9AS2 - 3.2 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - dimethyltryptamine pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule - - 2025-04-02
Gq/11 αq Human mini-GαqiN: Gq scaffold, Gi2 N-term helix 60 β1 Human γ2 Human Cryo-EM 9AS4 - 3.1 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule Gumpper RH, Jain MK, Kim K, Sun R, Sun N, Xu Z, DiBerto JF, Krumm BE, Kapolka NJ, Kaniskan HU, Nichols DE, Jin J, Fay JF, Roth BL 10.1038/S41467-025-57956-7 2025-04-02
Gq/11 αq Human mini-GαqiN: Gi2 backbone, Gq specificity 59 β1 Human γ2 Human Cryo-EM 9AS6 - 3.1 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - mescaline pubchem gtoplig chembl_ligand
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule - - 2025-04-02
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 9AST 9AST_refined 3.1 XCR1 XCR1 XCR1 Chemokine A (Rhodopsin) Human - - LargeBit XCL1 CC3
Protein Agonist XCL1 (Rat), XCL2 (Human), XCL1 (Mouse), XCL1 (Human) Peptide Zhang X, Schlimgen RR, Singh S, Tomani MP, Volkman BF, Zhang C 10.1073/PNAS.2405732121 2024-12-11
Gs αs Human DNGs: dominant-negative Gs protein 60 β1 Human γ2 Human Cryo-EM 9AU0 - 2.5 PD2R PTGDR DP1 Prostanoid A (Rhodopsin) Human - Nanobody-35 - CHEMBL1591294 chembl_ligand pubchem pubchem
Small molecule Agonist PGF2α, PGE1, Δ12-PGJ2, PGE2, PGD2, PGI2, thromboxane A2 Small molecule - - 2025-08-27
Gi/o αi3 Human DN Gαi1: S47N/G203A/E245A/A326S 64 β2 Human γ2 Human Cryo-EM 9AVL - 3.8 CASR CASR CaS Calcium-sensing C (Glutamate) Human - - - CYCLOMETHYLTRYPTOPHAN pubchem
Calcium pubchem
tecalcet pubchem gtoplig chembl_ligand
Small molecule
Small molecule
Small molecule 		Agonist D-tryptophan, Mg2+, spermine, Ca2+ Small molecule - - 2024-04-17
Gq/11 αq Human mGsqi: Gs backbone, Gi1 C-term α5 57 β1 Human γ2 Human Cryo-EM 9BKJ - 2.6 CCKAR CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CCK-8 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
AMINO GROUP pubchem
Peptide
Small molecule 		Agonist gastrin-17 (Human), CCK-33 (Mouse), CCK-4 (Human), CCK-8 (Human), CCK-33 (Human), gastrin-17 (Rat), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Harikumar KG, Zhao P, Cary BP, Xu X, Desai AJ, Dong M, Mobbs JI, Toufaily C, Furness SGB, Christopoulos A, Belousoff MJ, Wootten D, Sexton PM, Miller LJ 10.1371/JOURNAL.PBIO.3002673 2024-05-22
Gq/11 αq Human mini-Gsqi: Gs w/ Gq-mimetic C-term mods 57 β1 Human γ2 Human Cryo-EM 9BKK - 2.5 CCKAR CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CCK-8 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Peptide Agonist gastrin-17 (Human), CCK-33 (Mouse), CCK-4 (Human), CCK-8 (Human), CCK-33 (Human), gastrin-17 (Rat), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Harikumar KG, Zhao P, Cary BP, Xu X, Desai AJ, Dong M, Mobbs JI, Toufaily C, Furness SGB, Christopoulos A, Belousoff MJ, Wootten D, Sexton PM, Miller LJ 10.1371/JOURNAL.PBIO.3002673 2024-05-22
Gs αs Human DNGs: dominant-negative Gs protein 59 β1 Human γ2 Human Cryo-EM 9BQ3 - 2.8 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP2 		- cagrilintide pubchem gtoplig drugbank
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide - - 2025-04-23
Gs αs Human DNGs: DN Gs for active complex stability 58 β1 Human γ2 Human Cryo-EM 9BUB - 2.3 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - cagrilintide pubchem gtoplig drugbank
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide - - 2025-04-23
Gi/o αi1 Rat Gαi1 with G203A dominant-negative mutation 60 β1 Bovine γ2 Bovine Cryo-EM 9CBM - 3.2 ADA2A ADRA2A α2A Adrenoceptors A (Rhodopsin) Human T4-Lysozyme - - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Lou JS, Su M, Wang J, Do HN, Miao Y, Huang XY 10.1038/S12276-024-01296-X 2024-09-11
Gq/11 αq Human mGαi/s/q: Gαi1 N-term, Gαq α5(345-359) 59 β1 Human γ2 Human Cryo-EM 9CLW - 3.2 FFAR2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - - LargeBit AMG7703 pubchem gtoplig chembl_ligand chembl_ligand pubchem
CHEMBL4176503 chembl_ligand pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		butyric acid, propanoic acid, trans-2-methylcrotonic acid, acetic acid Small molecule - - 2025-06-25
Gq/11 αq Human GqiN: Gq N-term(1-32)→Gi1(1-28), scFv16 59 β1 Human γ2 Human Cryo-EM 9D4Z - 2.7 PAR1 F2R PAR1 Proteinase-activated A (Rhodopsin) Human - - - - - - thrombin (Human), thrombin (Rat), thrombin (Mouse) Peptide Lyu Z, Lyu X, Malyutin AG, Xia G, Carney D, Alves VM, Falk M, Arora N, Zou H, McGrath AP, Kang Y 10.1038/S41467-025-59138-X 2025-05-07
Gq/11 αq Human mini-GαqiN: Gs template, Gq C-term 55 β1 Human γ2 Human Cryo-EM 9DQH 9DQH_refined 2.9 MRGRD MRGPRD MRGPRD Orphan A (Rhodopsin) Human BRIL - - EP-2825 pubchem
Small molecule Agonist β-alanine Small molecule - - 2024-12-11
Gq/11 αq Human MiniGq (miniGαqiN): Gs + Gi/q specificity 55 β1 Human γ2 Human Cryo-EM 9DQJ 9DQJ_refined 2.9 MRGRD MRGPRD MRGPRD Orphan A (Rhodopsin) Human BRIL - - EP-3945 pubchem
Small molecule Agonist β-alanine Small molecule - - 2024-12-11
Gi/o αo Human DN Gαo: S47N/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 9DYD - 3.0 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - (3aS,12bR)-asenapine pubchem
PtdIns4P pubchem
Small molecule
Small molecule 		Agonist (partial)
PAM 		5-hydroxytryptamine Small molecule - - 2025-08-13
Gi/o αi1 Human jsGiq: Gαi1 w/ spider Gαq1 tail, 3 muts 63 β1 Human γ2 Human Cryo-EM 9EPP - 4.1 B1B1U5 HaRh1 Rhodopsin Opsin (sight) A (Rhodopsin) Hasarius adansoni - - - 11,20-Ethanoretinal pubchem
Small molecule Agonist - - - - 2024-10-23
Gi/o αi1 Human jsGiq: human Gαi1 + spider Gαq1 muts, α5 replaced 65 β1 Human γ2 Human Cryo-EM 9EPQ - 4.2 B1B1U5 HaRh1 Rhodopsin Opsin (sight) A (Rhodopsin) Hasarius adansoni - - - 11,20-Ethanoretinal pubchem
Small molecule Agonist - - - - 2024-10-23
Gs αs Human Gαs: N-term replaced by Gαi (1-18) 58 β1 Human γ2 Human Cryo-EM 9GYO - 2.5 GPBAR GPBAR1 GPBA Bile acid A (Rhodopsin) Human BRIL Nanobody-35 - CHEMBL2331646 chembl_ligand pubchem
Small molecule Agonist lithocholic acid, deoxycholic acid, cholic acid, chenodeoxycholic acid Small molecule - - 2024-10-09
Gq/11 αq Human MiniGαs/q: Gs backbone, Gq α5, stabilizing muts 59 β1 Human γ2 Human Cryo-EM 9ITB - 2.9 LPAR6 LPAR6 LPA6 Lysophospholipid (LPA) A (Rhodopsin) Human BRIL Nanobody-35 LgBiT
HiBiT 		LPA pubchem
Lipid Agonist LPA Small molecule Duan Y, Xu Z, Hao B, Zhang A, Guo C, He Y 10.1073/PNAS.2415426122 2025-01-15
G12/13 α13 Human mini-G13: Gs+Gα13 α5 helix+Gαi1 N-term, scFv16 57 β1 Human γ2 Human Cryo-EM 9ITE - 3.1 LPAR6 LPAR6 LPA6 Lysophospholipid (LPA) A (Rhodopsin) Human BRIL - LgBiT LPA pubchem
Lipid Agonist LPA Small molecule Duan Y, Xu Z, Hao B, Zhang A, Guo C, He Y 10.1073/PNAS.2415426122 2025-01-15
Gi/o αi1 Bovine LPAR1-Gi1 fusion, scFv16, LgBiT/HiBiT tags 63 β1 Rat γ2 Human Cryo-EM 9J5V - 2.9 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - LgBiT
HiBiT 		CpY pubchem gtoplig
Small molecule Agonist LPA Small molecule - - 2024-11-27
Gq/11 αq Human Gi2-miniGq chimera: α5 tail from Gq/11 57 β1 Human γ2 Human Cryo-EM 9J87 - 2.8 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human - - - 5-MeOT pubchem gtoplig chembl_ligand
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule - - 2026-02-25
Gq/11 αq Human miniGs/q chimera: Gs body + Gq α5 helix 62 β1 Human γ2 Human Cryo-EM 9JCL - 2.8 P2RY1 P2RY1 P2Y1 P2Y A (Rhodopsin) Human - Nanobody-35 - ADP pubchem gtoplig chembl_ligand
Small molecule Agonist ADP, ATP Small molecule - - 2025-09-10
Gq/11 αq Human miniGs/q: miniGs backbone, Gq α5 mutations 61 β1 Human γ2 Human Cryo-EM 9JFX - 2.9 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 - - None - - - Yue X, Peng L, Liu S, Zhang B, Zhang X, Chang H, Pei Y, Li X, Liu J, Shui W, Wu L, Xu H, Liu ZJ, Hua T 10.1038/S41422-025-01092-W 2025-04-23
Gq/11 αq Human miniGs/q: Gq α5 helix; 7 stabilizing muts 61 β1 Human γ2 Human Cryo-EM 9JFZ - 2.9 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 - - None - - - Yue X, Peng L, Liu S, Zhang B, Zhang X, Chang H, Pei Y, Li X, Liu J, Shui W, Wu L, Xu H, Liu ZJ, Hua T 10.1038/S41422-025-01092-W 2025-04-23
Gq/11 αq Human mGαsq chimera; Gαi1-based scaffold 61 β1 Human γ2 Human Cryo-EM 9JH5 - 2.8 CLTR2 CYSLTR2 CysLT2 Leukotriene A (Rhodopsin) Human BRIL Nanobody-35 Endoglucanase H C16:0 ceramide pubchem
Small molecule Agonist LTC4, LTE4, LTD4 Small molecule Zhang S, Lin H, Wang J, Rui J, Wang T, Cai Z, Huang S, Gao Y, Ma T, Fan R, Dai R, Li Z, Jia Y, Chen Q, He H, Tan J, Zhu S, Gu R, Dong Z, Li M, Xie E, Fu Y, Zheng J, Jiang C, Sun J, Kong W 10.1038/S41586-025-08792-8 2025-04-23
Gq/11 αq Human mini-Gs/q71: Gαi N-term/AHD; G203A/A326S 55 β1 Rat γ2 Bovine Cryo-EM 9K07 - 2.8 BRS3 BRS3 BB3 Bombesin A (Rhodopsin) Human - Nanobody-35 LgBiT
HiBiT (Peptide 86 subunit) 		DSO-5a
Small molecule Agonist - - - - 2025-08-27
Gq/11 αq Human Mini-Gs/q: α5 from Gq, N-term Gi1 for NB 57 β1 Human γ2 Human Cryo-EM 9K0K - 3.1 P2RY4 P2RY4 P2Y4 P2Y A (Rhodopsin) Human - Nanobody-35 - UTP pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist UTP, ATP Small molecule Lan B, Zhang S, Chen K, Dai S, Fei J, Gao K, Sun X, Lin B, Liu X 10.1038/S41421-025-00797-X 2025-06-11
Gq/11 αq Human Mini-Gs/q: Gs backbone, Gq specificity res 57 β1 Human γ2 Human Cryo-EM 9K0X - 2.8 P2RY2 P2RY2 P2Y2 P2Y A (Rhodopsin) Human - Nanobody-35 - ATP pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist UTP, ATP Small molecule Lan B, Zhang S, Chen K, Dai S, Fei J, Gao K, Sun X, Lin B, Liu X 10.1038/S41421-025-00797-X 2025-06-11
Gi/o αi1 Human Engineered DN Gαi1: S47C/G202T +3 more muts 62 β1 Human γ2 Human Cryo-EM 9K1D - 3.3 FFAR2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - - - butyric acid pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem chembl_ligand pubchem
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Agonist
PAM 		butyric acid, propanoic acid, trans-2-methylcrotonic acid, acetic acid Small molecule Ke Y, Huang Y, Yi C, Ma L, Chu X, Wu B, Zhao Q, Han S 10.1016/J.CELREP.2024.115024 2024-12-11
Gq/11 αq Human Mini-Gs/q70 chimera, GTPase domain only 58 β1 Human γ2 Human Cryo-EM 9K25 - 3.3 P2RY2 P2RY2 P2Y2 P2Y A (Rhodopsin) Human - Nanobody-35 - - None - UTP, ATP Small molecule Lan B, Zhang S, Chen K, Dai S, Fei J, Gao K, Sun X, Lin B, Liu X 10.1038/S41421-025-00797-X 2025-06-11
Gi/o αgust Human Gαi1 chimera: α5 from gustducin (GNAT3) 64 β1 Human γ2 Human Cryo-EM 9KPE - 3.4 T2R16 TAS2R16 TAS2R16 Taste 2 T2 (Taste 2) Human - - NanA (exo-alpha-sialidase)
LgBiT 		salicin pubchem gtoplig
Small molecule Agonist - - Wang X, Zhou C, Ao W, Wu L, Wu Y, Xu W, Liu S, Tan Q, Wang L, Zhao F, Liu J, Pei Y, Zhao S, Hua T 10.1016/J.CELREP.2025.115604 2025-04-02
Gq/11 αq Human mini-GsqiN: Gαs+Gαi1 αN+Gαq α5(36 res) 59 β1 Human γ2 Human Cryo-EM 9L74 - 3.7 S1PR3 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - Nanobody-35 - d16:1 S1P pubchem
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid - - 2025-11-26
Gs αolf Human mini-Golf: N-term(1-27)→Gαi1(1-18), scFv16 61 β1 Human γ2 Human Cryo-EM 9LDV - 2.8 O6C76 OR6C76 OR6C76 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human BRIL - - ethyl (2R,3S)-3-methyl-3-phenyl-oxirane-2-carboxylate pubchem
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Agonist
PAM 		- - - - 2026-01-28
Gq/11 αq Human miniGαs w/ Gαi1 N-term & Gαq, for scFv16 59 β1 Human γ2 Human Cryo-EM 9M1S - 2.7 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human BRIL Nanobody-35 - Itaconic acid pubchem
Small molecule Agonist α-ketoglutaric acid Small molecule None 10.1038/S44318-026-00823-Y 2026-06-17
Gs αolf Human Mini-Gαolf: N-term from Gαi1 for scFv16 61 β1 Human γ2 Human Cryo-EM 9LE1 - 3.3 OR6A2 OR6A2 OR6A2 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human BRIL - - (E)-dec-2-enal pubchem
Small molecule Agonist - - - - 2026-01-28
Gs αolf Human Mini-Golf/Gαi1 N-term chimera, scFv16 binding 61 β1 Human γ2 Human Cryo-EM 9LE2 - 3.3 OR6A2 OR6A2 OR6A2 Olfactory family 6 O2 (Olfactory/extra-nasal 2) Human - - - (E)-dec-2-enal pubchem
Small molecule Agonist - - - - 2026-01-28
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 9LR1 - 2.5 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - JN241-9
Protein Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide - - 2026-02-04
Gs αs Human Gs α subunit, short isoform 59 β1 Human γ2 Human Cryo-EM 9M0X - 2.7 Q5QNQ1 taar13d taar13d Unclassified A (Rhodopsin) Zebrafish - Nanobody-35 - Agmatine pubchem drugbank
Agmatine pubchem drugbank
Small molecule
Small molecule 		Agonist
Unknown 		- - - - 2026-03-04
Gq/11 αq Human mini-Gαs w/ Gαi1 N-term, Gαq α5 helix 60 β1 Human γ2 Human Cryo-EM 9M1H - 2.6 PE2R1 PTGER1 EP1 Prostanoid A (Rhodopsin) Human BRIL - LgBiT PGE2 pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Meng X, Li Y, Xu J, Wu K, Hu W, Wu C, Xu HE, Xu Y 10.1073/PNAS.2423840122 2025-04-30
Gi/o αi1 Human mini-Gs/i chimera, Gi1-derived α5 tail 59 β1 Human γ2 Human Cryo-EM 9N09 - 2.6 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - Nanobody-35 - CHEMBL6164470 chembl_ligand pubchem
Small molecule Agonist acetylcholine Small molecule - - 2026-01-28
Gi/o αgust Human miniGs/gust25: Gs + gustducin α5, fused to TAS1R3 62 β1 Human γ2 Human Cryo-EM 9NOX - 3.0 TS1R2 TAS1R2 TAS1R2 Taste 1 C (Glutamate) Human - Nanobody-35 - - None - - - Juen Z, Lu Z, Yu R, Chang AN, Wang B, Fitzpatrick AWP, Zuker CS 10.1016/J.CELL.2025.04.021 2025-05-14
Gi/o αi1 Human Human Gαi1 subunit 63 β1 Human γ2 Human Cryo-EM 9PU5 - 3.5 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - DAMGO pubchem gtoplig chembl_ligand pubchem
BMS-986187 pubchem gtoplig chembl_ligand
Peptide
Small molecule 		Agonist
PAM 		[Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2026-05-27
Gi/o αi1 Human Human Gi1 heterotrimer 63 β1 Human γ2 Human Cryo-EM 9PUD - 3.0 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - DAMGO pubchem gtoplig chembl_ligand pubchem
Peptide Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2026-05-27
Gi/o αi1 Human - 99 β1 Human γ2 Human Cryo-EM 9PY2 - 3.2 OPRM OPRM1 μ Opioid A (Rhodopsin) Human b562RIL - - loperamide pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2025-11-12
Gq/11 αq Human Mini-Gαq: Gs scaffold, Gαi1 N-term, scFv16 61 β1 Human γ2 Human Cryo-EM 9U4W - 3.2 GNRHR GNRHR GnRH1 Gonadotrophin-releasing hormone A (Rhodopsin) Pig - - - CHEMBL266314 chembl_ligand pubchem pubchem drugbank pubchem chembl_ligand pubchem
Peptide Agonist - - Shen S, He X, Liu H, Hu W, Xu HE, Duan J 10.1073/PNAS.2500112122 2025-06-11
Gq/11 α11 Human Human Gα11 C-term α5 helix (residues 335-359) 7 - - - - Cryo-EM 9UCP - 2.9 ACM1 CHRM1 M1 Acetylcholine (muscarinic) A (Rhodopsin) Human - - De novo designed fusion protein iperoxo pubchem gtoplig chembl_ligand
Nanobody Nb1B4
Small molecule
Protein 		Agonist
Allosteric agonist 		acetylcholine Small molecule Zhang X, Gao K, Nie J, Meng H, Sun X, Zhao J, Liu X 10.1073/PNAS.2508879122 2025-10-29
Gq/11 αq Human Mini-Gq protein for complex stabilization 59 β1 Human γ2 Human Cryo-EM 9UK2 - 2.9 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human - - - - None - α-ketoglutaric acid Small molecule - - 2026-04-22
Gq/11 αq Rat Gq heterotrimer complex 61 β1 Rat γ2 Bovine Cryo-EM 9UST - 3.0 A0A9L0JPP9 - MRGPRE Orphan A (Rhodopsin) Donkey - - - (E)-3-(2-methoxyphenyl)prop-2-enal pubchem
Small molecule Agonist - - - - 2025-07-02
Gs αs Bovine mDN-Gs: Gs/Gi1 chimera, 8 stability muts, Δ254-263 60 β1 Human γ2 Human Cryo-EM 9UWQ - 3.1 CALCR CALCR CT Calcitonin B1 (Secretin) Human - RAMP1 - cagrilintide pubchem gtoplig drugbank
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Gu YM, Yuan QN, Li X, He Q, Xu HE, Zhao LH 10.1038/S41401-025-01635-2 2026-05-27
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 9UXU - 3.6 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - salvinorin A pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem chembl_ligand pubchem drugbank
Small molecule Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-05-27
Gq/11 αq Human Gαq chimera: mini-Gαs skeleton + Gi1 N-term 59 β1 Human γ2 Human Cryo-EM 9UY3 - 2.5 GHSR GHSR ghrelin Ghrelin A (Rhodopsin) Human BRIL Nanobody-35 LgBiT Anamorelin pubchem
Small molecule Agonist [des-Gln14]ghrelin (Mouse), liver enriched antimicrobial peptide 2 (Human), ghrelin (Mouse), [des-Gln14]ghrelin (Human), ghrelin (Human) Peptide - - 2025-07-02
Gq/11 αq Human ModGαq: Gs scaffold, Gq α5, Gi1 N-term(1-18) 61 β1 Human γ2 Human Cryo-EM 9VO2 - 2.7 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human BRIL - - - None - α-ketoglutaric acid Small molecule Xiao W, Zhu Y, Tang X, Zhu K, Zhang W, Chen M, Cai K, Xu S, Wu Z, Wang M, Liu J, Long L, Tan Z, Wu A, Zhou S, Zhao Z, Tang Y, Huang Y, Wang B, Liu F, Wang Q, Yang F, Jian D, Shi W, Xie H, Chen X, Guo L, Deng Z, Sun J, Li J 10.1016/J.CELL.2026.01.036 2026-03-18
Gi/o αi1 Human Gi heterotrimer complex 62 β1 Human γ2 Human Cryo-EM 9VPM - 4.0 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - - - - apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide - - 2026-07-08
Gq/11 αq Human Gq heterotrimer (Gαq/β1/γ2) 58 β1 Human γ2 Human Cryo-EM 9VUS - 2.4 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human BRIL - Maltose-binding protein (MBP) α-ketoglutaric acid pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist α-ketoglutaric acid Small molecule - - 2026-07-15
Gq/11 αq Human miniGs/q70: Gq α5 tail LQMNLREYNLV 52 β1 Human γ2 Human Cryo-EM 9W2G - 3.4 NK2R TACR2 NK2 Tachykinin A (Rhodopsin) Human - Nanobody-35 - EB1001
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide - - 2026-06-17
Gs αs Human MiniGαs: GTPase domain, truncated to 250 res 56 β1 Human γ2 Human Cryo-EM 9W45 - 3.2 Q7TRW7 Or1d2 OR1D2 Olfactory family 1 O2 (Olfactory/extra-nasal 2) Mouse - Nanobody-35 - Methyl cinnamate pubchem
Small molecule Agonist - - - - 2026-03-04
Gs αs Human mini-Gαs used for complex stabilization 55 β1 Human γ2 Human Cryo-EM 9WG4 - 3.3 O52E8 OR52E8 OR52E8 Olfactory family 52 O1 (Olfactory/extra-nasal 1) Human - Nanobody-35 - (3R)-3-Hydroxy-3-methylhexanoic acid pubchem
Small molecule Agonist - - - - 2026-06-17
Gq/11 αq Human mini-GsqiN: Gs + Gαi αN + Gαq C-term(36aa) 58 β1 Human γ2 Human Cryo-EM 9WP9 - 3.3 S1PR3 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - Nanobody-35 - sphingosine 1-phosphate pubchem gtoplig chembl_ligand
Lipid Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Yamauchi M, Im D, Maeda S, Ikuta T, Toyomoto M, Asada H, Sugita Y, Kishikawa JI, Noda T, Kato T, Inoue A, Iwata S, Hagiwara M 10.1073/PNAS.2507421122 2025-11-26
Gs αs Human Mini-Gs399, stabilizes active-state complex 56 β1 Human γ2 Human Cryo-EM 9WPM - 2.6 O5B21 OR5B21 OR5B21 Olfactory family 5 O2 (Olfactory/extra-nasal 2) Human - Nanobody-35 - - None - - - Han X, Zhang MH, Rong NK, Zhu KK, Pei Y, Ge XY, Liu Q, Lu H, Liu J, Zhang LJ, Bao HQ, Pi JH, Fan L, Fu Y, Shao XH, Yan WQ, Gao XH, Zhang MY, Guo LL, Lu Y, Ning SL, Zhang H, Xu YF, Feng XY, Cheng J, Xia M, Li Q, Yu X, Yang F, Sun JP 10.1016/J.CELL.2025.12.018 2026-01-28
Gq/11 αq Human Gi2-mini-Gq chimera for Gq-specific coupling 59 β1 Human γ2 Human Cryo-EM 9X22 - 2.9 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - [125I]GLP-1-(7-36)-amide pubchem gtoplig pubchem
Protein Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhou Q, Li J, Zhang Y, Cai X, Han W, Yang D, Wang MW 10.1016/J.APSB.2026.01.023 2026-03-25
Gi/o αi1 Human miniGαist: Gi/Gt chimera, Venus fusion 60 β1 Human γ2 Human Cryo-EM 9YDA - 2.9 OPSG OPN1MW OPN1MW Opsin (sight) A (Rhodopsin) Human - - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Yao W, Fay JF, Farrens DL 10.1073/PNAS.2516318122 2025-12-24
Gi/o αi1 Human mGsi: mini-Gs w/ Gi C-term α5 helix 59 β1 Human γ2 Human Cryo-EM 9YDP - 2.0 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - Nanobody-35 - DADLE pubchem gtoplig chembl_ligand drugbank pubchem
Peptide Agonist [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Mobbs JI, Nguyen MD, Deo O, Bartuzi D, Venugopal H, Alvi S, Pham V, Barnes N, Christopoulos A, Poole DP, Carbone SE, Jorg M, Capuano B, Carlsson J, Gondin AB, Scammells PJ, Valant C, Thal DM 10.1101/2025.10.16.682975 2025-12-10
Gi/o αi1 Human Human native wild-type Gαi1 62 β1 Human γ2 Human Cryo-EM 20ZD - 2.8 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Wild-type human Gi1 heterotrimer subunits 62 β1 Human γ2 Human Cryo-EM 20ZG - 2.4 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human WT human Gi1 heterotrimer (native, non-chimeric) 62 β1 Human γ2 Human Cryo-EM 20ZH - 2.4 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human - 64 β1 Mouse γ2 Bovine Cryo-EM 22EM - 2.9 OPRK OPRK1 κ Opioid A (Rhodopsin) Human BRIL - - beta01
Peptide Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-05-06
Gi/o αi1 Human - 64 β1 Rat γ2 Bovine Cryo-EM 22ES - 2.4 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - difelikefalin pubchem gtoplig chembl_ligand drugbank pubchem
Peptide Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-05-06
Gi/o αi1 Human Gαi1-Gγ2 fusion (linker); Gβ1-HiBiT tag 63 β1 Bovine γ2 Bovine Cryo-EM 24XZ - 2.9 P2Y14 P2RY14 P2Y14 P2Y A (Rhodopsin) Human BRIL - LgBiT tag
GFP 		UDP pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist UDP, UDP-galactose, UDP-glucose, UDP N-acetyl-glucosamine, UDP-glucuronic acid Small molecule None 10.1016/J.BBRC.2026.153976 2026-06-10
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 25NV - 3.2 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - SPT
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide - - 2026-06-03
Gs αs Human DNGs: dominant-negative Gs protein 60 β1 Human γ2 Human Cryo-EM 25NX - 2.9 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Peptide 2 (PTHrP analogue)
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Kim TW, Gerrard EJ, Shin J, Gardella TJ, Wootten D, Sexton PM, Cary BP, Gellman SH 10.1021/JACS.6C02192 2026-06-03
Gs αs Human Gs α5 tail sequence (QRMHLRQYELL), GNAS 60 β1 Rat γ2 Bovine Cryo-EM 27XK - 2.6 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Glucagon-like peptide 1(7-36) pubchem
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein - - 2026-07-01
Gq/11 αq Human Gαq chimera: Gαi1 N-term, C3S mut, scFv16 62 β1 Human γ2 Human Cryo-EM 9VAW - 2.2 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Wild-type human Gαi1 65 β1 Human γ2 Human Cryo-EM 9VB6 - 3.4 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi3 Human DN Gi3: S47N/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 9VJ6 - 2.6 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - NLX-101 pubchem gtoplig chembl_ligand
Small molecule Agonist 5-hydroxytryptamine Small molecule - - 2025-11-12
Gs αs Human Human Gs-short heterotrimer, no chimera 58 β1 Human γ2 Human Cryo-EM 9VMG - 2.8 A0A678XLR1 - A0A678XLR1 Orphan A (Rhodopsin) Sea lamprey - Nanobody-35 - spermine pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist - - Jiang K, Zeng L, Zhang W, He X, Zheng Y, Wang L, Zhang Z, Pu J, Deng C, Yang F, Zhao S, Xu F 10.1038/S41421-025-00839-4 2026-05-13
Gq/11 αq Human modGαq: Gs scaffold, Gq α5 helix, Gαi1 N-term 61 β1 Human γ2 Human Cryo-EM 9VMN - 2.6 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human BRIL - - α-ketoglutaric acid pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist α-ketoglutaric acid Small molecule Xiao W, Zhu Y, Tang X, Zhu K, Zhang W, Chen M, Cai K, Xu S, Wu Z, Wang M, Liu J, Long L, Tan Z, Wu A, Zhou S, Zhao Z, Tang Y, Huang Y, Wang B, Liu F, Wang Q, Yang F, Jian D, Shi W, Xie H, Chen X, Guo L, Deng Z, Sun J, Li J 10.1016/J.CELL.2026.01.036 2026-03-18
Gq/11 αq Human ModGαq: Gs scaffold, Gq α5, Gi1 N-term 61 β1 Human γ2 Human Cryo-EM 9VMO - 2.4 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human BRIL - - Itaconic acid pubchem
Small molecule Agonist α-ketoglutaric acid Small molecule Xiao W, Zhu Y, Tang X, Zhu K, Zhang W, Chen M, Cai K, Xu S, Wu Z, Wang M, Liu J, Long L, Tan Z, Wu A, Zhou S, Zhao Z, Tang Y, Huang Y, Wang B, Liu F, Wang Q, Yang F, Jian D, Shi W, Xie H, Chen X, Guo L, Deng Z, Sun J, Li J 10.1016/J.CELL.2026.01.036 2026-03-18
Gq/11 αq Human modGαq: miniGs scaffold, Gq α5, Gi1 N-term 60 β1 Human γ2 Human Cryo-EM 9VMP - 2.5 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human BRIL - - A-1 pubchem
Small molecule Agonist α-ketoglutaric acid Small molecule - - 2026-03-18
Gq/11 αq Human Human Gq heterotrimer 61 β1 Human γ2 Human Cryo-EM 9VV6 - 2.6 OXGR1 OXGR1 oxoglutarate Oxoglutarate A (Rhodopsin) Human BRIL - Maltose/maltodextrin-binding periplasmic protein Itaconic acid pubchem
Small molecule Agonist α-ketoglutaric acid Small molecule - - 2026-07-15
Gq/11 αq Human miniGs/q70: Gs C-term replaced w/ Gq residues 52 β1 Human γ2 Human Cryo-EM 9W1J - 3.0 NK2R TACR2 NK2 Tachykinin A (Rhodopsin) Human - Nanobody-35 - neurokinin A (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide - - 2026-06-17
Gq/11 αq Human mini-Gs/q70: Gq α5(LQMNLREYNLV) for coupling 52 β1 Human γ2 Human Cryo-EM 9W2H - 3.1 NK2R TACR2 NK2 Tachykinin A (Rhodopsin) Human - Nanobody-35 - EB1002 pubchem
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide - - 2026-06-17
Gq/11 αq Human miniGs/q70: mini-Gs + Gq α5 helix (LQMNLREYNLV) 52 β1 Human γ2 Human Cryo-EM 9W2I - 2.9 NK2R TACR2 NK2 Tachykinin A (Rhodopsin) Human - Nanobody-35 - Peptide 336 (P336) spinning GLU-LYS-TYR-VAL-GLY-MLE-NLE-NH2
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide - - 2026-06-17
Gq/11 αq Human miniGs/q70: Gs α5 helix → Gq (LQMNLREYNLV) 52 β1 Human γ2 Human Cryo-EM 9W2J - 2.8 NK2R TACR2 NK2 Tachykinin A (Rhodopsin) Human - Nanobody-35 - Peptide 383 (P383)
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide - - 2026-06-17
Gi/o αi1 Human mini-Gs/i143: N-term/AH from Gαi1, scFv16 56 β1 Human γ2 Human Cryo-EM 9X40 - 3.1 MAS MAS1 MAS1 Orphan A (Rhodopsin) Human - - - AR234958 pubchem
Small molecule Agonist - - - - 2026-05-20
Gs αs Human DN Gs: 9 muts incl S54N/G226A/A366S 57 β1 Human γ2 Human Cryo-EM 9WEY - 3.3 UL33 UL33 UL33 Unclassified A (Rhodopsin) strain AD169 - Nanobody-35 LgBiT
HiBiT 		- - - - - Drzazga AK, Suzuki S, Wouters C, Faas F, Nishikawa K, Kamegawa A, Fujiyoshi Y, Rosenkilde MM, Tsutsumi N 10.1038/S42003-026-09660-5 2026-02-25
Gq/11 αq Human MiniGq, stabilizes active-state complex 60 β1 Human γ2 Human Cryo-EM 9WQL - 3.2 GRM5 GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human - - - L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
CDPPB pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		L-glutamic acid Small molecule Lu Y, Wen T, Lu X, Zhang G, Meng T, Liu T, Wang X, Shen Y, Yang X 10.1126/SCIADV.AEE0044 2026-05-27
Gi/o αi1 Human mini-Gs/i143: N-term+αH from Gαi1, scFv16 57 β1 Human γ2 Human Cryo-EM 9X3Z - 2.5 MAS MAS1 MAS1 Orphan A (Rhodopsin) Human - - - neuropeptide FF (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist - - Zhang Y, Wang Q, Liu H, Shan H, Gu Y, Yang J, Gao Y, Wu K, Yang D, Xu HE 10.1038/S44318-026-00764-6 2026-04-15
Gi/o αi1 Human Native human Gi heterotrimer 64 β1 Human γ2 Human Cryo-EM 9WQM - 3.3 GRM1 GRM1 mGlu1 Metabotropic glutamate C (Glutamate) Human - - - L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
Ro0711401 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		L-glutamic acid Small molecule - - 2026-05-27
Gq/11 αq Human MiniGq construct 60 β1 Human γ2 Human Cryo-EM 9WQN - 3.7 GRM1 GRM1 mGlu1 Metabotropic glutamate C (Glutamate) Human - - - L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
Ro0711401 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		L-glutamic acid Small molecule - - 2026-05-27
Gi/o αi1 Bovine DN Gαi1: S47N/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 9XC6 - 3.0 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - BMS-986187 pubchem gtoplig chembl_ligand
(-)-methadone pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		[Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2026-07-08
Gi/o αi1 Bovine DN Gi: S47N/G203A/E245A/A326S mutations 64 β1 Human γ2 Human Cryo-EM 9XDR - 2.6 OPRK OPRK1 κ Opioid A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		BMS-986187 pubchem gtoplig chembl_ligand
asimadoline pubchem gtoplig chembl_ligand drugbank
Small molecule
Small molecule 		Ago-PAM
Agonist 		[Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-07-08
Gi/o αi2 Human DN Gαi2: S47N/G204A/E246A/A327S; Gβ1-HiBiT 63 β1 Human γ2 Human Cryo-EM 9XF4 - 3.1 OPRD OPRD1 δ Opioid A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		BMS-986187 pubchem gtoplig chembl_ligand
[Leu]enkephalin (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot pubchem
Small molecule
Peptide 		Ago-PAM
Agonist 		[Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-07-08
Gi/o αi1 Human Gi Gγ-Gα fusion, DN muts S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 9XHH - 3.0 CCR7 CCR7 CCR7 Chemokine A (Rhodopsin) Human - - LgBiT
HiBiT 		C-C motif chemokine 19
Protein Agonist CCL21 (Human), CCL19 (Human) Peptide Tanaka K, Nishikawa K, Shiimura Y, Fujiyoshi Y, Tsutsumi N 10.1073/PNAS.2533975123 2026-04-22
Gi/o αi1 Human Gγ2/Gαi1 fusion, DN muts; Gβ-HiBiT tag 62 β1 Human γ2 Human Cryo-EM 9XHI - 3.2 CCR7 CCR7 CCR7 Chemokine A (Rhodopsin) Human - - LgBiT
HiBiT 		C-C motif chemokine 21
Protein Agonist CCL21 (Human), CCL19 (Human) Peptide Tanaka K, Nishikawa K, Shiimura Y, Fujiyoshi Y, Tsutsumi N 10.1073/PNAS.2533975123 2026-04-22
Gq/11 αq Human mini-Gαs: Gαi1 N-term + Gαq C-term(348-359) 60 β1 Human γ2 Human Cryo-EM 9XQC - 3.0 GPR75 GPR75 GPR75 Orphan A (Rhodopsin) Human - - NbALFA
Maltose-binding protein
LgBiT 		- None - CCL5 (Human) Peptide Zhu ZN, You CZ, Yuan QN, Xu JY, Gu ZY, Huang Z, Liu M, Shan B, Wang JJ, Hu W, Wang K, Yin WC, Xu YW, Xu HE, Wu CR 10.1038/S41401-025-01720-6 2026-02-04
Gi/o αi1 Human mini-Gsi: Gs + Gi1 α5 helix, sep. chain 59 β1 Human γ2 Human Cryo-EM 9YDQ - 1.9 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - Nanobody-35 - DADLE pubchem gtoplig chembl_ligand drugbank pubchem
MIPS3614 pubchem
Peptide
Small molecule 		Agonist
PAM 		[Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2025-12-10
Gi/o αi1 Human mGsi: Gi α5 specificity; only α5 modeled 59 β1 Human γ2 Human Cryo-EM 9YDR - 2.1 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - Nanobody-35 - DADLE pubchem gtoplig chembl_ligand drugbank pubchem
MIPS3983
Peptide
Small molecule 		Agonist
PAM 		[Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2025-12-10
Gi/o αi1 Human miniGist: mini-Gs + transducin α5 helix (GαCT) 60 β1 Human γ2 Human Cryo-EM 9YGZ - 3.0 OPSG OPN1MW OPN1MW Opsin (sight) A (Rhodopsin) Human - - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Yao W, Fay JF, Farrens DL 10.1016/J.BPJ.2026.03.029 2026-05-20
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S; Gβ1 His-tag 62 β1 Human γ2 Human Cryo-EM 12IZ - 2.7 CNR2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - - - '5249 pubchem
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule - - 2026-07-15
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 12JA - 2.9 CNR2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - - - '1029
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule - - 2026-07-15
Gi/o αi1 Human Gi heterotrimer complex 63 β1 Human γ2 Human Cryo-EM 20YC - 3.4 GP174 GPR174 GPR174 Orphan A (Rhodopsin) Human - - - - None - lysophosphatidylserine Lipid - - 2026-04-15
Gi/o αi1 Human WT human Gi1; Gβ has accidental T159I mutation 62 β1 Human γ2 Human Cryo-EM 20ZC - 2.6 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Native human Gi1 heterotrimer, nucleotide-free NC1 62 β1 Human γ2 Human Cryo-EM 20ZI - 2.7 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Native human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 20ZJ - 2.9 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Nucleotide-free NC3 state, Gβ N-term 6xHis tag 62 β1 Human γ2 Human Cryo-EM 20ZK - 2.7 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 20ZL - 3.1 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αo Human MiniGαoA fused to Gγ2 for expression 59 β1 Human γ2 Human Cryo-EM 21AG - 3.1 5HT1F HTR1F 5-HT1F 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - LY334370 pubchem gtoplig chembl_ligand
Small molecule Agonist 5-hydroxytryptamine Small molecule - - 2026-04-08
Gi/o αi1 Human DN Gαi1 mutant 63 β1 Human γ2 Human Cryo-EM 23IV - 2.4 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - LZD503 pubchem
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule - - 2026-05-20
Gi/o αi1 Human DN Gαi1: muts for stability, low GDP affinity 63 β1 Human γ2 Human Cryo-EM 23IW - 2.4 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - LZD503 pubchem
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule - - 2026-05-20
Gi/o αi1 Human - 62 β1 Rat γ2 Bovine Cryo-EM 23OI - 2.7 OPRX OPRL1 NOP Opioid A (Rhodopsin) Human - - - cebranopadol pubchem gtoplig chembl_ligand chembl_ligand chembl_ligand drugbank pubchem
Small molecule Agonist nociceptin/orphanin FQ (Human) Peptide - - 2026-07-01
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 24QH - 2.7 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - - None - linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule - - 2026-07-08
Gs αs Human Gs-short heterotrimer 57 β1 Rat γ2 Bovine Cryo-EM 24TB - 3.0 GHRHR GHRHR GHRH Glucagon B1 (Secretin) Human - - - - None - GHRH (Mouse), GHRH (Rat), GHRH (Human) Peptide Wang MW, Hang K, Qiu Y, Chen X, Chen Y, Huang S, Cong Z, Zhou Q 10.1093/PROCEL/PWAG016 2026-07-08
Gs αs Human Engineered Gs protein heterotrimer 58 β1 Rat γ2 Bovine Cryo-EM 24TI - 2.9 GHRHR GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 - PCO371 pubchem gtoplig chembl_ligand drugbank
Small molecule Allosteric agonist GHRH (Mouse), GHRH (Rat), GHRH (Human) Peptide Wang MW, Hang K, Qiu Y, Chen X, Chen Y, Huang S, Cong Z, Zhou Q 10.1093/PROCEL/PWAG016 2026-07-08
Gq/11 αq Human Gq heterotrimer (Gαq/β1/γ2) 0 β1 Human γ2 Human Cryo-EM 24XB - 2.7 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - - None - linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule - - 2026-07-08
Gs αs Bovine Gαs/Gαi1 chimera: G226A/A366S DN muts 57 β1 Bovine γ2 Bovine Cryo-EM 7D68 - 3.0 GLP2R GLP2R GLP-2 Glucagon B1 (Secretin) Human - Nanobody-35 LgBiT
HiBiT 		glucagon-like peptide 2 (Human) pubchem gtoplig uniprot pubchem
Protein Agonist glucagon-like peptide 2 (Mouse), glucagon-like peptide 2-(3-33) (Mouse), glucagon-like peptide 2-(3-33) (Human), glucagon-like peptide 2 (Human) Protein Sun W, Chen LN, Zhou Q, Zhao LH, Yang D, Zhang H, Cong Z, Shen DD, Zhao F, Zhou F, Cai X, Chen Y, Zhou Y, Gadgaard S, van der Velden WJC, Zhao S, Jiang Y, Rosenkilde MM, Xu HE, Zhang Y, Wang MW 10.1038/S41422-020-00442-0 2020-12-16
Gs αs Human Mini-Gs: truncated Gs GTPase domain, 8 muts 50 - - - - X-ray 5G53 5G53_refined 3.4 AA2AR ADORA2A A2A Adenosine A (Rhodopsin) Human - - - NECA pubchem gtoplig chembl_ligand
Small molecule Agonist adenosine Small molecule Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG 10.1038/NATURE18966 2016-08-03
Gi/o αo Human MiniGαo1: ΔH-domain, GPS mut H248A/T250A 61 β1 Human γ2 Human Cryo-EM 7D76 - 3.1 AGRG3 ADGRG3 ADGRG3 ADGRG B2 (Adhesion) Human - - - beclomethasone pubchem
Small molecule Agonist - - Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP 10.1038/S41586-020-03083-W 2021-02-03
Gi/o αo Human Human Gαo1 (miniGαo), ΔAHD, C351 palmitoylated 61 β1 Human γ2 Human Cryo-EM 7D77 - 2.9 AGRG3 ADGRG3 ADGRG3 ADGRG B2 (Adhesion) Human - - - cortisol pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist - - Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H, Qu C, Shen Q, Tian C, Li ZJ, Li S, Wang GY, Tao X, Wen X, Zhong YN, Yang J, Yi F, Yu X, Xu HE, Zhang Y, Sun JP 10.1038/S41586-020-03083-W 2021-02-03
Gi/o αi1 Human WT Gi heterotrimer, apyrase-induced apo state 61 β1 Human γ2 Human Cryo-EM 6DDE - 3.5 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - DAMGO pubchem gtoplig chembl_ligand pubchem
Peptide Agonist - - Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13
Gs αs Human Gs: human Gαs-short, rat Gβ1, bovine Gγ2 59 β1 Rat γ2 Bovine Cryo-EM 5VAI - 4.1 G1SGD4 GLP1R GLP-1 Glucagon B1 (Secretin) Rabbit - Nanobody-35 - glucagon-like peptide 1-(7-37) (Human) pubchem gtoplig uniprot uniprot uniprot chembl_ligand pubchem
Peptide Agonist - - Zhang Y, Sun B, Feng D, Hu H, Chu M, Qu Q, Tarrasch JT, Li S, Sun Kobilka T, Kobilka BK, Skiniotis G 10.1038/NATURE22394 2017-05-24
Gs αs Human DN Gs: S54N/G226A/E268A + Gi2 substitutions 49 β1 Human γ2 Human Cryo-EM 6B3J - 3.3 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Exendin-P5
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, Christopoulos A, Sexton PM, Wootten D 10.1038/NATURE25773 2018-02-21
Gi/o αi2 Human DN Gαi2: S47N/G204A/A327S/E246A 59 β1 Human γ2 Human Cryo-EM 6D9H 6D9H_refined 3.6 AA1R ADORA1 A1 Adenosine A (Rhodopsin) Human - - Muscarinic acetylcholine receptor M4 N-terminus adenosine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist adenosine Small molecule Draper-Joyce CJ, Khoshouei M, Thal DM, Liang YL, Nguyen ATN, Furness SGB, Venugopal H, Baltos JA, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, Christopoulos A 10.1038/S41586-018-0236-6 2018-06-20
Gs αs Human DNGs: DN Gs for signaling complex stability 48 β1 Human γ2 Human Cryo-EM 6E3Y 6E3Y_refined 3.3 CALRL CALCRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- calcitonin gene-related peptide 1 uniprot
Peptide Agonist - - Liang YL, Khoshouei M, Deganutti G, Glukhova A, Koole C, Peat TS, Radjainia M, Plitzko JM, Baumeister W, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Wootten D, Sexton PM 10.1038/S41586-018-0535-Y 2018-09-19
Gi/o αi1 Human Nucleotide-free Gi complex, WT human Gαi 61 β1 Human γ2 Human Cryo-EM 6DDF - 3.5 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - DAMGO pubchem gtoplig chembl_ligand pubchem
Peptide Agonist - - Koehl A, Hu H, Maeda S, Zhang Y, Qu Q, Paggi JM, Latorraca NR, Hilger D, Dawson R, Matile H, Schertler GFX, Granier S, Weis WI, Dror RO, Manglik A, Skiniotis G, Kobilka BK 10.1038/S41586-018-0219-7 2018-06-13
Gi/o αi1 Human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 6KPG 6KPG_refined 3.0 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human BRIL - - AM841 pubchem gtoplig chembl_ligand
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ 10.1016/J.CELL.2020.01.008 2020-02-12
Gi/o αo Human GoA heterotrimer: human Gα, mouse Gβ1, Gγ2 60 β1 Mouse γ2 Human Cryo-EM 6K41 - 2.9 ADA2B ADRA2B α2B Adrenoceptors A (Rhodopsin) Human T4-Lysozyme - - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Yuan D, Liu Z, Kaindl J, Maeda S, Zhao J, Sun X, Xu J, Gmeiner P, Wang HW, Kobilka BK 10.1038/S41589-020-0492-2 2020-04-15
Gi/o αi1 Human Native human Gi heterotrimer 62 β1 Human γ2 Human Cryo-EM 6KPF 6KPF_refined 2.9 CNR2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human BRIL - - AM12033 pubchem
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Hua T, Li X, Wu L, Iliopoulos-Tsoutsouvas C, Wang Y, Wu M, Shen L, Brust CA, Nikas SP, Song F, Song X, Yuan S, Sun Q, Wu Y, Jiang S, Grim TW, Benchama O, Stahl EL, Zvonok N, Zhao S, Bohn LM, Makriyannis A, Liu ZJ 10.1016/J.CELL.2020.01.008 2020-02-12
Gi/o αo Human Mini-Go: truncated GTPase domain of Gαo 51 - - - - X-ray 6FUF 6FUF_refined 3.1 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Tsai CJ, Pamula F, Nehme R, Muhle J, Weinert T, Flock T, Nogly P, Edwards PC, Carpenter B, Gruhl T, Ma P, Deupi X, Standfuss J, Tate CG, Schertler GFX 10.1126/SCIADV.AAT7052 2018-10-03
Gi/o αo Human Mini-Go heterotrimer w/ Gβ1γ2, α-core only 59 β1 Human γ2 Human Cryo-EM 6G79 - 3.8 5HT1B HTR1B 5-HT1B 5-Hydroxytryptamine A (Rhodopsin) Human - - - donitriptan pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist 5-HT-moduline, tryptamine, 5-hydroxytryptamine Small molecule Garcia-Nafria J, Nehme R, Edwards PC, Tate CG 10.1038/S41586-018-0241-9 2018-06-20
Gs αs Human Mini-Gs: 8 muts + 3 deletions incl AHD 57 β1 Human γ2 Human Cryo-EM 6GDG 6GDG_refined 4.1 AA2AR ADORA2A A2A Adenosine A (Rhodopsin) Human Thioredoxin (TrxA) Nanobody-35 - NECA pubchem gtoplig chembl_ligand
Small molecule Agonist adenosine Small molecule Garcia-Nafria J, Lee Y, Bai X, Carpenter B, Tate CG 10.7554/ELIFE.35946 2018-05-16
Gi/o αi1 Human Gi heterotrimer complex 65 β1 Human γ2 Human Cryo-EM 6LFM 6LFM_refined 3.5 CXCR2 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - - - Interleukin-8
Protein Agonist CXCL5 (Rat), CXCL5 (Mouse), CXCL1 (Rat), CXCL7 (Human), CXCL1 (Mouse), CXCL2 (Mouse), CXCL3 (Human), CXCL2 (Human), CXCL5 (Human), CXCL6 (Human), CXCL2 (Rat), CXCL3 (Rat), CXCL3 (Mouse), CXCL1 (Human), CXCL8 (Human) Peptide Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ 10.1038/S41586-020-2492-5 2020-09-02
Gi/o αi1 Human Gi1 heterotrimer 65 β1 Human γ2 Human Cryo-EM 6LFO 6LFO_refined 3.4 CXCR2 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - - - Interleukin-8
Protein Agonist CXCL5 (Rat), CXCL5 (Mouse), CXCL1 (Rat), CXCL7 (Human), CXCL1 (Mouse), CXCL2 (Mouse), CXCL3 (Human), CXCL2 (Human), CXCL5 (Human), CXCL6 (Human), CXCL2 (Rat), CXCL3 (Rat), CXCL3 (Mouse), CXCL1 (Human), CXCL8 (Human) Peptide Liu K, Wu L, Yuan S, Wu M, Xu Y, Sun Q, Li S, Zhao S, Hua T, Liu ZJ 10.1038/S41586-020-2492-5 2020-09-02
Gi/o αi1 Human Human Gi1 heterotrimer 63 β1 Human γ2 Human Cryo-EM 6LML 6LML_refined 3.9 GLR GCGR glucagon Glucagon B1 (Secretin) Human - - - Glucagon pubchem
Small molecule Agonist glucagon (Human) Protein Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B 10.1126/SCIENCE.AAZ5346 2020-04-01
Gs αs Human Mini-Gs: truncated Gαs for stability 61 β1 Human γ2 Human Cryo-EM 6LI3 - 3.3 GPR52 GPR52 GPR52 Orphan A (Rhodopsin) Human - Nanobody-35 - - None - - - Lin X, Li M, Wang N, Wu Y, Luo Z, Guo S, Han GW, Li S, Yue Y, Wei X, Xie X, Chen Y, Zhao S, Wu J, Lei M, Xu F 10.1038/S41586-020-2019-0 2020-02-26
Gs αs Human Native human Gs heterotrimer 59 β1 Human γ2 Human Cryo-EM 6LMK 6LMK_refined 3.7 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Glucagon pubchem
Small molecule Agonist glucagon (Human) Protein Qiao A, Han S, Li X, Li Z, Zhao P, Dai A, Chang R, Tai L, Tan Q, Chu X, Ma L, Thorsen TS, Reedtz-Runge S, Yang D, Wang MW, Sexton PM, Wootten D, Sun F, Zhao Q, Wu B 10.1126/SCIENCE.AAZ5346 2020-04-01
Gs αs Human Mini-Gs protein 57 β1 Rat γ2 Bovine Cryo-EM 6LPB 6LPB_refined 3.9 PACR ADCYAP1R1 PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP-38 pubchem
Peptide Agonist PHV (Rat), VIP (Human), PHV (Human), PHM (Human), PHI (Mouse), PACAP-38 (Human), PACAP-27 (Human) Protein Kobayashi K, Shihoya W, Nishizawa T, Kadji FMN, Aoki J, Inoue A, Nureki O 10.1038/S41594-020-0386-8 2020-03-11
Gs αs Human DN Gs: 8 muts S54N/G226A/E268A...I285T 55 β1 Human γ2 Human Cryo-EM 6M1H - 3.6 PACR ADCYAP1R1 PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - maxadilan gtoplig uniprot pubchem
Peptide Agonist PHV (Rat), VIP (Human), PHV (Human), PHM (Human), PHI (Mouse), PACAP-38 (Human), PACAP-27 (Human) Protein Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y 10.1038/S41422-020-0280-2 2020-03-11
Gs αs Human DNGs: 8 muts S54N/G226A/E268A...I285T 57 β1 Human γ2 Human Cryo-EM 6M1I - 3.5 PACR ADCYAP1R1 PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP-38 pubchem
Peptide Agonist PHV (Rat), VIP (Human), PHV (Human), PHM (Human), PHI (Mouse), PACAP-38 (Human), PACAP-27 (Human) Protein Wang J, Song X, Zhang D, Chen X, Li X, Sun Y, Li C, Song Y, Ding Y, Ren R, Harrington EH, Hu LA, Zhong W, Xu C, Huang X, Wang HW, Ma Y 10.1038/S41422-020-0280-2 2020-03-11
Gi/o αi1 Human Wild-type human Gi heterotrimer 62 β1 Human γ2 Human Cryo-EM 6N4B 6N4B_refined 3.0 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - MDMB-Fubinaca pubchem gtoplig
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Krishna Kumar K, Shalev-Benami M, Robertson MJ, Hu H, Banister SD, Hollingsworth SA, Latorraca NR, Kato HE, Hilger D, Maeda S, Weis WI, Farrens DL, Dror RO, Malhotra SV, Kobilka BK, Skiniotis G 10.1016/J.CELL.2018.11.040 2019-01-30
Gs αs Human Gs heterotrimer complex 43 β1 Human γ2 Human Cryo-EM 6NIY - 3.3 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - CALCITONIN SALMON chembl_ligand drug_central pubchem pubchem
Protein Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Dal Maso E, Glukhova A, Zhu Y, Garcia-Nafria J, Tate CG, Atanasio S, Reynolds CA, Ramirez-Aportela E, Carazo JM, Hick CA, Furness SGB, Hay DL, Liang YL, Miller LJ, Christopoulos A, Wang MW, Wootten D, Sexton PM 10.1021/ACSPTSCI.8B00056 2019-01-23
Gs αs Human Human Gs heterotrimer 59 β1 Human γ2 Human Cryo-EM 6NI3 6NI3_refined 3.8 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human T4-Lysozyme Nanobody-35 - CHEMBL1615159 chembl_ligand pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Nguyen AH, Thomsen ARB, Cahill TJ 3rd, Huang R, Huang LY, Marcink T, Clarke OB, Heissel S, Masoudi A, Ben-Hail D, Samaan F, Dandey VP, Tan YZ, Hong C, Mahoney JP, Triest S, Little J 4th, Chen X, Sunahara R, Steyaert J, Molina H, Yu Z, des Georges A, Lefkowitz RJ 10.1038/S41594-019-0330-Y 2019-11-20
Gi/o αi1 Human Nucleotide-free human Gi1, canonical C state, WT 62 β1 Human γ2 Human Cryo-EM 6OS9 6OS9_refined 3.0 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10
Gs αs Human DN Gs: S54N/G226A/E268A +5 Gi2 substitutions 49 β1 Human γ2 Human Cryo-EM 6P9Y - 3.0 PACR ADCYAP1R1 PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP-38 pubchem
Peptide Agonist PHV (Rat), VIP (Human), PHV (Human), PHM (Human), PHI (Mouse), PACAP-38 (Human), PACAP-27 (Human) Protein Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.01.012 2020-02-05
Gs αs Human DN Gs: muts alter nucleotide handling 49 β1 Human γ2 Human Cryo-EM 6ORV 6ORV_refined 3.0 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHEMBL3950796 chembl_ligand pubchem
Small molecule Allosteric agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, Miller LJ, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/s41586-019-1902-z 2020-01-08
Gi/o αi1 Human Wild-type human G protein heterotrimer 62 β1 Human γ2 Human Cryo-EM 6OSA - 3.0 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kato HE, Zhang Y, Hu H, Suomivuori CM, Kadji FMN, Aoki J, Krishna Kumar K, Fonseca R, Hilger D, Huang W, Latorraca NR, Inoue A, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41586-019-1337-6 2019-07-10
Gs αs Human GsDN: Gαs+Gαi1 chimera for Nb35 binding 58 β1 Human γ2 Human Cryo-EM 6PB1 6PB1_refined 2.8 CRHR2 CRHR2 CRF2 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - CHEMBL427807 chembl_ligand pubchem
Cholesterol pubchem drugbank
Protein
Small molecule 		Agonist
PAM 		urocortin 2 (Rat), urocortin 3 (Human), corticotrophin-releasing hormone (Human), urocortin 2 (Human), urocortin 1 (Human), urocortin 1 (Mouse) Peptide Ma S, Shen Q, Zhao LH, Mao C, Zhou XE, Shen DD, de Waal PW, Bi P, Li C, Jiang Y, Wang MW, Sexton PM, Wootten D, Melcher K, Zhang Y, Xu HE 10.1016/J.MOLCEL.2020.01.013 2020-02-12
Gi/o αi1 Human DN Gαi1: S47N/G204A/E246A/A327S 100 β1 Human γ2 Human Cryo-EM 6OT0 - 3.9 SMO SMO SMO Oxysterol F (Frizzled) Human - - - 24(S),25-Epoxycholesterol pubchem
Lipid Agonist - - Qi X, Liu H, Thompson B, McDonald J, Zhang C, Li X 10.1038/S41586-019-1286-0 2019-06-12
Gs αs Human DN Gαs: S54N/G226A/E268A +Gi2-like subs 49 β1 Human γ2 Human Cryo-EM 6P9X - 2.9 CRHR1 CRHR1 CRF1 Corticotropin-releasing factor B1 (Secretin) Human - Nanobody-35 - corticorelin drug_central pubchem
Protein Agonist corticotrophin-releasing hormone (Human), urocortin 1 (Human), urocortin 1 (Mouse), urocortin 2 (Human) Peptide Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.01.012 2020-02-05
Gi/o αo Human GoAiN: αN helix muts (Gi1-like), for scFv16 61 β1 Human γ2 Human Cryo-EM 6OIK 6OIK_refined 3.6 ACM2 CHRM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - iperoxo pubchem gtoplig chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		acetylcholine Small molecule Maeda S, Qu Q, Robertson MJ, Skiniotis G, Kobilka BK 10.1126/SCIENCE.AAW5188 2019-05-08
Gi/o αi1 Human DN Gαi1 (G203A/A326S); bovine/rat subunits 61 β1 Human γ2 Human Cryo-EM 6OMM 6OMM_refined 3.2 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - - - WKYMVM pubchem
Small molecule Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide Zhuang Y, Liu H, Edward Zhou X, Kumar Verma R, de Waal PW, Jang W, Xu TH, Wang L, Meng X, Zhao G, Kang Y, Melcher K, Fan H, Lambert NA, Eric Xu H, Zhang C 10.1038/S41467-020-14728-9 2020-02-26
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 100 β1 Human γ2 Human Cryo-EM 6PT0 6PT0_refined 3.2 CNR2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - - - WIN55212-2 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Xing C, Zhuang Y, Xu TH, Feng Z, Zhou XE, Chen M, Wang L, Meng X, Xue Y, Wang J, Liu H, McGuire TF, Zhao G, Melcher K, Zhang C, Xu HE, Xie XQ 10.1016/J.CELL.2020.01.007 2020-02-12
Gs αs Human DN Gs: 8 muts; C-term HiBiT fusion 61 β1 Human γ2 Human Cryo-EM 6VN7 6VN7_refined 3.2 VIPR1 VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 LgBiT
HiBiT 		PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Protein Agonist VIP (Human), GHRH (Rat), secretin (Rat), PHM (Human), GHRH (Mouse), PHI (Mouse), PACAP-38 (Human), secretin (Mouse), GHRH (Human), secretin (Pig), PACAP-27 (Human) Protein Duan J, Shen DD, Zhou XE, Bi P, Liu QF, Tan YX, Zhuang YW, Zhang HB, Xu PY, Huang SJ, Ma SS, He XH, Melcher K, Zhang Y, Xu HE, Jiang Y 10.1038/S41467-020-17933-8 2020-09-02
Gs αs Human DNGs: mutations incl A366S 48 β1 Human γ2 Human Cryo-EM 6UVA - 2.3 CALRL CALCRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- ADM2 (Adrenomedullin 2 / Intermedin)
Peptide Agonist - - Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-04-01
Gs αs Human Gs heterotrimer 57 β1 Human γ2 Human Cryo-EM 6VCB - 3.3 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - glucagon-like peptide 1-(7-37) (Human) pubchem gtoplig uniprot uniprot uniprot chembl_ligand pubchem
CHEMBL5197819 chembl_ligand pubchem
Peptide
Small molecule 		Agonist
PAM 		glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Bueno AB, Sun B, Willard FS, Feng D, Ho JD, Wainscott DB, Showalter AD, Vieth M, Chen Q, Stutsman C, Chau B, Ficorilli J, Agejas FJ, Cumming GR, Jimenez A, Rojo I, Kobilka TS, Kobilka BK, Sloop KW 10.1038/S41589-020-0589-7 2020-07-22
Gs αs Human Human DN Gs (DNGs) 58 β1 Human γ2 Human Cryo-EM 7CX3 - 2.8 PE2R2 PTGER2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - taprenepag pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05
Gs αs Human DNGs: dominant-negative Gs protein 48 β1 Human γ2 Human Cryo-EM 6UUN 6UUN_refined 3.0 CALRL CALCRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP2 		- adrenomedullin uniprot pubchem
Peptide Agonist - - Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-03-25
Gs αs Human DN Gs (DNGs): A366S mutation 48 β1 Human γ2 Human Cryo-EM 6UUS 6UUS_refined 2.4 CALRL CALCRL calcitonin-like Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- ADM pubchem
Peptide Agonist - - Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM 10.1021/ACSPTSCI.9B00080 2020-04-01
Gs αs Human DN Gs: 8 mutations for stabilization 56 β1 Human γ2 Human Cryo-EM 6WHC 6WHC_refined 3.4 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 15 (P15)
Peptide Agonist glucagon (Human) Protein Chang R, Zhang X, Qiao A, Dai A, Belousoff MJ, Tan Q, Shao L, Zhong L, Lin G, Liang YL, Ma L, Han S, Yang D, Danev R, Wang MW, Wootten D, Wu B, Sexton PM 10.1074/JBC.RA120.013793 2020-05-27
Gs αs Human Human Gαs short splice variant 56 β1 Human γ2 Human Cryo-EM 6WPW 6WPW_refined 3.1 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Glucagon derivative ZP3780
Peptide Agonist glucagon (Human) Protein Hilger D, Kumar KK, Hu H, Pedersen MF, O'Brien ES, Giehm L, Jennings C, Eskici G, Inoue A, Lerch M, Mathiesen JM, Skiniotis G, Kobilka BK 10.1126/SCIENCE.ABA3373 2020-08-12
Gs αs Human DNGαsv2: A366S mutation 49 β1 Human γ2 Human Cryo-EM 6WI9 6WI9_refined 4.3 SCTR SCTR secretin Glucagon B1 (Secretin) Human - Nanobody-35 - SECRETIN chembl_ligand drug_central pubchem pubchem drugbank
Protein Agonist secretin (Mouse), secretin (Pig), VIP (Human) Protein Dong M, Deganutti G, Piper SJ, Liang YL, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ 10.1038/S41467-020-17791-4 2020-08-12
Gi/o αo Human MiniGo construct 59 β1 Rat γ2 Human Cryo-EM 6WWZ 6WWZ_refined 3.3 CCR6 CCR6 CCR6 Chemokine A (Rhodopsin) Human BRIL - - CCL20
Protein Agonist CCL20 (Mouse), CCL20 (Human), CCL20 (Rat), beta-defensin 4A (Human) Peptide Wasilko DJ, Johnson ZL, Ammirati M, Che Y, Griffor MC, Han S, Wu H 10.1038/S41467-020-16820-6 2020-06-24
Gs αs Human DNGasv2: A366S mutation 61 β1 Human γ2 Human Cryo-EM 6WZG 6WZG_refined 2.3 SCTR SCTR secretin Glucagon B1 (Secretin) Human - Nanobody-35 - SECRETIN chembl_ligand drug_central pubchem pubchem drugbank
Protein Agonist secretin (Mouse), secretin (Pig), VIP (Human) Protein Dong M, Deganutti G, Piper SJ, Liang YL, Khoshouei M, Belousoff MJ, Harikumar KG, Reynolds CA, Glukhova A, Furness SGB, Christopoulos A, Danev R, Wootten D, Sexton PM, Miller LJ 10.1038/S41467-020-17791-4 2020-08-12
Gs αs Human DNGas: DN Gs stabilizing complex 90 β1 Human γ2 Human Cryo-EM 6X18 - 2.1 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - GLP-1(7-36)NH2 pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.09.020 2020-09-09
Gs αs Human DN Gαs (DNGαs) with stabilizing mutations 89 β1 Human γ2 Human Cryo-EM 6X19 - 2.1 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - CHU-128 pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.09.020 2020-09-09
Gs αs Human DNGas: DN Gs muts for stability 89 β1 Human γ2 Human Cryo-EM 6X1A - 2.5 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - danuglipron pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Senel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, Miller LJ, Reedtz-Runge S, Langmead CJ, Gloriam DE, Danev R, Sexton PM, Wootten D 10.1016/J.MOLCEL.2020.09.020 2020-09-09
Gi/o αi1 Human Human Gi heterotrimer 61 β1 Human γ2 Human Cryo-EM 6XBJ - 3.9 SMO SMO SMO Oxysterol F (Frizzled) Human - - - Cholesterol pubchem drugbank
Small molecule Agonist - - Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30
Gi/o αi1 Human Wild-type human Gi heterotrimer 61 β1 Human γ2 Human Cryo-EM 6XBK - 3.2 SMO SMO SMO Oxysterol F (Frizzled) Human - - - Cholesterol pubchem drugbank
Small molecule Agonist - - Qi X, Friedberg L, De Bose-Boyd R, Long T, Li X 10.1038/S41589-020-0646-2 2020-09-30
Gs αs Human Gs-iN: αN helix replaced by Gαi1 (1-31) 59 β1 Human γ2 Human Cryo-EM 7AUE 7AUE_refined 3.0 MC4R MC4R MC4 Melanocortin A (Rhodopsin) Human - - - setmelanotide pubchem gtoplig drug_central drugbank
Calcium pubchem
Peptide
Small molecule 		Agonist
Cofactor 		ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M 10.1126/SCIENCE.ABF7958 2021-04-28
Gs αs Human Physiological human Gs heterotrimer 54 β1 Human γ2 Human Cryo-EM 7BB6 - 4.2 V2R AVPR2 V2 Vasopressin and oxytocin A (Rhodopsin) Human - Nanobody-35 - vasopressin (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem pubchem
Peptide Agonist vasopressin (Human), oxytocin (Human) Peptide Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B 10.1126/SCIADV.ABG5628 2021-06-02
Gs αs Human Physiological Gs short isoform, non-chimeric 55 β1 Human γ2 Human Cryo-EM 7BB7 - 4.4 V2R AVPR2 V2 Vasopressin and oxytocin A (Rhodopsin) Human - Nanobody-35 - vasopressin (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem pubchem
Peptide Agonist vasopressin (Human), oxytocin (Human) Peptide Bous J, Orcel H, Floquet N, Leyrat C, Lai-Kee-Him J, Gaibelet G, Ancelin A, Saint-Paul J, Trapani S, Louet M, Sounier R, Demene H, Granier S, Bron P, Mouillac B 10.1126/SCIADV.ABG5628 2021-06-02
Gs αs Human Human Gαs-short w/ bovine Gβ1/Gγ2 50 β1 Bovine γ2 Bovine Cryo-EM 7BZ2 7BZ2_refined 3.8 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - ARFORMOTEROL chembl_ligand pubchem drugbank drug_central pubchem drugbank
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Zhang Y, Yang F, Ling S, Lv P, Zhou Y, Fang W, Sun W, Zhang L, Shi P, Tian C 10.1038/S41421-020-0176-9 2020-08-05
Gs αs Human DNGs: dominant-negative Gs protein 60 β1 Human γ2 Human Cryo-EM 7CKW 7CKW_refined 3.2 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - fenoldopam pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand pubchem gtoplig pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z 10.1016/J.CELL.2021.01.028 2021-03-03
Gs αs Human DNGas: DN Gs short isoform (Gnas2) 60 β1 Human γ2 Human Cryo-EM 7CKX - 3.5 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - A77636 pubchem gtoplig chembl_ligand
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z 10.1016/J.CELL.2021.01.028 2021-03-03
Gi/o αi1 Human DN Gαi1: S47N/G203A/E345A/A326S 64 β1 Human γ2 Human Cryo-EM 7CMU - 3.0 DRD3 DRD3 D3 Dopamine A (Rhodopsin) Human BRIL - - pramipexole pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist dopamine Small molecule Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE 10.1016/J.MOLCEL.2021.01.003 2021-03-10
Gs αs Human Gα alpha-helical domain (AHD) not modeled 49 β1 Human γ2 Human Cryo-EM 7C2E - 4.2 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - RGT1383 pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Ma H, Huang W, Wang X, Zhao L, Jiang Y, Liu F, Guo W, Sun X, Zhong W, Yuan D, Xu HE 10.1038/S41422-020-0384-8 2020-08-26
Gs αs Human DN Gs protein, e.g. G226A mutation 60 β1 Human γ2 Human Cryo-EM 7CKY - 3.2 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL3697578 chembl_ligand pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z 10.1016/J.CELL.2021.01.028 2021-03-03
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 7CX2 - 2.8 PE2R2 PTGER2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 7CX4 7CX4_refined 2.9 PE2R2 PTGER2 EP2 Prostanoid A (Rhodopsin) Human - Nanobody-35 - evatanepag pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Qu C, Mao C, Xiao P, Shen Q, Zhong YN, Yang F, Shen DD, Tao X, Zhang H, Yan X, Zhao RJ, He J, Guan Y, Zhang C, Hou G, Zhang PJ, Hou G, Li Z, Yu X, Chai RJ, Guan YF, Sun JP, Zhang Y 10.1126/SCIADV.ABF1268 2021-05-05
Gs αs Human Mini-Gs: AHD reverted, but not resolved 58 β1 Rat γ2 Bovine Cryo-EM 7D3S 7D3S_refined 2.9 SCTR SCTR secretin Glucagon B1 (Secretin) Human - Nanobody-35 - SECRETIN chembl_ligand drug_central pubchem pubchem drugbank
Protein Agonist secretin (Mouse), secretin (Pig), VIP (Human) Protein Fukuhara S, Kobayashi K, Kusakizako T, Iida W, Kato M, Shihoya W, Nureki O 10.1016/J.BBRC.2020.08.042 2020-11-04
Gi/o αi1 Human WT: human Gαi1, rat Gβ1, bovine Gγ2 62 β1 Rat γ2 Bovine Cryo-EM 7DB6 7DB6_refined 3.3 MTR1A MTNR1A MT1 Melatonin A (Rhodopsin) Human - - - ramelteon pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist melatonin Small molecule Okamoto HH, Miyauchi H, Inoue A, Raimondi F, Tsujimoto H, Kusakizako T, Shihoya W, Yamashita K, Suno R, Nomura N, Kobayashi T, Iwata S, Nishizawa T, Nureki O 10.1038/S41594-021-00634-1 2021-08-18
Gi/o αi1 Human DN Gαi1: S47N/G203A/E345A/A326S 64 β1 Human γ2 Human Cryo-EM 7CMV - 2.7 DRD3 DRD3 D3 Dopamine A (Rhodopsin) Human BRIL - - CHEMBL70565 chembl_ligand pubchem
Small molecule Agonist dopamine Small molecule Xu P, Huang S, Mao C, Krumm BE, Zhou XE, Tan Y, Huang XP, Liu Y, Shen DD, Jiang Y, Yu X, Jiang H, Melcher K, Roth BL, Cheng X, Zhang Y, Xu HE 10.1016/J.MOLCEL.2021.01.003 2021-03-10
Gs αs Human DNGs: dominant-negative Gs protein 60 β1 Human γ2 Human Cryo-EM 7CRH 7CRH_refined 3.3 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - SKF-83959 pubchem gtoplig chembl_ligand chembl_ligand pubchem pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Xiao P, Yan W, Gou L, Zhong YN, Kong L, Wu C, Wen X, Yuan Y, Cao S, Qu C, Yang X, Yang CC, Xia A, Hu Z, Zhang Q, He YH, Zhang DL, Zhang C, Hou GH, Liu H, Zhu L, Fu P, Yang S, Rosenbaum DM, Sun JP, Du Y, Zhang L, Yu X, Shao Z 10.1016/J.CELL.2021.01.028 2021-03-03
Gs αs Human Mini-Gs399 stabilizing construct 58 β1 Human γ2 Human Cryo-EM 7D7M 7D7M_refined 3.3 PE2R4 PTGER4 EP4 Prostanoid A (Rhodopsin) Human - Nanobody-35 - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Nojima S, Fujita Y, Kimura KT, Nomura N, Suno R, Morimoto K, Yamamoto M, Noda T, Iwata S, Shigematsu H, Kobayashi T 10.1016/J.STR.2020.11.007 2020-11-18
Gi/o αi1 Human DN human Gαi1 protein 62 β1 Human γ2 Human Cryo-EM 7S8M - 2.5 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human BRIL - - CORTISTATIN-14 chembl_ligand pubchem
Peptide Agonist PAMP-20 (Human) Peptide Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gs αs Human DN human Gs: 8 stabilizing mutations 60 β1 Rat γ2 Bovine Cryo-EM 7DUR - 3.3 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Compound 2 pubchem
Small molecule Ago-PAM glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-021-24058-Z 2021-08-11
Gs αs Human Gs heterotrimer; human Gαs-short, bovine β/γ 55 β1 Bovine γ2 Bovine Cryo-EM 7DHI - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - levosalbutamol pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist (partial) (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Yang F, Ling S, Zhou Y, Zhang Y, Lv P, Liu S, Fang W, Sun W, Hu LA, Zhang L, Shi P, Tian C 10.1093/NSR/NWAA284 2020-12-16
Gs αs Human Human Gαs-short, bovine Gβ1/Gγ2, no muts 49 β1 Bovine γ2 Bovine Cryo-EM 7DHR 7DHR_refined 3.8 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - LEVISOPRENALINE chembl_ligand pubchem drug_central
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Yang F, Ling S, Zhou Y, Zhang Y, Lv P, Liu S, Fang W, Sun W, Hu LA, Zhang L, Shi P, Tian C 10.1093/NSR/NWAA284 2020-12-16
Gi/o αi1 Human DN human Gαi1: S47N/G203A/A326S/E245A 62 β1 Human γ2 Human Cryo-EM 7E32 - 2.9 5HT1D HTR1D 5-HT1D 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist 5-HT-moduline, 5-hydroxytryptamine Small molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-21
Gi/o αi1 Human DN human Gαi1: S47N/G203A/A326S/E245A 61 β1 Human γ2 Human Cryo-EM 7E33 7E33_refined 2.9 5HT1E HTR1E 5-HT1E 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - BRL-54443 pubchem gtoplig chembl_ligand
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule Xu P, Huang S, Zhang H, Mao C, Zhou XE, Cheng X, Simon IA, Shen DD, Yen HY, Robinson CV, Harpsoe K, Svensson B, Guo J, Jiang H, Gloriam DE, Melcher K, Jiang Y, Zhang Y, Xu HE 10.1038/S41586-021-03376-8 2021-04-14
Gi/o αi3 Human DN Gαi3: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 7E9H - 4.0 GRM4 GRM4 mGlu4 Metabotropic glutamate C (Glutamate) Human - - - L-serine-O-phosphate pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist L-serine-O-phosphate, L-glutamic acid Small molecule Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B 10.1038/S41586-021-03495-2 2021-06-23
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 99 β1 Human γ2 Human Cryo-EM 7EB2 - 3.5 GABR2 GABBR2 GABAB2 GABAB C (Glutamate) Human - - - (-)-baclofen pubchem gtoplig chembl_ligand drugbank drugbank pubchem
rac-BHFF pubchem
Small molecule
Small molecule 		Agonist
PAM 		- - Shen C, Mao C, Xu C, Jin N, Zhang H, Shen DD, Shen Q, Wang X, Hou T, Chen Z, Rondard P, Pin JP, Zhang Y, Liu J 10.1038/S41586-021-03507-1 2021-05-05
Gi/o αo Human Wild-type human GoA heterotrimer 61 β1 Human γ2 Human Cryo-EM 7EJ8 - 3.0 ADA2A ADRA2A α2A Adrenoceptors A (Rhodopsin) Human - - - brimonidine (UK14304) pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y 10.1126/SCIADV.ABJ5347 2022-04-13
Gs αs Human Mini-Gs: minimal Gαs for structural stability 59 β1 Rat γ2 Bovine Cryo-EM 7DH5 - 3.2 ADRB3 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog - Nanobody-35 - mirabegron pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist - - Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O 10.1016/J.MOLCEL.2021.06.024 2021-08-04
Gs αs Human DNGs: 8 mutations 61 β1 Rat γ2 Bovine Cryo-EM 7DUQ - 2.5 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Compound 2 pubchem
glucagon-like peptide 1-(7-37) (Human) pubchem gtoplig uniprot uniprot uniprot chembl_ligand pubchem
Small molecule
Peptide 		Ago-PAM
Agonist 		glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-021-24058-Z 2021-07-14
Gi/o αi1 Human DN Gi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 7E9G - 3.5 GRM2 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - - - eglumegad pubchem gtoplig chembl_ligand
JNJ-40411813 pubchem gtoplig chembl_ligand drugbank
DN13
Small molecule
Small molecule
Protein 		Agonist
PAM
PAM 		L-glutamic acid Small molecule Lin S, Han S, Cai X, Tan Q, Zhou K, Wang D, Wang X, Du J, Yi C, Chu X, Dai A, Zhou Y, Chen Y, Zhou Y, Liu H, Liu J, Yang D, Wang MW, Zhao Q, Wu B 10.1038/S41586-021-03495-2 2021-06-23
Gi/o αo Human Nucleotide-free GoA heterotrimer complex 61 β1 Human γ2 Human Cryo-EM 7EJ0 - 3.2 ADA2A ADRA2A α2A Adrenoceptors A (Rhodopsin) Human - - - (-)-noradrenaline pubchem gtoplig chembl_ligand drugbank drug_central pubchem pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y 10.1126/SCIADV.ABJ5347 2022-04-13
Gi/o αi1 Human Human Gi1 heterotrimer complex 61 β1 Human γ2 Human Cryo-EM 7EJX - 2.4 GPR88 GPR88 GPR88 Orphan A (Rhodopsin) Human BRIL - - compound 2 [PMID: 24793972] pubchem gtoplig chembl_ligand
Small molecule Allosteric agonist - - Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y 10.1038/S41467-022-30081-5 2022-04-13
Gi/o αi1 Human DN human Gαi1: G203A/A326S mutations 62 β1 Human γ2 Human Cryo-EM 7EO2 7EO2_refined 2.9 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - LgBiT
HiBiT 		(S)-FTY720-phosphate pubchem gtoplig chembl_ligand
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y 10.1038/S41589-021-00930-3 2022-01-05
Gs αs Human Mini-Gs: αN helix replaced by Gαi equivalent 57 β1 Human γ2 Human Cryo-EM 7XY6 - 3.0 AA2BR ADORA2B A2B Adenosine A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		BAY 60-6583 pubchem gtoplig chembl_ligand
Small molecule Agonist (partial) adenosine Small molecule Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G 10.1126/SCIADV.ADD3709 2023-05-03
Gi/o αo Human Wild-type GoA heterotrimer 59 β1 Human γ2 Human Cryo-EM 7EJA - 3.6 ADA2A ADRA2A α2A Adrenoceptors A (Rhodopsin) Human - - - dexmedetomidine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y 10.1126/SCIADV.ABJ5347 2022-04-13
Gi/o αo Human GoA heterotrimer signaling complex 61 β1 Human γ2 Human Cryo-EM 7EJK - 3.4 ADA2A ADRA2A α2A Adrenoceptors A (Rhodopsin) Human - - - oxymetazoline pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule Xu J, Cao S, Hubner H, Weikert D, Chen G, Lu Q, Yuan D, Gmeiner P, Liu Z, Du Y 10.1126/SCIADV.ABJ5347 2022-04-13
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 43 β1 Human γ2 Human Cryo-EM 7EO4 7EO4_refined 2.9 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - LgBiT siponimod pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y 10.1038/S41589-021-00930-3 2022-01-05
Gi/o αi1 Human Wild-type human Gαi1 64 β1 Human γ2 Human Cryo-EM 7EVY - 3.0 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human T4-Lysozyme - - siponimod pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z 10.1038/S41422-021-00566-X 2021-09-29
Gi/o αi1 Human Wild-type human Gαi1 protein 64 β1 Human γ2 Human Cryo-EM 7EVZ - 3.1 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human T4-Lysozyme - - cenerimod pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z 10.1038/S41422-021-00566-X 2021-09-29
Gi/o αi1 Human Wild-type human Gαi1 subunit 64 β1 Human γ2 Human Cryo-EM 7EW0 7EW0_refined 3.4 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human T4-Lysozyme - - ozanimod pubchem gtoplig drug_central chembl_ligand drugbank pubchem
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z 10.1038/S41422-021-00566-X 2021-09-29
Gi/o αi1 Human WT human Gαi1 subunit (P63096), unmodified 64 β1 Human γ2 Human Cryo-EM 7EW1 7EW1_refined 3.4 S1PR5 S1PR5 S1P5 Lysophospholipid (S1P) A (Rhodopsin) Human - - - siponimod pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z 10.1038/S41422-021-00566-X 2021-09-29
Gi/o αi1 Human Wild-type human Gi heterotrimer 64 β1 Human γ2 Human Cryo-EM 7EW7 - 3.3 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human T4-Lysozyme - - SEW2871 pubchem gtoplig chembl_ligand
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Yuan Y, Jia G, Wu C, Wang W, Cheng L, Li Q, Li Z, Luo K, Yang S, Yan W, Su Z, Shao Z 10.1038/S41422-021-00566-X 2021-09-29
Gs αs Human Wild-type Gs heterotrimer 54 β1 Human γ2 Human Cryo-EM 7EPT - 3.0 AGRD1 ADGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - Nanobody-35 - - - - dihydrotestosterone Small molecule Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F, Zhou F, Xi YT, Yin W, Liu FZ, He DF, Zhang DL, Zhu ZL, Jiang Y, Du L, Feng SQ, Schoneberg T, Liebscher I, Xu HE, Sun JP 10.1038/S41586-022-04619-Y 2022-05-11
Gi/o αi1 Human Gi1 heterotrimer, Gβ1 N-term 6xHis tag 62 β1 Human γ2 Human Cryo-EM 7EUO 7EUO_refined 2.9 FPR1 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - - - fMet-Leu-Phe pubchem gtoplig chembl_ligand
Peptide Agonist spinorphin (Human), cathepsin G (Rat), fMet-Leu-Phe-Ile-Ile, annexin I-(2-26) (Human), mitochondrial peptde fMMYALF, mitochondrial peptide fMFADRW, fMet-Leu-Phe, annexin I (Rat), annexin I (Mouse), cathepsin G (Mouse), cathepsin G (Human), annexin I (Human) Peptide Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD 10.1038/S41467-022-32822-Y 2022-05-25
Gs αs Human DN human Gs: S54N/G226A +6 more mutations 60 β1 Rat γ2 Bovine Cryo-EM 7EVM - 2.5 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Compound 2 pubchem
Small molecule Ago-PAM glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cong Z, Chen LN, Ma H, Zhou Q, Zou X, Ye C, Dai A, Liu Q, Huang W, Sun X, Wang X, Xu P, Zhao L, Xia T, Zhong W, Yang D, Eric Xu H, Zhang Y, Wang MW 10.1038/S41467-021-24058-Z 2021-08-11
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW2 - 3.1 S1PR3 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - - - (S)-FTY720-phosphate pubchem gtoplig chembl_ligand
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z 10.1038/S41422-021-00567-W 2021-09-29
Gi/o αi1 Human Wild-type G protein subunits for complex 64 β1 Human γ2 Human Cryo-EM 7EW3 - 3.1 S1PR3 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - - - sphingosine 1-phosphate pubchem gtoplig chembl_ligand
Lipid Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z 10.1038/S41422-021-00567-W 2021-09-29
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7EW4 7EW4_refined 3.2 S1PR3 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - - - CYM-5541 pubchem gtoplig chembl_ligand
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Zhao C, Cheng L, Wang W, Wang H, Luo Y, Feng Y, Wang X, Fu H, Cai Y, Yang S, Fu P, Yan W, Shao Z 10.1038/S41422-021-00567-W 2021-09-29
Gi/o αi1 Human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 7EXD 7EXD_refined 3.4 5HT1F HTR1F 5-HT1F 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - lasmiditan pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule Huang S, Xu P, Tan Y, You C, Zhang Y, Jiang Y, Xu HE 10.1038/S41422-021-00527-4 2021-08-04
Gi/o αi1 Human DN Gαi1: G203A/A326S 61 β1 Human γ2 Human Cryo-EM 7EZH - 3.2 CCKAR CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CCK-8 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Peptide Agonist gastrin-17 (Human), CCK-33 (Mouse), CCK-4 (Human), CCK-8 (Human), CCK-33 (Human), gastrin-17 (Rat), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y 10.1038/S41589-021-00841-3 2021-08-25
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 7F1R - 3.0 CCR5 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - - - - CCL3 (Mouse), CCL7 (Human), CCL13 (Human), CCL11 (Rat), CCL16 (Human), CCL11 (Mouse), CCL8 (Human), CCL2 (Rat), CCL5 (Mouse), CCL14 (Human), CCL4 (Mouse), CCL5 (Human), CCL4 (Human), CCL3 (Rat), CCL3 (Human), CCL7 (Rat), CCL11 (Human), CCL2 (Human), CCL4 (Rat), CCL8 (Mouse), CCL7 (Mouse), CCL2 (Mouse) Peptide - - 2021-07-14
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 7F1S 7F1S_refined 2.8 CCR5 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - - None - CCL3 (Mouse), CCL7 (Human), CCL13 (Human), CCL11 (Rat), CCL16 (Human), CCL11 (Mouse), CCL8 (Human), CCL2 (Rat), CCL5 (Mouse), CCL14 (Human), CCL4 (Mouse), CCL5 (Human), CCL4 (Human), CCL3 (Rat), CCL3 (Human), CCL7 (Rat), CCL11 (Human), CCL2 (Human), CCL4 (Rat), CCL8 (Mouse), CCL7 (Mouse), CCL2 (Mouse) Peptide Zhang H, Chen K, Tan Q, Shao Q, Han S, Zhang C, Yi C, Chu X, Zhu Y, Xu Y, Zhao Q, Wu B 10.1038/S41467-021-24438-5 2021-07-14
Gs αs Human Gs/Gi1 chimera (N-term+AHD); DN G203A/A326S 58 β1 Human γ2 Human Cryo-EM 7EZK - 3.1 CCKAR CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - - - CCK-8 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Peptide Agonist gastrin-17 (Human), CCK-33 (Mouse), CCK-4 (Human), CCK-8 (Human), CCK-33 (Human), gastrin-17 (Rat), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Liu Q, Yang D, Zhuang Y, Croll TI, Cai X, Dai A, He X, Duan J, Yin W, Ye C, Zhou F, Wu B, Zhao Q, Xu HE, Wang MW, Jiang Y 10.1038/S41589-021-00841-3 2021-08-25
Gs αs Human mini-Gs: thermostable, AHD deleted, stab muts 58 β1 Human γ2 Human Cryo-EM 7F0T - 3.1 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S 10.1126/SCIADV.ABO4158 2022-06-15
Gs αs Human Mini-Gs: thermostable, AHD deleted 60 β1 Human γ2 Human Cryo-EM 7F1O - 3.1 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S 10.1126/SCIADV.ABO4158 2022-06-15
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 7F1Q - 2.9 CCR5 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - - - - CCL3 (Mouse), CCL7 (Human), CCL13 (Human), CCL11 (Rat), CCL16 (Human), CCL11 (Mouse), CCL8 (Human), CCL2 (Rat), CCL5 (Mouse), CCL14 (Human), CCL4 (Mouse), CCL5 (Human), CCL4 (Human), CCL3 (Rat), CCL3 (Human), CCL7 (Rat), CCL11 (Human), CCL2 (Human), CCL4 (Rat), CCL8 (Mouse), CCL7 (Mouse), CCL2 (Mouse) Peptide - - 2021-07-14
Gs αs Human DNGs: DN Gs to stabilize complex 58 β1 Human γ2 Human Cryo-EM 7F53 - 3.0 MC4R MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - Alpha-MSH pubchem
Calcium pubchem
Small molecule
Small molecule 		Agonist
Cofactor 		ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y 10.1038/S41422-021-00552-3 2021-11-03
Gs αs Human Thermostable miniGs399, ΔAHD 60 β1 Human γ2 Human Cryo-EM 7F1Z - 3.5 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - - - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S 10.1126/SCIADV.ABO4158 2022-06-15
Gs αs Human mini-Gs: AHD deleted, I372A mut, GTP-bound 60 β1 Human γ2 Human Cryo-EM 7F23 - 3.6 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S 10.1126/SCIADV.ABO4158 2022-06-15
Gs αs Human Thermostable miniGs399: ΔAHD, I372A mutation 57 β1 Human γ2 Human Cryo-EM 7F24 - 4.2 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - - - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, Zheng S 10.1126/SCIADV.ABO4158 2022-06-15
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 7F54 - 3.0 MC4R MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - afamelanotide pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y 10.1038/S41422-021-00552-3 2021-11-03
Gs αs Human DNGαs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 7F55 - 3.1 MC4R MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - bremelanotide pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Peptide Agonist ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y 10.1038/S41422-021-00552-3 2021-11-03
Gs αs Human DNGs: G226A/V272D/A326S 58 β1 Human γ2 Human Cryo-EM 7F58 7F58_refined 3.1 MC4R MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - THIQ pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand chembl_ligand pubchem pubchem
Small molecule Agonist ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP, Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y 10.1038/S41422-021-00552-3 2021-11-03
Gi/o αi2 Human DN Gi2: S47N/G204A/E246A/A327S 61 β1 Human γ2 Human Cryo-EM 7F8V - 3.3 GASR CCKBR CCK2 Cholecystokinin A (Rhodopsin) Human - - - desulfated gastrin-17 (Human) pubchem gtoplig uniprot chembl_ligand pubchem
Peptide Agonist gastrin-17 (Human), gastrin-34 (Human), CCK-33 (Mouse), gastrin-71 (Human), CCK-4 (Human), CCK-8 (Human), desulfated gastrin-17 (Human), CCK-33 (Human), desulfated gastrin-34 (Human), desulfated gastrin-71 (Human), desulfated gastrin-14 (Human), gastrin-17 (Rat), gastrin-14 (Human), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Zhang X, He C, Wang M, Zhou Q, Yang D, Zhu Y, Feng W, Zhang H, Dai A, Chu X, Wang J, Yang Z, Jiang Y, Sensfuss U, Tan Q, Han S, Reedtz-Runge S, Xu HE, Zhao S, Wang MW, Wu B, Zhao Q 10.1038/S41589-021-00866-8 2021-10-13
Gq/11 αq Human DN mutations R183Q/Q209L to stabilize complex 63 β1 Human γ2 Human Cryo-EM 7F6I 7F6I_refined 2.8 BKRB2 BDKRB2 B2 Bradykinin A (Rhodopsin) Human - - Maltose-binding protein kallidin (Human) pubchem gtoplig uniprot chembl_ligand
Peptide Agonist [des-Arg10]kallidin (Human), kallidin (Human), T-kinin (Human), Lys-[Hyp3]-bradykinin (Human), bradykinin (Human), [des-Arg9]bradykinin (Human), [Hyp3]bradykinin (Human) Peptide Shen J, Zhang D, Fu Y, Chen A, Yang X, Zhang H 10.1038/S41467-022-28399-1 2022-01-05
Gs αs Human Mini-Gs/Gi1 chimera (dual metadata IDs) 60 β1 Rat γ2 Bovine Cryo-EM 7DW9 - 2.6 V2R AVPR2 V2 Vasopressin and oxytocin A (Rhodopsin) Human - Nanobody-35 - vasopressin (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem pubchem
Peptide Agonist vasopressin (Human), oxytocin (Human) Peptide Zhou F, Ye C, Ma X, Yin W, Croll TI, Zhou Q, He X, Zhang X, Yang D, Wang P, Xu HE, Wang MW, Jiang Y 10.1038/S41422-021-00480-2 2021-07-21
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 7JHJ - 3.2 Q3KSP2 BILF1 BILF1 Unclassified A (Rhodopsin) HHV-4 - - - - None - - - Tsutsumi N, Qu Q, Mavri M, Baggesen MS, Maeda S, Waghray D, Berg C, Kobilka BK, Rosenkilde MM, Skiniotis G, Garcia KC 10.1016/J.IMMUNI.2021.06.001 2021-07-07
Gs αs Human Gs heterotrimer complexed with Nb35 86 β1 Human γ2 Human X-ray 7JOZ 7JOZ_refined 3.8 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human T4-Lysozyme Nanobody-35 - CHEMBL4453318 chembl_ligand pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Sun B, Feng D, Chu ML, Fish I, Lovera S, Sands ZA, Kelm S, Valade A, Wood M, Ceska T, Kobilka TS, Lebon F, Kobilka BK 10.1038/S41467-021-23519-9 2021-04-14
Gs αs Human DN Gs: G226A/A366S 60 β1 Human γ2 Human Cryo-EM 7JV5 - 3.0 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - SKF-81297 pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24
Gs αs Human Mini-Gs (mislabeled mini-Gi in metadata) 60 β1 Human γ2 Human Cryo-EM 7JVQ 7JVQ_refined 3.0 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - apomorphine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24
Gi/o αi1 Human DN Gαi1: S47N/G203A/E345A/A326S 63 β1 Human γ2 Human Cryo-EM 7JVR - 2.8 DRD2 DRD2 D2 Dopamine A (Rhodopsin) Human BRIL - - bromocriptine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist dopamine Small molecule Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24
Gs αs Human Gs/Gi chimera: Gαs N-term→Gαi for scFv16 58 β1 Human γ2 Human Cryo-EM 7KH0 - 2.8 V2R AVPR2 V2 Vasopressin and oxytocin A (Rhodopsin) Human - Nanobody-35 - vasopressin (Human) pubchem gtoplig chembl_ligand drugbank drug_central uniprot uniprot uniprot pubchem pubchem
Peptide Agonist vasopressin (Human), oxytocin (Human) Peptide Wang L, Xu J, Cao S, Sun D, Liu H, Lu Q, Liu Z, Du Y, Zhang C 10.1038/S41422-021-00483-Z 2021-05-26
Gs αs Human DN Gs: G226A/A366S 60 β1 Human γ2 Human Cryo-EM 7JVP - 2.9 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 b2-Adrenergic Receptor N-terminal tail SKF-83959 pubchem gtoplig chembl_ligand chembl_ligand pubchem pubchem
Small molecule Agonist (partial) 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Zhuang Y, Xu P, Mao C, Wang L, Krumm B, Zhou XE, Huang S, Liu H, Cheng X, Huang XP, Shen DD, Xu T, Liu YF, Wang Y, Guo J, Jiang Y, Jiang H, Melcher K, Roth BL, Zhang Y, Zhang C, Xu HE 10.1016/J.CELL.2021.01.027 2021-02-24
Gi/o αi1 Human WT human Gi; Gαi1 myristoylated, Gγ1 prenylated 95 β1 Human γT1 Human Cryo-EM 7L0Q - 4.3 NTR1 Ntsr1 NTS1 Neurotensin A (Rhodopsin) Rat - - - NTS8–13 pubchem
Peptide Agonist neurotensin (Human), neuromedin N (Mouse) Peptide Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06
Gi/o αi1 Human WT human subunits; AHD masked, not in PDB coords 63 β1 Human γT1 Human Cryo-EM 7L0R - 4.2 NTR1 Ntsr1 NTS1 Neurotensin A (Rhodopsin) Rat - - - NTS8–13 pubchem
Peptide Agonist neurotensin (Human), neuromedin N (Mouse) Peptide Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06
Gs αs Human DNGs: 9 muts incl S54N/G226A/A366S 89 β1 Human γ2 Human Cryo-EM 7KI1 - 2.5 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - taspoglutide pubchem gtoplig drugbank
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhang X, Belousoff MJ, Liang YL, Danev R, Sexton PM, Wootten D 10.1016/J.CELREP.2021.109374 2021-08-04
Gi/o αi1 Human WT human Gi1β1γ1, apyrase; AHD masked in 7L0P 63 β1 Human γT1 Human Cryo-EM 7L0P - 4.1 NTR1 Ntsr1 NTS1 Neurotensin A (Rhodopsin) Rat - - - NTS8–13 pubchem
Peptide Agonist neurotensin (Human), neuromedin N (Mouse) Peptide - - 2021-01-06
Gs αs Human DNGas: DN Gs for stabilization 62 β1 Human γ2 Human Cryo-EM 7LCI 7LCI_refined 2.9 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - danuglipron pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhang X, Johnson RM, Drulyte I, Yu L, Kotecha A, Danev R, Wootten D, Sexton PM, Belousoff MJ 10.1016/J.STR.2021.04.008 2021-01-20
Gi/o αi2 Human DN Gαi2 with stabilizing point mutations 59 β1 Human γ2 Human Cryo-EM 7LD3 - 3.2 AA1R ADORA1 A1 Adenosine A (Rhodopsin) Human - - - adenosine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
MIPS521 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		adenosine Small molecule Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A 10.1038/S41586-021-03897-2 2021-09-08
Gi/o αi2 Human DN Gαi2 (DNGi2): S47N/G203A/E245A/A326S 59 β1 Human γ2 Human Cryo-EM 7LD4 7LD4_refined 3.3 AA1R ADORA1 A1 Adenosine A (Rhodopsin) Human - - - adenosine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist adenosine Small molecule Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, White PJ, Scammells P, May LT, Sexton PM, Danev R, Miao Y, Glukhova A, Imlach WL, Christopoulos A 10.1038/S41586-021-03897-2 2021-09-08
Gi/o αi1 Human Nucleotide-free: myristoyl-Gαi1, prenyl-Gγ1 95 β1 Human γT1 Human Cryo-EM 7L0S - 4.5 NTR1 Ntsr1 NTS1 Neurotensin A (Rhodopsin) Rat - - - NTS8–13 pubchem
Peptide Agonist neurotensin (Human), neuromedin N (Mouse) Peptide Zhang M, Gui M, Wang ZF, Gorgulla C, Yu JJ, Wu H, Sun ZJ, Klenk C, Merklinger L, Morstein L, Hagn F, Pluckthun A, Brown A, Nasr ML, Wagner G 10.1038/S41594-020-00554-6 2021-01-06
Gi/o αi1 Human WT human Gi1/Gβ1/Gγ2, apyrase nucleotide-free 61 β1 Human γ2 Human Cryo-EM 7NA8 - 2.7 GHSR GHSR ghrelin Ghrelin A (Rhodopsin) Human - - - ibutamoren pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Agonist
PAM 		[des-Gln14]ghrelin (Mouse), liver enriched antimicrobial peptide 2 (Human), ghrelin (Mouse), [des-Gln14]ghrelin (Human), ghrelin (Human) Peptide Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C 10.1038/S41467-021-26735-5 2021-12-15
Gs αs Human DNGs: DN Gs protein for stabilization 59 β1 Human γ2 Human Cryo-EM 7LLL - 3.7 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Exendin-4 pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D 10.1038/S41467-021-27760-0 2022-01-12
Gs αs Human DNGαs: muts stabilize nucleotide-free state 50 β1 Human γ2 Human Cryo-EM 7LLY 7LLY_refined 3.3 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Oxyntomodulin pubchem pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Deganutti G, Liang YL, Zhang X, Khoshouei M, Clydesdale L, Belousoff MJ, Venugopal H, Truong TT, Glukhova A, Keller AN, Gregory KJ, Leach K, Christopoulos A, Danev R, Reynolds CA, Zhao P, Sexton PM, Wootten D 10.1038/S41467-021-27760-0 2022-01-12
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 58 β1 Human γ2 Human Cryo-EM 7MTS - 3.2 GRM2 GRM2 mGlu2 Metabotropic glutamate C (Glutamate) Human - - - ADX55164 pubchem
L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
Small molecule
Small molecule 		Ago-PAM
Agonist 		L-glutamic acid Small molecule Seven AB, Barros-Alvarez X, de Lapeyriere M, Papasergi-Scott MM, Robertson MJ, Zhang C, Nwokonko RM, Gao Y, Meyerowitz JG, Rocher JP, Schelshorn D, Kobilka BK, Mathiesen JM, Skiniotis G 10.1038/S41586-021-03680-3 2021-07-07
Gi/o αi1 Human WT Gi, Gβ1 N-term 6xHis tag, nucleotide-free 61 β1 Human γ2 Human Cryo-EM 7NA7 7NA7_refined 2.7 GHSR GHSR ghrelin Ghrelin A (Rhodopsin) Human - - - Ghrelin-27
Peptide Agonist [des-Gln14]ghrelin (Mouse), liver enriched antimicrobial peptide 2 (Human), ghrelin (Mouse), [des-Gln14]ghrelin (Human), ghrelin (Human) Peptide Liu H, Sun D, Myasnikov A, Damian M, Baneres JL, Sun J, Zhang C 10.1038/S41467-021-26735-5 2021-12-15
Gs αs Human GsDN: DN Gs for stabilization 61 β1 Rat γ2 Human Cryo-EM 7MBX - 2.0 CCKAR CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - Nanobody-35 - CCK-8 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Peptide Agonist gastrin-17 (Human), CCK-33 (Mouse), CCK-4 (Human), CCK-8 (Human), CCK-33 (Human), gastrin-17 (Rat), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Mobbs JI, Belousoff MJ, Harikumar KG, Piper SJ, Xu X, Furness SGB, Venugopal H, Christopoulos A, Danev R, Wootten D, Thal DM, Miller LJ, Sexton PM 10.1371/JOURNAL.PBIO.3001295 2021-05-26
Gs αs Human Gs-alpha short isoform Gnas-2 48 β1 Rat γ2 Bovine Cryo-EM 7PIU - 2.6 MC4R MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - setmelanotide pubchem gtoplig drug_central drugbank
Peptide Agonist ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P 10.1038/S41422-021-00569-8 2021-11-17
Gs αs Human Gs heterotrimer; Gα short isoform Gnas-2 46 β1 Rat γ2 Mouse Cryo-EM 7PIV 7PIV_refined 2.9 MC4R MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 - afamelanotide pubchem gtoplig chembl_ligand chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Heyder NA, Kleinau G, Speck D, Schmidt A, Paisdzior S, Szczepek M, Bauer B, Koch A, Gallandi M, Kwiatkowski D, Burger J, Mielke T, Beck-Sickinger AG, Hildebrand PW, Spahn CMT, Hilger D, Schacherl M, Biebermann H, Hilal T, Kuhnen P, Kobilka BK, Scheerer P 10.1038/S41422-021-00569-8 2021-11-17
Gs αs Human GsαiN18: Gαs N-term→Gαi3, for scFv16 56 β1 Human γ2 Human Cryo-EM 7RA3 - 3.2 GIPR GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - Gastric inhibitory polypeptide pubchem
Peptide Agonist gastric inhibitory polypeptide (Mouse), gastric inhibitory polypeptide (Human) Peptide Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
Gs αs Human GsαiN18: Gs N-term(1-25)→Gi1(1-18), scFv16 56 β1 Human γ2 Human Cryo-EM 7RBT 7RBT_refined 3.1 GIPR GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - tirzepatide pubchem gtoplig
LSN3556672 pubchem
Peptide
Small molecule 		Agonist
PAM 		gastric inhibitory polypeptide (Mouse), gastric inhibitory polypeptide (Human) Peptide Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
Gs αs Human GsαiN18: Gαs N-term→Gαi1(1-18), scFv16 56 β1 Human γ2 Human Cryo-EM 7RG9 7RG9_refined 3.2 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - - None - glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
Gs αs Human GsαiN18: Gαs N-term→Gαi3(1-18), scFv16 55 β1 Human γ2 Human Cryo-EM 7RGP - 2.9 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - tirzepatide pubchem gtoplig
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW 10.1073/PNAS.2116506119 2022-04-13
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7RKN - 3.6 US28 US28 US28 Unclassified A (Rhodopsin) strain AD169 - - - Fractalkine
Protein Agonist (partial) - - Tsutsumi N, Maeda S, Qu Q, Vogele M, Jude KM, Suomivuori CM, Panova O, Waghray D, Kato HE, Velasco A, Dror RO, Skiniotis G, Kobilka BK, Garcia KC 10.1126/SCIADV.ABL5442 2022-01-26
Gs αs Human MiniGs399: mutated, truncated Gαs 55 β1 Human γ2 Human Cryo-EM 7RMH 7RMH_refined 3.1 NK1R TACR1 NK1 Tachykinin A (Rhodopsin) Human - Nanobody-35 - substance P (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide Harris JA, Faust B, Gondin AB, Damgen MA, Suomivuori CM, Veldhuis NA, Cheng Y, Dror RO, Thal DM, Manglik A 10.1038/S41589-021-00890-8 2021-11-03
Gi/o αi1 Human DN Gαi1 62 β1 Human γ2 Human Cryo-EM 7S8O - 2.6 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human BRIL - - (R)-ZINC-3573 pubchem gtoplig chembl_ligand
Small molecule Agonist PAMP-20 (Human) Peptide Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL 10.1038/S41586-021-04126-6 2021-11-17
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7SBF - 2.9 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse BRIL - - PZM21 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist (partial) - - Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P 10.1002/ANIE.202200269 2022-04-20
Gi/o αi1 Human Wild-type Gi heterotrimer 61 β1 Human γ2 Human Cryo-EM 7SCG - 3.0 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - FH210 pubchem
Small molecule Agonist - - Wang H, Hetzer F, Huang W, Qu Q, Meyerowitz J, Kaindl J, Hubner H, Skiniotis G, Kobilka BK, Gmeiner P 10.1002/ANIE.202200269 2022-04-20
Gs αs Human DNGs: DN Gs for stabilization 60 β1 Human γ2 Human Cryo-EM 7RTB 7RTB_refined 2.1 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide-19
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Johnson RM, Zhang X, Piper SJ, Nettleton TJ, Vandekolk TH, Langmead CJ, Danev R, Sexton PM, Wootten D 10.1016/J.BBRC.2021.09.016 2021-10-06
Gs αs Human DNGαs: dominant-negative Gs protein 59 β1 Human γ2 Human Cryo-EM 7S1M 7S1M_refined 2.4 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Ex4-D-Ala
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cary BP, Deganutti G, Zhao P, Truong TT, Piper SJ, Liu X, Belousoff MJ, Danev R, Sexton PM, Wootten D, Gellman SH 10.1038/S41589-021-00945-W 2022-01-05
G12/13 α13 Human Gα13/Gαi2 chimera, linker + 7 stab muts 56 β1 Human γ2 Human Cryo-EM 7SF7 - 2.9 AGRL3 ADGRL3 ADGRL3 ADGRL B2 (Adhesion) Human - - - - - - - - Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G 10.1038/S41586-022-04575-7 2022-04-27
G12/13 α13 Human Gi2-miniG13 chimera, linker+7 stabilizing muts 56 β1 Human γ2 Human Cryo-EM 7SF8 - 2.7 AGRG1 ADGRG1 ADGRG1 ADGRG B2 (Adhesion) Human - - - - - - - - Barros-Alvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB, Kwarcinski FE, Su H, Peroto MC, Meyerowitz JG, Shalev-Benami M, Tall GG, Skiniotis G 10.1038/S41586-022-04575-7 2022-04-27
Gi/o αi1 Human DN bovine Gαi1: G203A/A326S mutations 61 β1 Bovine γ2 Bovine Cryo-EM 7SQO - 3.2 OX2R HCRTR2 OX2 Orexin A (Rhodopsin) Human - - - danavorexton pubchem gtoplig chembl_ligand pubchem drugbank
Small molecule Agonist orexin-B (Mouse), orexin-A (Human), orexin-B (Human) Peptide Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM 10.1038/S41467-022-30601-3 2022-05-25
Gi/o αi3 Human DN Gαi3 62 β1 Human γ2 Human Cryo-EM 7T10 - 2.5 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - - SOMATOSTATIN chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G 10.1038/S41594-022-00727-5 2022-03-09
Gi/o αi3 Human DN Gαi3, complex stabilizer 62 β1 Human γ2 Human Cryo-EM 7T11 7T11_refined 2.7 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - - octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Robertson MJ, Meyerowitz JG, Panova O, Borrelli K, Skiniotis G 10.1038/S41594-022-00727-5 2022-03-09
Gi/o αi1 Human Gi1 heterotrimer complex 62 β1 Human γ2 Human Cryo-EM 7T2G - 2.5 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse BRIL - - Mitragynine pseudoindoxyl
Small molecule Agonist (partial) - - Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41589-022-01208-Y 2022-12-07
G12/13 α13 Human Gα13iN: αN helix replaced by Gαi1 60 β1 Human γ2 Human Cryo-EM 7T6B 7T6B_refined 3.2 S1PR2 S1PR2 S1P2 Lysophospholipid (S1P) A (Rhodopsin) Human - - - sphingosine 1-phosphate pubchem gtoplig chembl_ligand
Lipid Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Chen H, Chen K, Huang W, Staudt LM, Cyster JG, Li X 10.1126/SCIADV.ABN0067 2022-04-06
Gi/o αi1 Human DN Gi1: G203A/A326S 61 β1 Rat γ2 Bovine Cryo-EM 7T6S 7T6S_refined 3.0 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - - - compound 43 [PMID: 21173551] pubchem gtoplig chembl_ligand
Small molecule Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C 10.1038/S41467-022-28586-0 2022-03-30
Gi/o αi1 Human DN Gαi1: G203A/A326S 61 β1 Rat γ2 Bovine Cryo-EM 7T6V 7T6V_refined 3.1 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - - - fMLFII
Peptide Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide Zhuang Y, Wang L, Guo J, Sun D, Wang Y, Liu W, Xu HE, Zhang C 10.1038/S41467-022-28586-0 2022-03-30
Gi/o αi1 Human Gi1 heterotrimer: Gαi1/Gβ1/Gγ2 61 β1 Human γ2 Human Cryo-EM 7T2H - 3.2 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse BRIL - - LOFENTANIL chembl_ligand pubchem drugbank
Small molecule Agonist - - Qu Q, Huang W, Aydin D, Paggi JM, Seven AB, Wang H, Chakraborty S, Che T, DiBerto JF, Robertson MJ, Inoue A, Suomivuori CM, Roth BL, Majumdar S, Dror RO, Kobilka BK, Skiniotis G 10.1038/S41589-022-01208-Y 2022-12-07
Gi/o αo Human Mini-Gαo, stabilized construct 62 β1 Human γ2 Human Cryo-EM 7T8X 7T8X_refined 3.2 ACM2 CHRM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist acetylcholine Small molecule - - 2023-01-25
Gi/o αo Human GoA heterotrimer, α is miniGαo per paper 62 β1 Human γ2 Human Cryo-EM 7T90 7T90_refined 3.3 ACM2 CHRM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist acetylcholine Small molecule - - 2023-01-25
Gi/o αo Human MiniGαo construct 62 β1 Human γ2 Human Cryo-EM 7T94 - 3.2 ACM2 CHRM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
LY2119620 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		acetylcholine Small molecule - - 2023-01-25
Gi/o αo Human MiniGo (miniGαo) construct 62 β1 Human γ2 Human Cryo-EM 7T96 7T96_refined 3.2 ACM2 CHRM2 M2 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
LY2119620 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		acetylcholine Small molecule - - 2023-01-25
Gs αs Human MiniGs399: GTPase domain(1-261), thermostable 56 β1 Human γ2 Human Cryo-EM 7T9N - 2.9 TSHR TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - M22 Fab (chain H)
M22 Fab (chain L)
Protein
Protein 		Agonist TSH (Rat), TSH (Human), TSH (Mouse) Peptide Faust B, Billesbolle CB, Suomivuori CM, Singh I, Zhang K, Hoppe N, Pinto AFM, Diedrich JK, Muftuoglu Y, Szkudlinski MW, Saghatelian A, Dror RO, Cheng Y, Manglik A 10.1038/S41586-022-05159-1 2022-08-03
Gi/o αi1 Human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 7TRP - 2.4 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - iperoxo pubchem gtoplig chembl_ligand
LY2033298 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		acetylcholine Small molecule - - 2023-05-17
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7TRQ - 2.5 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - iperoxo pubchem gtoplig chembl_ligand
VU0467154 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		acetylcholine Small molecule - - 2023-05-17
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 7TRS - 2.8 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - acetylcholine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist acetylcholine Small molecule - - 2023-05-17
Gi/o αi1 Human Wild-type human Gi heterotrimer 64 β1 Human γ2 Human Cryo-EM 7TUZ 7TUZ_refined 3.1 GP183 GPR183 GPR183 Orphan A (Rhodopsin) Human - - - 7α,25-dihydroxycholesterol pubchem gtoplig chembl_ligand
Small molecule Agonist 7α,25-dihydroxycholesterol, 27-hydroxycholesterol, 7β, 27-dihydroxycholesterol, 7α,27-dihydroxycholesterol, 7α-hydroxycholesterol, 25-hydroxycholesterol, 7β, 25-dihydroxycholesterol, 7β-hydroxycholesterol Small molecule Chen H, Huang W, Li X 10.1016/J.STR.2022.04.006 2022-04-13
Gs αs Human DN Gs (DNGs) with stabilizing mutations 58 β1 Human γ2 Human Cryo-EM 7TYI - 3.3 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Islet amyloid polypeptide pubchem
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-30
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 7TYL - 3.3 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - rat amylin pubchem
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human mini-Gs fused to receptor C-term (res 737) 57 β1 Human γ2 Human Cryo-EM 7TMW - 3.2 RXFP1 RXFP1 RXFP1 Relaxin family peptide A (Rhodopsin) Human - Nanobody-35 - - None - relaxin-1 (Human), relaxin-3 (Human), relaxin (Human) Peptide - - 2023-02-15
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7TRK - 2.8 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - iperoxo pubchem gtoplig chembl_ligand
Small molecule Agonist acetylcholine Small molecule - - 2023-05-17
Gs αs Human DN heterotrimeric Gs (DNGs) 58 β1 Human γ2 Human Cryo-EM 7TYF - 2.2 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- rat amylin pubchem
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human Dominant-negative Gs (DNGs) 58 β1 Human γ2 Human Cryo-EM 7TYH - 3.3 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP2 		- calcitonin (Human) pubchem gtoplig chembl_ligand uniprot drug_central pubchem
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human DNGs: DN Gs for stabilization 58 β1 Human γ2 Human Cryo-EM 7TYO - 2.7 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - calcitonin (Human) pubchem gtoplig chembl_ligand uniprot drug_central pubchem
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 7TYY - 3.0 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP2 		- CALCITONIN SALMON chembl_ligand drug_central pubchem pubchem
Protein Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human DNGs: dominant-negative Gs protein 59 β1 Human γ2 Human Cryo-EM 7TZF - 2.4 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- rat amylin pubchem
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gi/o αo Human MiniGo construct (Gαo-based) 60 β1 Human γ2 Human Cryo-EM 7UM5 7UM5_refined 2.7 5HT5A HTR5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human - - - 5-CT pubchem gtoplig chembl_ligand
Small molecule Agonist 5-hydroxytryptamine Small molecule Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 7TYN - 2.6 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - CALCITONIN SALMON chembl_ligand drug_central pubchem pubchem
Protein Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-30
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 7TYW - 3.0 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- CALCITONIN SALMON chembl_ligand drug_central pubchem pubchem
Protein Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-23
Gs αs Human DNGs: dominant-negative Gs protein 59 β1 Human γ2 Human Cryo-EM 7TYX - 2.6 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP2 		- rat amylin pubchem
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Liang YL, Johnson RM, Josephs TM, Fletcher MM, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM 10.1126/SCIENCE.ABM9609 2022-03-30
Gi/o αi1 Human Standard Gi heterotrimer 61 β1 Human γ2 Human Cryo-EM 7U2K - 3.3 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - CHEMBL147044 chembl_ligand pubchem
Small molecule Agonist - - Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S 10.1038/S41586-022-05588-Y 2022-12-07
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 7U2L - 3.2 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - C5 guano pubchem
Small molecule Agonist - - Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S 10.1038/S41586-022-05588-Y 2022-05-04
Gi/o αo Human MiniGo: truncated Gαo, not a fusion 60 β1 Human γ2 Human Cryo-EM 7UM7 7UM7_refined 2.8 5HT5A HTR5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human - - - methylergonovine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20
Gi/o αi1 Human Gi1 heterotrimer complex 62 β1 Human γ2 Human Cryo-EM 7V68 - 3.4 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human BRIL - - iperoxo pubchem gtoplig chembl_ligand
LY2119620 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		acetylcholine Small molecule Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T 10.1038/S41467-022-30595-Y 2022-05-11
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 7V69 - 3.4 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human BRIL - - - None - acetylcholine Small molecule Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T 10.1038/S41467-022-30595-Y 2022-05-11
Gi/o αi1 Human Wild-type human Gi heterotrimer 62 β1 Human γ2 Human Cryo-EM 7V6A - 3.6 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human BRIL - - CHEMBL6164470 chembl_ligand pubchem
Small molecule Allosteric agonist acetylcholine Small molecule Wang J, Wu M, Chen Z, Wu L, Wang T, Cao D, Wang H, Liu S, Xu Y, Li F, Liu J, Chen N, Zhao S, Cheng J, Wang S, Hua T 10.1038/S41467-022-30595-Y 2022-05-11
Gs αs Human Mini-Gs: Gs/Gi1 chimera, Ras domain modeled 60 β1 Rat γ2 Bovine Cryo-EM 7VAB 7VAB_refined 3.2 GIPR GIPR GIP Glucagon B1 (Secretin) Human BRIL Nanobody-35 - Non-acylated tirzepatide
Peptide Agonist gastric inhibitory polypeptide (Mouse), gastric inhibitory polypeptide (Human) Peptide Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
Gs αs Human DNGs: 8 muts to stabilize receptor complex 53 β1 Rat γ2 Bovine Cryo-EM 7VBH 7VBH_refined 3.0 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 20
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-04-06
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 7VDH - 2.9 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human BRIL - - compound 48/80 pubchem gtoplig
Small molecule Agonist PAMP-20 (Human) Peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gi/o αi1 Human DN Gαi1 with S47N/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 7VDL - 3.2 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human BRIL - - CORTISTATIN-14 chembl_ligand pubchem
Peptide Agonist PAMP-20 (Human) Peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 7VDM 7VDM_refined 3.0 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human BRIL - - substance P (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist PAMP-20 (Human) Peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gi/o αi1 Human Wild-type Gi heterotrimer 62 β1 Human γ2 Human Cryo-EM 7VFX 7VFX_refined 2.8 FPR1 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - - - fMIFL pubchem
Peptide Agonist spinorphin (Human), cathepsin G (Rat), fMet-Leu-Phe-Ile-Ile, annexin I-(2-26) (Human), mitochondrial peptde fMMYALF, mitochondrial peptide fMFADRW, fMet-Leu-Phe, annexin I (Rat), annexin I (Mouse), cathepsin G (Mouse), cathepsin G (Human), annexin I (Human) Peptide Chen G, Wang X, Liao Q, Ge Y, Jiao H, Chen Q, Liu Y, Lyu W, Zhu L, van Zundert GCP, Robertson MJ, Skiniotis G, Du Y, Hu H, Ye RD 10.1038/S41467-022-32822-Y 2022-09-21
Gi/o αi1 Human WT human Gi1; AHD not modeled (flexible) 63 β1 Human γ2 Human Cryo-EM 7VGX 7VGX_refined 3.2 NPY1R NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human - - - NEUROPEPTIDE-Y chembl_ligand pubchem
Protein Agonist neuropeptide Y (Human), pancreatic polypeptide (Human), peptide YY (Human), pancreatic polypeptide (Mouse), peptide YY (Mouse) Peptide Park C, Kim J, Ko SB, Choi YK, Jeong H, Woo H, Kang H, Bang I, Kim SA, Yoon TY, Seok C, Im W, Choi HJ 10.1038/S41467-022-28510-6 2022-02-23
Gi/o αi1 Human Gi heterotrimer complex 64 β1 Human γ2 Human Cryo-EM 7VIE 7VIE_refined 2.9 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BRIL - - sphingosine 1-phosphate pubchem gtoplig chembl_ligand
Lipid Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R 10.1073/PNAS.2117716119 2022-09-28
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VIF 7VIF_refined 2.8 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BRIL - - (S)-FTY720-phosphate pubchem gtoplig chembl_ligand
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R 10.1073/PNAS.2117716119 2022-09-28
Gi/o αi1 Human Gi1 heterotrimer 63 β1 Human γ2 Human Cryo-EM 7VIG 7VIG_refined 2.9 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BRIL - - icanbelimod pubchem gtoplig chembl_ligand
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R 10.1073/PNAS.2117716119 2022-09-28
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 7VIH 7VIH_refined 3.0 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BRIL - - icanbelimod pubchem gtoplig chembl_ligand
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Yu L, He L, Gan B, Ti R, Xiao Q, Hu H, Zhu L, Wang S, Ren R 10.1073/PNAS.2117716119 2022-09-28
Gi/o αi1 Human DN Gαi1; Gβ1 C-term SmBiT tag 64 β1 Human γ2 Human Cryo-EM 7VLA 7VLA_refined 2.7 CCR1 CCR1 CCR1 Chemokine A (Rhodopsin) Human - - - CCL15(27-92) (CCL15M)
Protein Agonist CCL3 (Mouse), CCL23 (Human), CCL8 (Human), CCL3 (Human), CCL7 (Rat), CCL7 (Human), CCL7 (Mouse), CCL5 (Mouse), CCL5 (Human), CCL13 (Human), CCL4 (Rat), CCL8 (Mouse), CCL16 (Human), CCL14 (Human), CCL3 (Rat), CCL4 (Mouse), CCL4 (Human), CCL15 (Human) Peptide Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H 10.1038/S41589-021-00918-Z 2022-03-23
Gi/o αi1 Human Wild-type human Gi heterotrimer 64 β1 Human γ2 Human Cryo-EM 7W0O 7W0O_refined 3.8 APJ APLNR apelin Apelin A (Rhodopsin) Human BRIL - - Elabela/Toddler-32 (Human) pubchem gtoplig uniprot
Peptide Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27
Gs αs Human Human mini-Gasstar, AHD restored, stabilizing muts 59 β1 Rat γ2 Bovine Cryo-EM 7VVJ 7VVJ_refined 3.2 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTHrP[1-36]
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αi1 Human WT human Gi1 heterotrimer, scFv16-stabilized 64 β1 Human γ2 Human Cryo-EM 7W0P 7W0P_refined 3.2 APJ APLNR apelin Apelin A (Rhodopsin) Human BRIL - - Elabela/Toddler-32 (Human) pubchem gtoplig uniprot
Peptide Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27
Gs αs Human Human mini-Gasstar: deletions/muts, stabilizer 58 β1 Rat γ2 Bovine Cryo-EM 7VVK - 3.3 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTH pubchem
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gs αs Human Human mini-Gsstar: stabilizing muts, ΔAHD 58 β1 Rat γ2 Bovine Cryo-EM 7VVL 7VVL_refined 2.8 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTH pubchem
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gs αs Human Mini-Gs (mini-Gasstar) 58 β1 Rat γ2 Bovine Cryo-EM 7VVM 7VVM_refined 3.2 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Parathyroid hormone
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gs αs Human Mini-Gs* (Gsstar): stabilizing mutations 58 β1 Rat γ2 Bovine Cryo-EM 7VVN 7VVN_refined 3.8 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTH pubchem
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gs αs Human Mini-Gs (mini-Gasstar) 58 β1 Rat γ2 Bovine Cryo-EM 7VVO 7VVO_refined 4.1 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTH pubchem
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Kobayashi K, Kawakami K, Kusakizako T, Miyauchi H, Tomita A, Kobayashi K, Shihoya W, Yamashita K, Nishizawa T, Kato HE, Inoue A, Nureki O 10.1016/J.MOLCEL.2022.07.003 2022-08-03
Gi/o αi1 Human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 7W0L 7W0L_refined 3.6 APJ APLNR apelin Apelin A (Rhodopsin) Human BRIL - - CHEMBL5812344 chembl_ligand pubchem
Small molecule Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27
Gi/o αo Human Engineered miniGαo1: H-domain deletion 60 β1 Human γ2 Human Cryo-EM 7W2Z 7W2Z_refined 2.8 GHSR GHSR ghrelin Ghrelin A (Rhodopsin) Human - - - Ghrelin pubchem
Small molecule Agonist [des-Gln14]ghrelin (Mouse), liver enriched antimicrobial peptide 2 (Human), ghrelin (Mouse), [des-Gln14]ghrelin (Human), ghrelin (Human) Peptide Qin J, Cai Y, Xu Z, Ming Q, Ji SY, Wu C, Zhang H, Mao C, Shen DD, Hirata K, Ma Y, Yan W, Zhang Y, Shao Z 10.1038/S41467-022-27975-9 2022-01-19
Gi/o αo Human GoA heterotrimer signaling complex 58 β1 Human γ2 Human Cryo-EM 7W6P - 3.5 ADA2A ADRA2A α2A Adrenoceptors A (Rhodopsin) Human - - - CHEMBL5542553 chembl_ligand pubchem
Small molecule Agonist (partial) (-)-noradrenaline, (-)-adrenaline Small molecule Fink EA, Xu J, Hubner H, Braz JM, Seemann P, Avet C, Craik V, Weikert D, Schmidt MF, Webb CM, Tolmachova NA, Moroz YS, Huang XP, Kalyanaraman C, Gahbauer S, Chen G, Liu Z, Jacobson MP, Irwin JJ, Bouvier M, Du Y, Shoichet BK, Basbaum AI, Gmeiner P 10.1126/SCIENCE.ABN7065 2022-09-28
Gi/o αo Human miniGo: engineered truncated Gαo subunit 60 β1 Human γ2 Human Cryo-EM 7UM6 - 2.8 5HT5A HTR5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - lisuride pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (partial) 5-hydroxytryptamine Small molecule Zhang S, Chen H, Zhang C, Yang Y, Popov P, Liu J, Krumm BE, Cao C, Kim K, Xiong Y, Katritch V, Shoichet BK, Jin J, Fay JF, Roth BL 10.1038/S41594-022-00796-6 2022-07-20
Gs αs Human G112: Gi1 N-term/AHD; G226A/L272D/A366S 60 β1 Rat γ2 Bovine Cryo-EM 7V9L - 2.6 GHRHR GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 LgBiT subunit
HiBiT subunit 		- None - GHRH (Mouse), GHRH (Rat), GHRH (Human) Peptide Cong Z, Zhou F, Zhang C, Zou X, Zhang H, Wang Y, Zhou Q, Cai X, Liu Q, Li J, Shao L, Mao C, Wang X, Wu J, Xia T, Zhao LH, Jiang H, Zhang Y, Xu HE, Cheng X, Yang D, Wang MW 10.1073/PNAS.2106606118 2022-04-06
Gs αs Human DNGαs: G226A/L272D/A366S; rat Gβ1/bo Gγ2 57 β1 Rat γ2 Bovine Cryo-EM 7V9M 7V9M_refined 3.3 GHRHR GHRHR GHRH Glucagon B1 (Secretin) Human - Nanobody-35 - GHRH (Human) pubchem gtoplig uniprot
Peptide Agonist GHRH (Mouse), GHRH (Rat), GHRH (Human) Peptide Cong Z, Zhou F, Zhang C, Zou X, Zhang H, Wang Y, Zhou Q, Cai X, Liu Q, Li J, Shao L, Mao C, Wang X, Wu J, Xia T, Zhao LH, Jiang H, Zhang Y, Xu HE, Cheng X, Yang D, Wang MW 10.1073/PNAS.2106606118 2021-10-20
Gs αs Human DN human Gs: 8 muts, limits G-protein dissociation 58 β1 Rat γ2 Bovine Cryo-EM 7VBI - 3.0 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Non-acylated tirzepatide
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhao F, Zhou Q, Cong Z, Hang K, Zou X, Zhang C, Chen Y, Dai A, Liang A, Ming Q, Wang M, Chen LN, Xu P, Chang R, Feng W, Xia T, Zhang Y, Wu B, Yang D, Zhao L, Xu HE, Wang MW 10.1038/S41467-022-28683-0 2022-03-02
Gi/o αi1 Human DN Gs (called DNGai1 in paper): G203A/A326S 62 β1 Rat γ2 Bovine Cryo-EM 7VGY - 3.1 MTR1A MTNR1A MT1 Melatonin A (Rhodopsin) Human - - - 2-iodo-melatonin pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist melatonin Small molecule Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y 10.1038/S41467-022-28111-3 2022-03-02
Gi/o αi1 Human DN G protein: G203A/A326S mutations 62 β1 Rat γ2 Bovine Cryo-EM 7VGZ 7VGZ_refined 3.3 MTR1A MTNR1A MT1 Melatonin A (Rhodopsin) Human - - - ramelteon pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist melatonin Small molecule Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y 10.1038/S41467-022-28111-3 2022-03-02
Gi/o αi1 Human DN Gs: G203A/A326S; γ subunit not modeled 61 β1 Rat - - Cryo-EM 7VH0 7VH0_refined 3.5 MTR1B MTNR1B MT2 Melatonin A (Rhodopsin) Human - - - ramelteon pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist melatonin Small molecule Wang Q, Lu Q, Guo Q, Teng M, Gong Q, Li X, Du Y, Liu Z, Tao Y 10.1038/S41467-022-28111-3 2022-03-02
Gi/o αi1 Human DN Gs: muts reduce nucleotide affinity 62 β1 Human γ2 Human Cryo-EM 7VL8 7VL8_refined 2.9 CCR1 CCR1 CCR1 Chemokine A (Rhodopsin) Human - - - - None - CCL3 (Mouse), CCL23 (Human), CCL8 (Human), CCL3 (Human), CCL7 (Rat), CCL7 (Human), CCL7 (Mouse), CCL5 (Mouse), CCL5 (Human), CCL13 (Human), CCL4 (Rat), CCL8 (Mouse), CCL16 (Human), CCL14 (Human), CCL3 (Rat), CCL4 (Mouse), CCL4 (Human), CCL15 (Human) Peptide Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H 10.1038/S41589-021-00918-Z 2022-03-23
Gi/o αi1 Human DN Gαi1, low nucleotide affinity; Gβ1-SmBiT 62 β1 Human γ2 Human Cryo-EM 7VL9 - 2.6 CCR1 CCR1 CCR1 Chemokine A (Rhodopsin) Human - - - CCL15(26-92)
Protein Agonist CCL3 (Mouse), CCL23 (Human), CCL8 (Human), CCL3 (Human), CCL7 (Rat), CCL7 (Human), CCL7 (Mouse), CCL5 (Mouse), CCL5 (Human), CCL13 (Human), CCL4 (Rat), CCL8 (Mouse), CCL16 (Human), CCL14 (Human), CCL3 (Rat), CCL4 (Mouse), CCL4 (Human), CCL15 (Human) Peptide Shao Z, Shen Q, Yao B, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Ma H, Chen ZH, Xu HE, Ying S, Zhang Y, Shen H 10.1038/S41589-021-00918-Z 2022-03-23
Gi/o αi1 Human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 7VUG 7VUG_refined 3.2 GP139 GPR139 GPR139 Orphan A (Rhodopsin) Human - - Endo-1
4-beta-xylanase 		JNJ-63533054 pubchem gtoplig chembl_ligand
Small molecule Agonist D-tryptophan, D-phenylalanine Small molecule Zhou Y, Daver H, Trapkov B, Wu L, Wu M, Harpsoe K, Gentry PR, Liu K, Larionova M, Liu J, Chen N, Brauner-Osborne H, Gloriam DE, Hua T, Liu ZJ 10.1038/S41422-021-00591-W 2021-12-29
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 7VV3 - 3.0 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human BRIL - - - None - PAMP-20 (Human) Peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gi/o αi1 Human DN human Gαi1: S47N/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 7VV5 7VV5_refined 2.8 MRGX2 MRGPRX2 MRGPRX2 Orphan A (Rhodopsin) Human BRIL - - compound 48/80 pubchem gtoplig
Small molecule Agonist PAMP-20 (Human) Peptide Yang F, Guo L, Li Y, Wang G, Wang J, Zhang C, Fang GX, Chen X, Liu L, Yan X, Liu Q, Qu C, Xu Y, Xiao P, Zhu Z, Li Z, Zhou J, Yu X, Gao N, Sun JP 10.1038/S41586-021-04077-Y 2021-12-01
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 7W0M 7W0M_refined 3.7 APJ APLNR apelin Apelin A (Rhodopsin) Human BRIL - - CHEMBL5812344 chembl_ligand pubchem
Small molecule Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27
Gi/o αi1 Human Gi1 heterotrimer complex 64 β1 Human γ2 Human Cryo-EM 7W0N - 4.2 APJ APLNR apelin Apelin A (Rhodopsin) Human BRIL - - Elabela/Toddler-32 (Human) pubchem gtoplig uniprot
Peptide Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Yue Y, Liu L, Wu LJ, Wu Y, Wang L, Li F, Liu J, Han GW, Chen B, Lin X, Brouillette RL, Breault E, Longpre JM, Shi S, Lei H, Sarret P, Stevens RC, Hanson MA, Xu F 10.1038/S41594-022-00797-5 2022-07-27
Gi/o αi1 Human DN Gαi1 (DNGαi1) 64 β1 Rat γ2 Bovine Cryo-EM 7WIC - 2.8 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - - SOMATOSTATIN chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C 10.1038/S41422-022-00669-Z 2022-06-01
Gs αs Human DN miniGs: multiple muts, AHD deleted 53 β1 Human γ2 Human Cryo-EM 7WU2 - 2.8 AGRD1 ADGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - Nanobody-35 - - None - dihydrotestosterone Small molecule Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gi/o αi1 Human MiniGi1: G42D/E43N + 5 more muts, ΔAHD 58 β1 Human γ2 Human Cryo-EM 7WU4 - 3.4 AGRF1 ADGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - - - LPC 16:0
Lipid PAM - - Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C, Han S, Shui W, Zhao Q, Wu B 10.1038/S41586-022-04580-W 2022-04-27
Gs αs Human DNGs: 8 stabilizing mutations 60 β1 Human γ2 Human Cryo-EM 7WCM 7WCM_refined 2.3 GP119 GPR119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human BRIL Nanobody-35 - MBX-2982 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide Small molecule Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A 10.1038/S41467-022-34696-6 2022-12-21
Gs αs Human DNGs: 8 point mutations 60 β1 Human γ2 Human Cryo-EM 7WCN 7WCN_refined 2.9 GP119 GPR119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - AR231453 pubchem gtoplig chembl_ligand
Small molecule Agonist SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide Small molecule Qian Y, Wang J, Yang L, Liu Y, Wang L, Liu W, Lin Y, Yang H, Ma L, Ye S, Wu S, Qiao A 10.1038/S41467-022-34696-6 2022-12-21
Gi/o αi1 Human DN Gαi1: G203A/A326S; S1PR1 F133W stabilizer 40 β1 Human γ2 Human Cryo-EM 7WF7 7WF7_refined 3.4 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human - - LgBiT
HiBiT 		sphingosine 1-phosphate pubchem gtoplig chembl_ligand
Lipid Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Xu Z, Ikuta T, Kawakami K, Kise R, Qian Y, Xia R, Sun MX, Zhang A, Guo C, Cai XH, Huang Z, Inoue A, He Y 10.1038/S41589-021-00930-3 2022-01-05
Gi/o αi1 Human DN Gαi1 (DNGαi1) 64 β1 Rat γ2 Bovine Cryo-EM 7WIG 7WIG_refined 2.7 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - - CHEMBL69303 chembl_ligand pubchem pubchem
Small molecule Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Chen LN, Wang WW, Dong YJ, Shen DD, Guo J, Yu X, Qin J, Ji SY, Zhang H, Shen Q, He Q, Yang B, Zhang Y, Li Q, Mao C 10.1038/S41422-022-00669-Z 2022-06-01
Gi/o αi1 Human Gi heterotrimer, designed per Kim et al. 2020 60 β1 Human γ2 Human Cryo-EM 7WJ5 7WJ5_refined 3.7 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human BRIL - - SOMATOSTATIN chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Heo Y, Yoon E, Jeon YE, Yun JH, Ishimoto N, Woo H, Park SY, Song JJ, Lee W 10.7554/ELIFE.76823 2022-07-13
Gi/o αi1 Human Gαi1: 4 DN muts S47N/G203A/E245A/A326S 64 β1 Rat γ2 Bovine Cryo-EM 7WQ3 7WQ3_refined 2.7 GALR1 GALR1 GAL1 Galanin A (Rhodopsin) Human - - - galanin(1-13)amide gtoplig pubchem
Peptide Agonist galanin-like peptide (Human), spexin-1 (Human), galanin (Human), galanin-like peptide (Mouse) Protein Duan J, Shen DD, Zhao T, Guo S, He X, Yin W, Xu P, Ji Y, Chen LN, Liu J, Zhang H, Liu Q, Shi Y, Cheng X, Jiang H, Eric Xu H, Zhang Y, Xie X, Jiang Y 10.1038/S41467-022-29072-3 2022-04-20
Gi/o αi1 Human - 38 β1 Human γ2 Human Cryo-EM 7WU9 7WU9_refined 3.4 PE2R3 PTGER3 EP3 Prostanoid A (Rhodopsin) Human - - - - None - PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Suno R, Sugita Y, Morimoto K, Takazaki H, Tsujimoto H, Hirose M, Suno-Ikeda C, Nomura N, Hino T, Inoue A, Iwasaki K, Kato T, Iwata S, Kobayashi T 10.1016/J.CELREP.2022.111323 2022-08-17
Gs αs Human Human mini-Gs: αN from Gαi1, for Nb35/scFv16 59 β1 Human γ2 Human Cryo-EM 7WUJ - 3.3 AGRG4 ADGRG4 ADGRG4 ADGRG B2 (Adhesion) Human - Nanobody-35 - - - - - - Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27
Gs αs Human DN short Gs (DNGs): S54N/G226A +6 more muts 55 β1 Human γ2 Human Cryo-EM 7WUQ - 2.9 AGRG2 Adgrg2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 mCherry - None - - - Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN, Yang CC, Li Y, Gong Z, Tao XN, Yang ZS, Lu Y, Li SL, He JY, Wang C, Zhang L, Kong L, Sun JP, Yu X 10.1038/S41586-022-04590-8 2022-04-27
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/A326S/E45A 62 β1 Human γ2 Human Cryo-EM 7WVU 7WVU_refined 3.3 FPR1 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - - - fMet-Leu-Phe pubchem gtoplig chembl_ligand
Peptide Agonist spinorphin (Human), cathepsin G (Rat), fMet-Leu-Phe-Ile-Ile, annexin I-(2-26) (Human), mitochondrial peptde fMMYALF, mitochondrial peptide fMFADRW, fMet-Leu-Phe, annexin I (Rat), annexin I (Mouse), cathepsin G (Mouse), cathepsin G (Human), annexin I (Human) Peptide Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B 10.1038/S41467-022-29361-X 2022-04-13
Gi/o αi2 Human DN Gαi2: S47N/G204A/A327S/E246A 63 β1 Human γ2 Human Cryo-EM 7WVV 7WVV_refined 2.9 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - N-formyl-MLFII (fM5)
Peptide Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B 10.1038/S41467-022-29361-X 2022-04-13
Gi/o αi2 Human DN Gαi2: S47N/G204A/A327S/E246A 63 β1 Human γ2 Human Cryo-EM 7WVW - 3.1 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - fM9
Peptide Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B 10.1038/S41467-022-29361-X 2022-04-13
Gs αs Human Mini-Gs: AHD deleted, stabilizing mutations 59 β1 Human γ2 Human Cryo-EM 7WXW - 2.8 AGRF1 ADGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - Nanobody-35 - - None - - - Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y 10.1038/S41467-022-33173-4 2022-09-28
G12/13 α13 Human Gα13/Gi chimera: Gi N-term & AHD, scFv16 55 β1 Human γ2 Human Cryo-EM 7WY0 - 2.8 AGRF1 ADGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - - - - - - - - Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y 10.1038/S41467-022-33173-4 2022-09-28
Gs αs Human Mini-Gαs (mini-Gas), AHD deleted 59 β1 Human γ2 Human Cryo-EM 7WY8 - 2.8 AGRL3 Adgrl3 ADGRL3 ADGRL B2 (Adhesion) Mouse - Nanobody-35 LgBiT
HiBiT 		- - - - - Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y 10.1016/J.MOLCEL.2022.10.009 2022-10-26
G12/13 α12 Human Gα12/Gαi chimera: N-term/AHD from Gαi 55 β1 Human γ2 Human Cryo-EM 7WZ7 - 2.8 AGRF1 ADGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - - - - - - - - Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y 10.1038/S41467-022-33173-4 2022-09-28
G12/13 α12 Human mini-G12/i chimera: Gαi AHD replaces G12 AHD 55 β1 Human γ2 Human Cryo-EM 7X10 - 2.9 AGRL3 Adgrl3 ADGRL3 ADGRL B2 (Adhesion) Mouse - - - - - - - - Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y 10.1016/J.MOLCEL.2022.10.009 2022-11-09
Gs αs Human Mini-Gs, GPCR-truncated Gα subunit 58 β1 Human γ2 Human Cryo-EM 7X2F 7X2F_refined 3.0 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
mevidalen pubchem gtoplig chembl_ligand pubchem
Small molecule
Small molecule 		Agonist
PAM 		5-hydroxytryptamine, noradrenaline, dopamine Small molecule Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S 10.1038/S41467-022-30929-W 2022-06-15
Gi/o αi1 Human DN Gi1: G203A/A326S 62 β1 Human γ2 Human Cryo-EM 7X2V - 3.1 AGRF1 ADGRF1 ADGRF1 ADGRF B2 (Adhesion) Human - - - - - - - - Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C, Wang G, He Y 10.1038/S41467-022-33173-4 2022-09-28
Gi/o αi1 Human DN Gαi1(4DN): S47N/G203A/E345A/A326S 63 β1 Human γ2 Human Cryo-EM 7X5H 7X5H_refined 3.1 5HT5A HTR5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		5-CT pubchem gtoplig chembl_ligand
Small molecule Agonist 5-hydroxytryptamine Small molecule Tan Y, Xu P, Huang S, Yang G, Zhou F, He X, Ma H, Xu HE, Jiang Y 10.1038/S41421-022-00412-3 2022-09-14
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S/E245A 61 β1 Human γ2 Human Cryo-EM 7X9A 7X9A_refined 3.2 NPY1R NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human - - - NEUROPEPTIDE-Y chembl_ligand pubchem
Protein Agonist neuropeptide Y (Human), pancreatic polypeptide (Human), peptide YY (Human), pancreatic polypeptide (Mouse), peptide YY (Mouse) Peptide Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B 10.1126/SCIADV.ABM1232 2022-05-18
Gs αs Human Mini-Gs protein 59 β1 Rat γ2 Bovine Cryo-EM 7XJH - 3.3 ADRB3 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog - Nanobody-35 - LEVISOPRENALINE chembl_ligand pubchem drug_central
Small molecule Agonist - - Nagiri C, Kobayashi K, Tomita A, Kato M, Kobayashi K, Yamashita K, Nishizawa T, Inoue A, Shihoya W, Nureki O 10.1016/J.MOLCEL.2021.06.024 2022-05-04
Gs αs Human Stabilized Gs: mini-Gs with AHD reverted 59 β1 Rat γ2 Bovine Cryo-EM 7XJI - 3.9 ADRB3 ADRB3 β3 Adrenoceptors A (Rhodopsin) Dog - Nanobody-35 - Solabegron pubchem
Small molecule Agonist - - Nureki I, Kobayashi K, Tanaka T, Demura K, Inoue A, Shihoya W, Nureki O 10.1016/J.BBRC.2022.04.065 2022-05-04
Gi/o αo Human Thermostable miniGαo: αN from Gαi1, scFv16 61 β1 Human γ2 Human Cryo-EM 7XJJ 7XJJ_refined 3.3 GALR1 GALR1 GAL1 Galanin A (Rhodopsin) Human - - - galanin(1-13)amide gtoplig pubchem
Peptide Agonist galanin-like peptide (Human), spexin-1 (Human), galanin (Human), galanin-like peptide (Mouse) Protein - - 2023-05-03
Gi/o αi1 Human Native human Gi1 heterotrimer 63 β1 Human γ2 Human Cryo-EM 7XK2 7XK2_refined 3.1 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - MK 6892 pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Yang Y, Kang HJ, Gao R, Wang J, Han GW, DiBerto JF, Wu L, Tong J, Qu L, Wu Y, Pileski R, Li X, Zhang XC, Zhao S, Kenakin T, Wang Q, Stevens RC, Peng W, Roth BL, Rao Z, Liu ZJ 10.1038/S41467-023-37177-6 2023-02-22
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 7XK8 7XK8_refined 3.3 NMUR2 NMUR2 NMU2 Neuromedin U A (Rhodopsin) Human - - - CHEMBL3315349 chembl_ligand pubchem
Protein Agonist neuromedin U-25 (Human), neuromedin S-36 (Mouse), neuromedin S-36 (Rat), neuromedin S-33 (Human), neuromedin U-23 (Rat) Peptide Zhao W, Zhang W, Wang M, Lu M, Chen S, Tang T, Schnapp G, Wagner H, Brennauer A, Yi C, Chu X, Han S, Wu B, Zhao Q 10.1038/S41467-022-34814-4 2023-02-22
Gs αs Human DNGs: dominant-negative Gs protein 57 β1 Human γ2 Human Cryo-EM 7XKD - 2.4 AGRG2 Adgrg2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - PRASTERONE chembl_ligand pubchem drugbank
Small molecule Agonist (partial) - - Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X 10.1038/S41589-022-01084-6 2022-08-10
Gs αs Human Mini-Gs protein 60 β1 Human γ2 Human Cryo-EM 7XKE - 2.9 AGRG2 Adgrg2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - PRASTERONE chembl_ligand pubchem drugbank
Small molecule Agonist - - Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X 10.1038/S41589-022-01084-6 2022-08-10
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 7XMR 7XMR_refined 3.1 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - - SOMATOSTATIN chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q 10.1038/S41422-022-00679-X 2022-08-03
Gs αs Human DN human Gs (DNGs) via mutagenesis 58 β1 Human γ2 Human Cryo-EM 7XOV - 3.0 CCKAR CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - Nanobody-35 - SR146131 pubchem gtoplig chembl_ligand
Small molecule Agonist gastrin-17 (Human), CCK-33 (Mouse), CCK-4 (Human), CCK-8 (Human), CCK-33 (Human), gastrin-17 (Rat), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM 10.1038/S41421-022-00420-3 2022-07-20
Gs αs Human DN Gs: 8 muts S54N/G226A/E268A...I285T 60 β1 Human γ2 Human Cryo-EM 7XT8 - 3.1 5HT4R HTR4 5-HT4 5-Hydroxytryptamine A (Rhodopsin) Human BRIL Nanobody-35 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist 5-hydroxytryptamine Small molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gi/o αi1 Human DN Gαi1: S54N/G226A +6 more mutations 62 β1 Human γ2 Human Cryo-EM 7XTA 7XTA_refined 3.2 5HT4R HTR4 5-HT4 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist 5-hydroxytryptamine Small molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gs αs Human DN Gs-short isoform: 8 stabilizing mutations 60 β1 Human γ2 Human Cryo-EM 7XTB 7XTB_refined 3.3 5HT6R HTR6 5-HT6 5-Hydroxytryptamine A (Rhodopsin) Human BRIL Nanobody-35 - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist 5-hydroxytryptamine Small molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gs αs Human DN Gs: 8 muts S54N/G226A/E268A...I285T 61 β1 Human γ2 Human Cryo-EM 7XTC 7XTC_refined 3.2 5HT7R HTR7 5-HT7 5-Hydroxytryptamine A (Rhodopsin) Human BRIL Nanobody-35 - 5-CT pubchem gtoplig chembl_ligand
Small molecule Agonist 5-hydroxytryptamine Small molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gs αs Human Human Gαs subunit, short isoform 58 β1 Human γ2 Human Cryo-EM 7XTQ 7XTQ_refined 3.2 GPBAR GPBAR1 GPBA Bile acid A (Rhodopsin) Human - Nanobody-35 - CHEMBL2181246 chembl_ligand pubchem
Small molecule Agonist lithocholic acid, deoxycholic acid, cholic acid, chenodeoxycholic acid Small molecule Ma L, Yang F, Wu X, Mao C, Guo L, Miao T, Zang SK, Jiang X, Shen DD, Wei T, Zhou H, Wei Q, Li S, Shu Q, Feng S, Jiang C, Chu B, Du L, Sun JP, Yu X, Zhang Y, Zhang P 10.1073/PNAS.2117054119 2022-07-06
Gs αs Human Mini-Gs: G226A/A366S/L272D mutations 60 β1 Human γ2 Human Cryo-EM 7XW5 - 3.0 TSHR TSHR TSH Glycoprotein hormone A (Rhodopsin) Human - Nanobody-35 - Thyrotropin (TSH) (chain X)
Thyrotropin (TSH) (chain Y)
ML-109 pubchem
Protein
Protein
Small molecule 		Agonist TSH (Rat), TSH (Human), TSH (Mouse) Peptide Duan J, Xu P, Luan X, Ji Y, He X, Song N, Yuan Q, Jin Y, Cheng X, Jiang H, Zheng J, Zhang S, Jiang Y, Xu HE 10.1038/S41586-022-05173-3 2022-08-24
Gs αs Human Mini-Gs: αN from Gαi1, scFv16; Gβ1-SmBiT 57 β1 Human γ2 Human Cryo-EM 7XY7 - 3.3 AA2BR ADORA2B A2B Adenosine A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		NECA pubchem gtoplig chembl_ligand
Small molecule Agonist adenosine Small molecule Chen Y, Zhang J, Weng Y, Xu Y, Lu W, Liu W, Liu M, Hua T, Song G 10.1126/SCIADV.ADD3709 2023-05-03
Gs αs Human DNGαs: 8 muts incl S54N/G226A/E268A 60 β1 Human γ2 Human Cryo-EM 7XZ5 - 3.1 GP119 GPR119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human BRIL Nanobody-35 - Lysophosphatidylcholine 18:1 pubchem
Lipid Agonist SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide Small molecule Xu P, Huang S, Guo S, Yun Y, Cheng X, He X, Cai P, Lan Y, Zhou H, Jiang H, Jiang Y, Xie X, Xu HE 10.1038/S41594-022-00816-5 2022-08-24
Gs αs Human DN Gs: 8 muts S54N/G226A/E268A...I285T 60 β1 Human γ2 Human Cryo-EM 7XZ6 - 2.8 GP119 GPR119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human BRIL Nanobody-35 - APD668 pubchem gtoplig chembl_ligand
Small molecule Agonist SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide Small molecule Xu P, Huang S, Guo S, Yun Y, Cheng X, He X, Cai P, Lan Y, Zhou H, Jiang H, Jiang Y, Xie X, Xu HE 10.1038/S41594-022-00816-5 2022-08-24
Gi/o αi1 Human DN Gi: G203A/A326S 62 β1 Mouse γ2 Mouse Cryo-EM 7Y12 - 3.1 MRGRD MRGPRD MRGPRD Orphan A (Rhodopsin) Human BRIL - - β-alanine pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist β-alanine Small molecule Suzuki S, Iida M, Hiroaki Y, Tanaka K, Kawamoto A, Kato T, Oshima A 10.1038/S42003-022-03668-3 2022-07-20
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 7Y64 - 2.9 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - - C5a anaphylatoxin
Protein Agonist C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z 10.1038/S41422-023-00779-2 2023-03-01
Gi/o αi1 Human G protein with N-terminal MYC epitope tag 64 β1 Human γ2 Human Cryo-EM 7Y65 - 3.2 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - - C5aPEP
Small molecule Agonist C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z 10.1038/S41422-023-00779-2 2023-03-01
Gi/o αi1 Human DN Gi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 7Y66 - 2.9 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - - BM213 pubchem
Peptide Agonist C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z 10.1038/S41422-023-00779-2 2023-03-01
Gi/o αi1 Human DN Gi: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 7Y67 7Y67_refined 2.8 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - - C089
Peptide Agonist C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide Feng Y, Zhao C, Deng Y, Wang H, Ma L, Liu S, Tian X, Wang B, Bin Y, Chen P, Yan W, Fu P, Shao Z 10.1038/S41422-023-00779-2 2023-03-01
Gi/o αi1 Human DNGai1: G203A/A326S 58 β1 Human γ2 Human Cryo-EM 7Y89 - 3.0 GPR17 GPR17 GPR17 Orphan A (Rhodopsin) Human - - - - None - UDP, UDP-galactose, ATP, LTD4, LTC4, LTE4, UDP-glucose Small molecule Ye F, Wong TS, Chen G, Zhang Z, Zhang B, Gan S, Gao W, Li J, Wu Z, Pan X, Du Y 10.1002/MCO2.159 2022-10-12
Gi/o αi1 Human DN human Gαi1: S47N/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 7YAE 7YAE_refined 3.4 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - - octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z 10.1038/S41467-023-36673-Z 2023-04-19
Gi/o αi1 Human DN Gs: S47N/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 7YAC 7YAC_refined 3.2 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - - paltusotine pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem
Small molecule Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Zhao J, Fu H, Yu J, Hong W, Tian X, Qi J, Sun S, Zhao C, Wu C, Xu Z, Cheng L, Chai R, Yan W, Wei X, Shao Z 10.1038/S41467-023-36673-Z 2023-04-19
G12/13 α12 Human Mini-G12: Gαi1 scaffold + Gα12 α5 helix 55 β1 Human γ2 Human Cryo-EM 7YDJ - 3.0 AGRE5 ADGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - - - - None - - - - - 2023-07-12
Gi/o αi2 Human DN human Gαi2: S47N/G204A/E246A/A327S 59 β1 Human γ2 Bovine Cryo-EM 7YK6 7YK6_refined 3.0 RL3R2 RXFP4 RXFP4 Relaxin family peptide A (Rhodopsin) Human BRIL - LgBiT CHEMBL4522365 chembl_ligand pubchem
Small molecule Agonist relaxin-3 (B chain) (Human), relaxin-3 (Human), INSL5 (Human) Peptide Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW 10.1038/S41467-023-36182-Z 2023-03-01
Gi/o αi2 Human DNGi2: S47N/G204A/E246A/A327S 61 β1 Human γ2 Bovine Cryo-EM 7YK7 7YK7_refined 2.8 RL3R2 RXFP4 RXFP4 Relaxin family peptide A (Rhodopsin) Human BRIL - - DC591053 pubchem gtoplig
Small molecule Agonist relaxin-3 (B chain) (Human), relaxin-3 (Human), INSL5 (Human) Peptide Chen Y, Zhou Q, Wang J, Xu Y, Wang Y, Yan J, Wang Y, Zhu Q, Zhao F, Li C, Chen CW, Cai X, Bathgate RAD, Shen C, Eric Xu H, Yang D, Liu H, Wang MW 10.1038/S41467-023-36182-Z 2023-03-01
Gs αs Human Gs-short heterotrimer 59 β1 Human γ2 Human Cryo-EM 7YP7 - 3.1 AGRG2 Adgrg2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - - None - - - - - 2022-08-24
Gs αs Human DN Gs: N-term replaced by Gαi1, for scFv16 59 β1 Human γ2 Human Cryo-EM 7YS6 7YS6_refined 3.0 5HT6R HTR6 5-HT6 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist 5-hydroxytryptamine Small molecule - - 2023-03-29
Gi/o αi1 Human WT Gi: human Gαi1, rat Gβ1, bovine Gγ2 63 β1 Rat γ2 Bovine Cryo-EM 7YU3 7YU3_refined 3.4 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - ONO-0740556 pubchem
Small molecule Agonist LPA Small molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αi1 Human Gi heterotrimer complex 63 β1 Rat γ2 Bovine Cryo-EM 7YU5 7YU5_refined 3.3 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - ONO-0740556 pubchem
Small molecule Agonist LPA Small molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αi1 Human Gi1(human)/Gβ1(rat)/Gγ2(bovine) heterotrimer 63 β1 Rat γ2 Bovine Cryo-EM 7YU6 7YU6_refined 3.5 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - ONO-0740556 pubchem
Small molecule Agonist LPA Small molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αi1 Human Gαi1(human)/Gβ1(rat)/Gγ2(bovine, C68S mutation) 63 β1 Rat γ2 Bovine Cryo-EM 7YU7 - 3.8 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - ONO-0740556 pubchem
Small molecule Agonist LPA Small molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αi1 Human WT human Gαi1, rat Gβ1, bovine Gγ2 63 β1 Rat γ2 Bovine Cryo-EM 7YU8 - 4.5 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human - - - ONO-0740556 pubchem
Small molecule Agonist LPA Small molecule Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O 10.1038/S41467-022-33121-2 2022-10-05
Gi/o αi2 Human DN Gαi2: S47N/G204A/A327S/E246A 61 β1 Human γ2 Human Cryo-EM 7WVX - 2.8 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - fhumanin
Peptide Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide Zhu Y, Lin X, Zong X, Han S, Wang M, Su Y, Ma L, Chu X, Yi C, Zhao Q, Wu B 10.1038/S41467-022-29361-X 2022-04-13
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S/E245A; Gβ-HiBiT 64 β1 Human γ2 Human Cryo-EM 7WYB - 3.0 AGRL3 Adgrl3 ADGRL3 ADGRL B2 (Adhesion) Mouse - - LgBiT - - - - - Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y, Yin H, Xiong Y, Zhang A, Guo C, Chen Z, Huang Z, He Y 10.1016/J.MOLCEL.2022.10.009 2022-10-26
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 7WZ4 - 3.0 GPR88 GPR88 GPR88 Orphan A (Rhodopsin) Human BRIL - - - None - - - Chen G, Xu J, Inoue A, Schmidt MF, Bai C, Lu Q, Gmeiner P, Liu Z, Du Y 10.1038/S41467-022-30081-5 2022-10-26
Gs αs Human Mini-Gs399: truncated version of Gs 58 β1 Human γ2 Human Cryo-EM 7X2D 7X2D_refined 3.3 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - tavapadon pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Teng X, Chen S, Nie Y, Xiao P, Yu X, Shao Z, Zheng S 10.1038/S41467-022-30929-W 2022-06-15
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S/E245A 62 β1 Human γ2 Human Cryo-EM 7X9B 7X9B_refined 3.4 NPY2R NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human - - - NEUROPEPTIDE-Y chembl_ligand pubchem
Protein Agonist neuropeptide Y (Human), neuropeptide Y-(3-36) (Human), pancreatic polypeptide (Rat), pancreatic polypeptide (Human), peptide YY (Human), pancreatic polypeptide (Mouse), PYY-(3-36) (Human), peptide YY (Mouse) Peptide Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B 10.1126/SCIADV.ABM1232 2022-05-18
Gi/o αi1 Human DN human Gαi1: S47C/G202T/G203A/A326S/E245A 61 β1 Human γ2 Human Cryo-EM 7X9C 7X9C_refined 3.0 NPY4R NPY4R Y4 Neuropeptide Y A (Rhodopsin) Human - - - PANCREATIC POLYPEPTIDE chembl_ligand pubchem
Protein Agonist PYY-(3-36) (Mouse), neuropeptide Y (Human), pancreatic polypeptide (Human), peptide YY (Human), pancreatic polypeptide (Mouse), peptide YY (Mouse) Peptide Tang T, Tan Q, Han S, Diemar A, Lobner K, Wang H, Schuss C, Behr V, Morl K, Wang M, Chu X, Yi C, Keller M, Kofoed J, Reedtz-Runge S, Kaiser A, Beck-Sickinger AG, Zhao Q, Wu B 10.1126/SCIADV.ABM1232 2022-05-18
Gi/o αi1 Human Human Gi1/Gβ1/Gγ2; Gβ1 has peptide86-NanoBiT tag 62 β1 Human γ2 Human Cryo-EM 7X9Y 7X9Y_refined 3.1 CCR3 CCR3 CCR3 Chemokine A (Rhodopsin) Human - - - - None - CCL24 (Mouse), CXCL10 (Mouse), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CCL11 (Rat), CCL11 (Mouse), CCL8 (Human), CXCL10 (Human), CCL2 (Rat), CCL5 (Mouse), CCL5 (Human), CCL28 (Mouse), CXCL9 (Human), CCL24 (Human), CXCL9 (Mouse), CCL7 (Rat), CCL11 (Human), CCL28 (Human), CCL2 (Human), CCL26 (Human), CCL8 (Mouse), CCL7 (Mouse), CCL2 (Mouse), CXCL11 (Human), CCL15 (Human) Peptide Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H 10.1038/S41421-022-00403-4 2022-08-24
Gi/o αi1 Human Gi1 heterotrimer; receptor-LgBiT/MBP, scFv16 65 β1 Human γ2 Human Cryo-EM 7XA3 7XA3_refined 2.9 CCR2 CCR2 CCR2 Chemokine A (Rhodopsin) Human - - - C-C motif chemokine 2 (CCL2)
Protein Agonist CCL24 (Human), CCL8 (Human), CCL2 (Rat), CCL7 (Rat), CCL11 (Human), CCL7 (Human), CCL2 (Human), CCL26 (Human), CCL13 (Human), CCL8 (Mouse), CCL11 (Rat), CCL16 (Human), CCL7 (Mouse), CCL2 (Mouse), CCL11 (Mouse) Peptide Shao Z, Tan Y, Shen Q, Hou L, Yao B, Qin J, Xu P, Mao C, Chen LN, Zhang H, Shen DD, Zhang C, Li W, Du X, Li F, Chen ZH, Jiang Y, Xu HE, Ying S, Ma H, Zhang Y, Shen H 10.1038/S41421-022-00403-4 2022-08-24
Gi/o αi1 Human DN Gαi1: G203A/A326S; Gβ1-HiBiT fusion 63 β1 Bovine γ2 Bovine Cryo-EM 7XAT 7XAT_refined 2.9 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - LargeBit
HiBiT 		SOMATOSTATIN chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide - - 2022-08-31
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 63 β1 Bovine γ2 Bovine Cryo-EM 7XAU - 3.0 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - LargeBit octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41421-022-00405-2 2022-08-31
Gi/o αi1 Human DN Gαi1: G203A/A326S 63 β1 Bovine γ2 Bovine Cryo-EM 7XAV 7XAV_refined 2.9 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - LargeBit LANREOTIDE chembl_ligand pubchem pubchem drugbank
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Bo Q, Yang F, Li Y, Meng X, Zhang H, Zhou Y, Ling S, Sun D, Lv P, Liu L, Shi P, Tian C 10.1038/S41421-022-00405-2 2022-08-31
Gs αs Human DNGs: dominant-negative Gs protein 57 β1 Human γ2 Human Cryo-EM 7XKF - 2.4 AGRG2 Adgrg2 ADGRG2 ADGRG B2 (Adhesion) Mouse - Nanobody-35 - PRASTERONE chembl_ligand pubchem drugbank
Small molecule Agonist - - Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C, Ping YQ, Zhao RJ, Ma CS, Liu CH, Zhang XN, Jiang D, Huang S, Xi YT, Zhang DL, Xue CY, Yang BS, Li JY, Lin HC, Zeng XH, Zhao H, Xu WM, Yi F, Liu Z, Sun JP, Yu X 10.1038/S41589-022-01084-6 2022-08-10
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 7XMS - 2.9 SSR4 SSTR4 SST4 Somatostatin A (Rhodopsin) Human - - - SOMATOSTATIN chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q 10.1038/S41422-022-00679-X 2022-08-03
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 7XMT 7XMT_refined 2.8 SSR4 SSTR4 SST4 Somatostatin A (Rhodopsin) Human - - - J-2156 pubchem gtoplig chembl_ligand
Small molecule Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Zhao W, Han S, Qiu N, Feng W, Lu M, Zhang W, Wang M, Zhou Q, Chen S, Xu W, Du J, Chu X, Yi C, Dai A, Hu L, Shen MY, Sun Y, Zhang Q, Ma Y, Zhong W, Yang D, Wang MW, Wu B, Zhao Q 10.1038/S41422-022-00679-X 2022-08-03
Gs αs Human DNGs: mutation limits G protein dissociation 58 β1 Human γ2 Human Cryo-EM 7XOU - 3.2 CCKAR CCKAR CCK1 Cholecystokinin A (Rhodopsin) Human - Nanobody-35 - CCK-8 (Human) pubchem gtoplig chembl_ligand drug_central uniprot uniprot uniprot drugbank pubchem
Peptide Agonist gastrin-17 (Human), CCK-33 (Mouse), CCK-4 (Human), CCK-8 (Human), CCK-33 (Human), gastrin-17 (Rat), CCK-58 (Human), desulfated cholecystokinin-8, gastrin-17 (Mouse), CCK-33 (Rat), CCK-39 (Human) Peptide Ding Y, Zhang H, Liao YY, Chen LN, Ji SY, Qin J, Mao C, Shen DD, Lin L, Wang H, Zhang Y, Li XM 10.1038/S41421-022-00420-3 2022-07-20
Gs αs Human DN Gs-short: S54N/G226A +6 more mutations 60 β1 Human γ2 Human Cryo-EM 7XT9 - 3.2 5HT4R HTR4 5-HT4 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - 5-hydroxytryptamine pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist 5-hydroxytryptamine Small molecule Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE 10.1016/J.MOLCEL.2022.05.031 2022-07-27
Gi/o αi2 Human - 61 β1 Human γ2 Human Cryo-EM 7XXI 7XXI_refined 3.0 P2Y12 P2RY12 P2Y12 P2Y A (Rhodopsin) Human - - - 2MeSADP pubchem gtoplig chembl_ligand
Small molecule Agonist ADP, ATP Small molecule - - 2023-06-07
Gi/o αi1 Human Gi1 heterotrimer, wild-type subunits 61 β1 Human γ2 Human Cryo-EM 7Y1F 7Y1F_refined 3.3 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - Dynorphin A13 pubchem
Small molecule Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Chen Y, Chen B, Wu T, Zhou F, Xu F 10.1093/PROCEL/PWAC033 2023-05-24
Gi/o αo Human Mini-Gαo subunit, truncated 60 β1 Human γ2 Human Cryo-EM 7Y24 - 3.3 SSR2 SSTR2 SST2 Somatostatin A (Rhodopsin) Human - - - octreotide pubchem gtoplig chembl_ligand drugbank pubchem pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Chen S, Teng X, Zheng S 10.1038/S41589-022-01130-3 2022-10-19
Gs αs Human Gs heterotrimer 57 β1 Rat γ2 Bovine Cryo-EM 7Y35 - 2.9 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - abaloparatide drug_central pubchem
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide - - 2023-07-05
Gs αs Human Human Gαs-short, rat Gβ1, bovine Gγ2 57 β1 Rat γ2 Bovine Cryo-EM 7Y36 - 2.8 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTH pubchem
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide - - 2023-07-05
Gs αs Human DNGas: 8 thermostable mutations 56 β1 Human γ2 Human Cryo-EM 7Y3G 7Y3G_refined 2.8 GPR12 GPR12 GPR12 Orphan A (Rhodopsin) Human - Nanobody-35 - - None - sphingosine 1-phosphate Lipid Li H, Zhang J, Yu Y, Luo F, Wu L, Liu J, Chen N, Liu Z, Hua T 10.1016/J.SCIB.2022.12.023 2023-06-07
G12/13 α13 Human Gi2-miniG13 chimera: Gi2 backbone, G13 α5 57 β1 Human γ2 Human Cryo-EM 7YDH - 3.1 AGRE5 ADGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - - - - None - - - Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
Gs αs Human MiniGs/Gi1 chimeric fusion 59 β1 Human γ2 Human Cryo-EM 7YDP - 3.1 AGRE5 ADGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - Nanobody-35 - - - - - - Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y 10.1016/J.CHEMBIOL.2023.08.003 2023-07-12
Gi/o αi1 Human DN human Gi1: G203A/A326S mutations 61 β1 Human γ2 Human Cryo-EM 7YKD - 2.8 CML1 CMKLR1 chemerin Chemerin receptor A (Rhodopsin) Human - - - chemerin C-terminal peptide pubchem gtoplig chembl_ligand pubchem
Peptide Agonist 18R-HEPE, EPA, resolvin E1, chemerin (Human) Peptide Wang J, Chen G, Liao Q, Lyu W, Liu A, Zhu L, Du Y, Ye RD 10.1073/PNAS.2214324120 2023-04-19
Gi/o αi1 Human Native human Gi: Gαi1/Gβ1(6xHis)/Gγ2 62 β1 Human γ2 Human Cryo-EM 7YON 7YON_refined 3.0 NPY2R NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human BRIL - - CHEMBL439904 chembl_ligand pubchem
Protein Agonist neuropeptide Y (Human), neuropeptide Y-(3-36) (Human), pancreatic polypeptide (Rat), pancreatic polypeptide (Human), peptide YY (Human), pancreatic polypeptide (Mouse), PYY-(3-36) (Human), peptide YY (Mouse) Peptide Kang H, Park C, Choi YK, Bae J, Kwon S, Kim J, Choi C, Seok C, Im W, Choi HJ 10.1016/J.STR.2022.11.010 2023-03-22
Gi/o αi1 Human Human Gi heterotrimer (Gαi1/Gβ1/Gγ2) 61 β1 Human γ2 Human Cryo-EM 7YOO 7YOO_refined 3.1 NPY2R NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human BRIL - - NEUROPEPTIDE-Y chembl_ligand pubchem
Protein Agonist neuropeptide Y (Human), neuropeptide Y-(3-36) (Human), pancreatic polypeptide (Rat), pancreatic polypeptide (Human), peptide YY (Human), pancreatic polypeptide (Mouse), PYY-(3-36) (Human), peptide YY (Mouse) Peptide Kang H, Park C, Choi YK, Bae J, Kwon S, Kim J, Choi C, Seok C, Im W, Choi HJ 10.1016/J.STR.2022.11.010 2023-03-22
Gi/o αi1 Human DN Gi1: S47N/E245A/G203A/A326S 60 β1 Human γ2 Human Cryo-EM 8DZP - 2.7 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - CHEMBL180126 chembl_ligand pubchem chembl_ligand pubchem
Small molecule Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03
Gi/o αo Human DN Go: C3S/S47N/G204A/E246A/A326S/M249K 61 β1 Human γ2 Human Cryo-EM 8DZQ 8DZQ_refined 2.8 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - CHEMBL180126 chembl_ligand pubchem chembl_ligand pubchem
Small molecule Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03
Gi/o αz Human Gαz chimera: Gi2 N-term, DN muts incl S47N/G204A 59 β1 Human γ2 Human Cryo-EM 8DZS - 2.7 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - CHEMBL277863 chembl_ligand pubchem
Small molecule Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Han J, Zhang J, Nazarova AL, Bernhard SM, Krumm BE, Zhao L, Lam JH, Rangari VA, Majumdar S, Nichols DE, Katritch V, Yuan P, Fay JF, Che T 10.1038/S41586-023-06030-7 2023-05-03
Gi/o αi1 Human Gai1_2M: DN Gαi1, G203A/A326S 64 β1 Rat γ2 Bovine Cryo-EM 8EF6 8EF6_refined 3.2 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - morphine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
Gs αs Human DNGsV1: DN Gs mutant 59 β1 Human γ2 Human Cryo-EM 8E3X 8E3X_refined 2.3 PACR ADCYAP1R1 PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Protein Agonist PHV (Rat), VIP (Human), PHV (Human), PHM (Human), PHI (Mouse), PACAP-38 (Human), PACAP-27 (Human) Protein Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/S41467-022-34629-3 2022-11-23
Gs αs Human DNGsV2: A366S mutation 56 β1 Human γ2 Human Cryo-EM 8E3Y - 2.3 VIPR1 VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Protein Agonist VIP (Human), GHRH (Rat), secretin (Rat), PHM (Human), GHRH (Mouse), PHI (Mouse), PACAP-38 (Human), secretin (Mouse), GHRH (Human), secretin (Pig), PACAP-27 (Human) Protein Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/S41467-022-34629-3 2022-11-23
Gs αs Human DNGsV2: A366S mutation 55 β1 Human γ2 Human Cryo-EM 8E3Z 8E3Z_refined 2.7 VIPR1 VIPR1 VPAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - Vasoactive intestinal polypeptide pubchem
Small molecule Agonist VIP (Human), GHRH (Rat), secretin (Rat), PHM (Human), GHRH (Mouse), PHI (Mouse), PACAP-38 (Human), secretin (Mouse), GHRH (Human), secretin (Pig), PACAP-27 (Human) Protein Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D 10.1038/S41467-022-34629-3 2022-11-23
Gi/o αo Human MiniGo: GTPase domain only, ΔAHD 61 β1 Human γ2 Human Cryo-EM 8E9X - 2.7 ACM4 CHRM4 M4 Acetylcholine (muscarinic) A (Rhodopsin) Human - - - CHEMBL73538 chembl_ligand pubchem
Small molecule Agonist acetylcholine Small molecule Zhang S, Gumpper RH, Huang XP, Liu Y, Krumm BE, Cao C, Fay JF, Roth BL 10.1038/S41586-022-05489-0 2022-11-30
Gi/o αi1 Human DN Gαi1: G203A/A326A 64 β1 Rat γ2 Bovine Cryo-EM 8EF5 - 3.3 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - fentanyl pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
Gi/o αi1 Human DN Gαi1: G203A/A326S 64 β1 Rat γ2 Bovine Cryo-EM 8EFB 8EFB_refined 3.2 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - OLICERIDINE chembl_ligand pubchem drugbank drug_central pubchem
Small molecule Agonist (partial) [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
Gi/o αi1 Human DN Gαi1: G203A/A326S, nucleotide-free state 64 β1 Rat γ2 Human Cryo-EM 8EFL 8EFL_refined 3.2 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - CHEMBL4452384 chembl_ligand pubchem
Small molecule Agonist (partial) [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
Gi/o αi1 Human DN Gαi1: G203A/A326S, only α5 modeled 64 β1 Rat γ2 Bovine Cryo-EM 8EFO - 2.8 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - PZM21 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Zhuang Y, Wang Y, He B, He X, Zhou XE, Guo S, Rao Q, Yang J, Liu J, Zhou Q, Wang X, Liu M, Liu W, Jiang X, Yang D, Jiang H, Shen J, Melcher K, Chen H, Jiang Y, Cheng X, Wang MW, Xie X, Xu HE 10.1016/J.CELL.2022.09.041 2022-11-09
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 8F0K - 1.9 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- San385
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02
Gs αs Human DNGs: dominant-negative Gs protein 59 β1 Human γ2 Human Cryo-EM 8F2A - 2.2 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- San385
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Gerrard E, Danev R, Fletcher MM, Dal Maso E, Schreuder H, Lorenz K, Evers A, Tiwari G, Besenius M, Li Z, Johnson RM, Wootten D, Sexton PM 10.1038/S41589-023-01393-4 2023-08-02
Gs αs Human MiniGs399: truncated/mutated Gαs-short 55 β1 Human γ2 Human Cryo-EM 8F76 8F76_refined 3.1 O51E2 OR51E2 OR51E2 Olfactory family 51 O1 (Olfactory/extra-nasal 1) Human - Nanobody-35 - propanoic acid pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem
Small molecule Agonist - - Billesbolle CB, de March CA, van der Velden WJC, Ma N, Tewari J, Del Torrent CL, Li L, Faust B, Vaidehi N, Matsunami H, Manglik A 10.1038/S41586-023-05798-Y 2023-03-22
Gi/o αi1 Human Gai1_2M: DN Gαi1, G203A/A326S 62 β1 Rat γ2 Bovine Cryo-EM 8F7S 8F7S_refined 3.0 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - - - deltorphin II pubchem gtoplig chembl_ligand pubchem
Peptide Agonist [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE 10.1016/J.CELL.2022.12.026 2022-12-14
Gi/o αi1 Human Gai1_4M: DN Gαi1, S47N/G203A/E245A/A326S 64 β1 Rat γ2 Bovine Cryo-EM 8F7W 8F7W_refined 3.2 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - dynorphin A-(1-8) (Human) pubchem gtoplig uniprot uniprot uniprot chembl_ligand
Peptide Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE 10.1016/J.CELL.2022.12.026 2022-12-14
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 62 β1 Rat γ2 Bovine Cryo-EM 8F7X 8F7X_refined 3.3 OPRX OPRL1 NOP Opioid A (Rhodopsin) Human - - - nociceptin/orphanin FQ (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist nociceptin/orphanin FQ (Human) Peptide Wang Y, Zhuang Y, DiBerto JF, Zhou XE, Schmitz GP, Yuan Q, Jain MK, Liu W, Melcher K, Jiang Y, Roth BL, Xu HE 10.1016/J.CELL.2022.12.026 2022-12-14
Gi/o αi1 Human DN Gi1: S47N/E245A/G203A/A326S 55 β1 Human γ2 Human Cryo-EM 8FEG - 2.5 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - DNCP-beta-NalA(1)
Peptide Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Muratspahic E, Deibler K, Han J, Tomasevic N, Jadhav KB, Olive-Marti AL, Hochrainer N, Hellinger R, Koehbach J, Fay JF, Rahman MH, Hegazy L, Craven TW, Varga BR, Bhardwaj G, Appourchaux K, Majumdar S, Muttenthaler M, Hosseinzadeh P, Craik DJ, Spetea M, Che T, Baker D, Gruber CW 10.1038/s41467-023-43718-w 2023-12-06
Gs αs Human DNGas: G226A/A366S 59 β1 Human γ2 Human Cryo-EM 8FLQ - 2.6 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTH pubchem
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gs αs Human DNGs: DN Gαs subunit 59 β1 Human γ2 Human Cryo-EM 8FLR - 2.9 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTHrP[1-36]
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gs αs Human DN Gαs protein 59 β1 Human γ2 Human Cryo-EM 8FLS - 3.1 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - abaloparatide drug_central pubchem
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gs αs Human DN Gαs protein 59 β1 Human γ2 Human Cryo-EM 8FLT - 3.0 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - M-PTH(1-14)
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gs αs Human DN Gs protein 58 β1 Human γ2 Human Cryo-EM 8FLU - 2.8 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Long-acting parathyroid hormone analog pubchem
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM 10.1016/J.STR.2023.04.002 2023-04-26
Gi/o αo Human Engineered mini-GαoA protein 60 β1 Human γ2 Human Cryo-EM 8FN0 - 2.9 NTR1 Ntsr1 NTS1 Neurotensin A (Rhodopsin) Rat - - - SBI-553 pubchem gtoplig chembl_ligand
NTS8–13 pubchem
Small molecule
Peptide 		Ago-PAM
Agonist 		neurotensin (Human), neuromedin N (Mouse) Peptide Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
Gi/o αo Human Truncated miniGoA heterotrimer 60 β1 Human γ2 Human Cryo-EM 8FN1 - 2.9 NTR1 Ntsr1 NTS1 Neurotensin A (Rhodopsin) Rat - - - NTS8–13 pubchem
Peptide Agonist neurotensin (Human), neuromedin N (Mouse) Peptide Krumm BE, DiBerto JF, Olsen RHJ, Kang HJ, Slocum ST, Zhang S, Strachan RT, Huang XP, Slosky LM, Pinkerton AB, Barak LS, Caron MG, Kenakin T, Fay JF, Roth BL 10.1021/ACS.BIOCHEM.3C00029 2023-03-29
Gs αs Human Gs heterotrimer w/ ZP3780; unproductive(RAMP2) 54 β1 Human γ2 Human Cryo-EM 8FU6 8FU6_refined 2.9 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Glucagon derivative ZP3780
Peptide Agonist glucagon (Human) Protein Krishna Kumar K, O'Brien ES, Habrian CH, Latorraca NR, Wang H, Tuneew I, Montabana E, Marqusee S, Hilger D, Isacoff EY, Mathiesen JM, Kobilka BK 10.1016/J.CELL.2023.02.028 2023-04-12
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S; Gγ2 fusion 66 β1 Human γ2 Human Cryo-EM 8FY8 - 2.8 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - 5-MeO-DMT pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist 5-hydroxytryptamine Small molecule Warren AL, Lankri D, Cunningham MJ, Serrano IC, Parise LF, Kruegel AC, Duggan P, Zilberg G, Capper MJ, Havel V, Russo SJ, Sames D, Wacker D 10.1038/S41586-024-07403-2 2024-05-15
Gi/o αi1 Human DN Gi1: Gαi1 4 muts; Gγ2-Gαi1 fusion 66 β1 Human γ2 Human Cryo-EM 8FYE - 2.9 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - CHEMBL352186 chembl_ligand pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule Warren AL, Lankri D, Cunningham MJ, Serrano IC, Parise LF, Kruegel AC, Duggan P, Zilberg G, Capper MJ, Havel V, Russo SJ, Sames D, Wacker D 10.1038/S41586-024-07403-2 2024-05-15
Gi/o αi1 Human DN Gi1: S47N/G203A/E245A/A326S 66 β1 Human γ2 Human Cryo-EM 8FYL - 2.9 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - vilazodone pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule Warren AL, Lankri D, Cunningham MJ, Serrano IC, Parise LF, Kruegel AC, Duggan P, Zilberg G, Capper MJ, Havel V, Russo SJ, Sames D, Wacker D 10.1038/S41586-024-07403-2 2024-05-15
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 66 β1 Human γ2 Human Cryo-EM 8FYT - 2.6 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist 5-hydroxytryptamine Small molecule Warren AL, Lankri D, Cunningham MJ, Serrano IC, Parise LF, Kruegel AC, Duggan P, Zilberg G, Capper MJ, Havel V, Russo SJ, Sames D, Wacker D 10.1038/S41586-024-07403-2 2024-05-15
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 66 β1 Human γ2 Human Cryo-EM 8FYX - 2.6 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - buspirone pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule Warren AL, Lankri D, Cunningham MJ, Serrano IC, Parise LF, Kruegel AC, Duggan P, Zilberg G, Capper MJ, Havel V, Russo SJ, Sames D, Wacker D 10.1038/S41586-024-07403-2 2024-05-15
Gi/o αi1 Human DNGαi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8G05 - 3.0 GPR84 GPR84 GPR84 Orphan A (Rhodopsin) Human - - - 6-n-octylaminouracil pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist - - Zhang X, Wang Y, Supekar S, Cao X, Zhou J, Dang J, Chen S, Jenkins L, Marsango S, Li X, Liu G, Milligan G, Feng M, Fan H, Gong W, Zhang C 10.1038/S41467-023-41201-0 2023-11-01
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8GAG 8GAG_refined 3.3 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - methyl (2R)-2-({(1M)-5-methyl-1-[3-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonyl}amino)-2-(thiophen-2-yl)propanoate pubchem
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule - - 2024-02-28
Gi/o αi1 Human - 56 β1 Human γ2 Human Cryo-EM 8GCM - 3.5 PE2R4 PTGER4 EP4 Prostanoid A (Rhodopsin) Human - - - L902688 pubchem
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-03
Gi/o αi1 Human Native-like human Gi heterotrimer 61 β1 Human γ2 Human Cryo-EM 8GCP 8GCP_refined 3.1 PE2R4 PTGER4 EP4 Prostanoid A (Rhodopsin) Human - - - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-03
G12/13 α13 Human Mini-G13/i: Gs backbone, Gαi1 N-term, G13 α5 56 β1 Human γ2 Human Cryo-EM 8KGG - 3.1 P2Y10 P2RY10 P2RY10 Orphan A (Rhodopsin) Human - - - LysoPS(18:0)
Small molecule Agonist sphingosine 1-phosphate, LPA Lipid Yin H, Kamakura N, Qian Y, Tatsumi M, Ikuta T, Liang J, Xu Z, Xia R, Zhang A, Guo C, Inoue A, He Y 10.1016/J.CHEMBIOL.2024.08.005 2024-07-31
Gs αs Human Gs-short heterotrimer; Gα modeled 1-248 54 β1 Human γ2 Human Cryo-EM 8GD9 - 3.2 PE2R4 PTGER4 EP4 Prostanoid A (Rhodopsin) Human - Nanobody-35 - Rivenprost pubchem
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-10
Gs αs Human Gαs (short isoform) subunit 58 β1 Human γ2 Human Cryo-EM 8GDA 8GDA_refined 3.3 PE2R4 PTGER4 EP4 Prostanoid A (Rhodopsin) Human - Nanobody-35 - L902688 pubchem
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-10
Gs αs Human Gαs subunit, short isoform 59 β1 Human γ2 Human Cryo-EM 8GDB 8GDB_refined 3.1 PE2R4 PTGER4 EP4 Prostanoid A (Rhodopsin) Human - Nanobody-35 - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-10
Gi/o αi1 Human - 58 β1 Human γ2 Human Cryo-EM 8GDC 8GDC_refined 3.5 PE2R3 PTGER3 EP3 Prostanoid A (Rhodopsin) Human - - - PGE2 pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Huang SM, Xiong MY, Liu L, Mu J, Wang MW, Jia YL, Cai K, Tie L, Zhang C, Cao S, Wen X, Wang JL, Guo SC, Li Y, Qu CX, He QT, Cai BY, Xue C, Gan S, Xie Y, Cong X, Yang Z, Kong W, Li S, Li Z, Xiao P, Yang F, Yu X, Guan YF, Zhang X, Liu Z, Yang BX, Du Y, Sun JP 10.1073/PNAS.2216329120 2024-01-10
Gs αs Human Human Gs heterotrimer w/ Gαs-short variant 59 β1 Human γ2 Human Cryo-EM 8GDZ - 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs-short heterotrimer, nucleotide-free 59 β1 Human γ2 Human Cryo-EM 8GE1 - 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs subunit, short isoform 59 β1 Human γ2 Human Cryo-EM 8GE2 - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Nucleotide-free Gs heterotrimer (short isoform) 60 β1 Human γ2 Human Cryo-EM 8GE3 - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gαs-short variant, nucleotide-free frame 59 β1 Human γ2 Human Cryo-EM 8GE4 - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs-short splice variant 59 β1 Human γ2 Human Cryo-EM 8GE5 - 3.2 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Nucleotide-free Gs, Gα short splice variant 59 β1 Human γ2 Human Cryo-EM 8GE6 8GE6_refined 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs heterotrimer: Gαs-short/Gβ1/Gγ2 58 β1 Human γ2 Human Cryo-EM 8GE7 8GE7_refined 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Nucleotide-free Gs, Gs-short splice variant 60 β1 Human γ2 Human Cryo-EM 8GE8 8GE8_refined 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs heterotrimer (Gαs-short/Gβ1/Gγ2) 60 β1 Human γ2 Human Cryo-EM 8GE9 8GE9_refined 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs short splice variant 61 β1 Human γ2 Human Cryo-EM 8GEA 8GEA_refined 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs heterotrimer w/ Gαs-short variant 59 β1 Human γ2 Human Cryo-EM 8GEB 8GEB_refined 3.6 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gαs short splice variant (isoform 2) 59 β1 Human γ2 Human Cryo-EM 8GEC 8GEC_refined 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs-short (Gnas2); Gβ1 His-tag/3C site 71 β1 Human γ2 Human Cryo-EM 8GED 8GED_refined 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Nucleotide-free Gs, 3DVA AHD closure frame 15/20 69 β1 Human γ2 Human Cryo-EM 8GEE 8GEE_refined 3.7 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs heterotrimer (short Gαs isoform) 71 β1 Human γ2 Human Cryo-EM 8GEF 8GEF_refined 3.8 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs-short splice variant 78 β1 Human γ2 Human Cryo-EM 8GEG 8GEG_refined 3.8 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human WT Gs heterotrimer (short Gαs isoform) 76 β1 Human γ2 Human Cryo-EM 8GEH 8GEH_refined 4.0 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Nucleotide-free Gs, 3DVA frame 19/20 70 β1 Human γ2 Human Cryo-EM 8GEI - 4.1 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Nucleotide-free Gs, short splice variant 79 β1 Human γ2 Human Cryo-EM 8GEJ 8GEJ_refined 4.2 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs short variant, no mutations 59 β1 Human γ2 Human Cryo-EM 8GFV - 3.1 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gs heterotrimer; human short variant GNAS2 59 β1 Human γ2 Human Cryo-EM 8GFW - 3.0 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs short splice variant (GNAS2) 59 β1 Human γ2 Human Cryo-EM 8GFX - 3.0 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human WT human Gs heterotrimer (short isoform) 58 β1 Human γ2 Human Cryo-EM 8GFY - 3.0 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gαs short splice variant 58 β1 Human γ2 Human Cryo-EM 8GFZ - 3.0 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs heterotrimer (short splice Gαs) 59 β1 Human γ2 Human Cryo-EM 8GG0 - 2.9 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs short splice variant 59 β1 Human γ2 Human Cryo-EM 8GG1 - 3.0 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gαs-short variant; GTP activation step 8/20 59 β1 Human γ2 Human Cryo-EM 8GG2 - 3.0 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human GTP-bound intermediate, Gs-short α subunit 59 β1 Human γ2 Human Cryo-EM 8GG3 - 3.1 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gαs short splice variant 59 β1 Human γ2 Human Cryo-EM 8GG4 - 3.2 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human GTP-bound Gs heterotrimer, Gs-short α subunit 60 β1 Human γ2 Human Cryo-EM 8GG5 - 3.2 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human WT human Gs heterotrimer (short splice variant) 60 β1 Human γ2 Human Cryo-EM 8GG6 - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gs-short heterotrimer, GTP-bound, frame 13/20 60 β1 Human γ2 Human Cryo-EM 8GG7 - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs heterotrimer; Gα is Gs-short variant 61 β1 Human γ2 Human Cryo-EM 8GG8 - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs heterotrimer w/ Gαs-short variant 76 β1 Human γ2 Human Cryo-EM 8GG9 8GG9_refined 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs-short, GTP transition intermediate #16/20 83 β1 Human γ2 Human Cryo-EM 8GGA 8GGA_refined 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gs-short heterotrimer; activation step 17 79 β1 Human γ2 Human Cryo-EM 8GGB 8GGB_refined 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs short splice variant (GNAS2) 75 β1 Human γ2 Human Cryo-EM 8GGC - 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs-short splice variant 92 β1 Human γ2 Human Cryo-EM 8GGE 8GGE_refined 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs short splice variant 91 β1 Human γ2 Human Cryo-EM 8GGF 8GGF_refined 3.6 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gi/o αi1 Human Human Gαi1 heterotrimer, bovine Gβ1/GγT1 62 β1 Bovine γT1 Bovine Cryo-EM 7O7F 7O7F_refined 3.2 CCR5 CCR5 CCR5 Chemokine A (Rhodopsin) Human - - - [6P4]CCL5
Protein Agonist CCL3 (Mouse), CCL7 (Human), CCL13 (Human), CCL11 (Rat), CCL16 (Human), CCL11 (Mouse), CCL8 (Human), CCL2 (Rat), CCL5 (Mouse), CCL14 (Human), CCL4 (Mouse), CCL5 (Human), CCL4 (Human), CCL3 (Rat), CCL3 (Human), CCL7 (Rat), CCL11 (Human), CCL2 (Human), CCL4 (Rat), CCL8 (Mouse), CCL7 (Mouse), CCL2 (Mouse) Peptide Isaikina P, Tsai CJ, Dietz N, Pamula F, Grahl A, Goldie KN, Guixa-Gonzalez R, Branco C, Paolini-Bertrand M, Calo N, Cerini F, Schertler GFX, Hartley O, Stahlberg H, Maier T, Deupi X, Grzesiek S 10.1126/SCIADV.ABG8685 2021-06-30
Gs αs Human mini-Gs399: N-term(20aa)→Gαi1(18aa) 57 β1 Human γ2 Human Cryo-EM 7P02 - 2.9 NK1R TACR1 NK1 Tachykinin A (Rhodopsin) Human - - - substance P (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide Thom C, Ehrenmann J, Vacca S, Waltenspuhl Y, Schoppe J, Medalia O, Pluckthun A 10.1126/SCIADV.ABK2872 2021-12-15
Gi/o αi1 Human Standard Gi1 heterotrimer for stabilization 62 β1 Human γ2 Human Cryo-EM 8GUQ 8GUQ_refined 3.1 CNR2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human BRIL - - olorinab pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T 10.1038/S41467-023-37112-9 2023-05-10
Gi/o αi1 Human Nucleotide-free human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 8GHV 8GHV_refined 2.8 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - CHEMBL4208628 chembl_ligand pubchem
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Krishna Kumar K, Robertson MJ, Thadhani E, Wang H, Suomivuori CM, Powers AS, Ji L, Nikas SP, Dror RO, Inoue A, Makriyannis A, Skiniotis G, Kobilka B 10.1038/S41467-023-37864-4 2023-05-24
Gi/o αi1 Human Wild-type human Gi heterotrimer 64 β1 Human γ2 Human Cryo-EM 8GUR 8GUR_refined 2.8 CNR2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human BRIL - - CP55940 pubchem gtoplig chembl_ligand
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T 10.1038/S41467-023-37112-9 2023-05-10
Gi/o αi1 Human Wild-type human Gi subunits 62 β1 Human γ2 Human Cryo-EM 8GUS - 3.0 CNR2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human BRIL - - CHEMBL2179724 chembl_ligand pubchem
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T 10.1038/S41467-023-37112-9 2023-05-10
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 8GUT 8GUT_refined 3.0 CNR2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human BRIL - - LEI-102 pubchem
Small molecule Agonist (partial) anandamide, 2-arachidonoylglycerol Small molecule Li X, Chang H, Bouma J, de Paus LV, Mukhopadhyay P, Paloczi J, Mustafa M, van der Horst C, Kumar SS, Wu L, Yu Y, van den Berg RJBHN, Janssen APA, Lichtman A, Liu ZJ, Pacher P, van der Stelt M, Heitman LH, Hua T 10.1038/S41467-023-37112-9 2023-05-10
Gs αs Human Mini-Gs (short isoform of Gαs) 58 β1 Rat γ2 Bovine Cryo-EM 8GW8 - 2.9 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PCO371 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Kobayashi K, Kawakami K, Kusakizako T, Tomita A, Nishimura M, Sawada K, Okamoto HH, Hiratsuka S, Nakamura G, Kuwabara R, Noda H, Muramatsu H, Shimizu M, Taguchi T, Inoue A, Murata T, Nureki O 10.1038/S41586-023-06169-3 2023-06-14
Gi/o αi1 Human Gγ2-(GSA)3-Gαi1 fusion construct 63 β1 Human γ2 Human Cryo-EM 8H2G 8H2G_refined 3.0 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule - - 2023-10-11
Gs αs Human Mini-Gαs, Gs/Gi chimera (dual accessions) 59 β1 Human γ2 Human Cryo-EM 8H4I - 3.1 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - Nanobody-35 - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21
Gs αs Human mDNGαs: Gi N-term/AHD, G226A/A366S, Gβ1-SmBiT 60 β1 Rat γ2 Bovine Cryo-EM 8HA0 - 2.6 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PTH pubchem
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Zhao LH, Yuan QN, Dai AT, He XH, Chen CW, Zhang C, Xu YW, Zhou Y, Wang MW, Yang DH, Xu HE 10.1038/S41401-022-01032-Z 2022-12-21
Gi/o αi1 Human DN Gαi1 (Gnai1): G203A/A326S 61 β1 Human γ2 Human Cryo-EM 8HBD 8HBD_refined 3.0 EDNRB EDNRB ETB Endothelin A (Rhodopsin) Human - - LgBiT sovateltide pubchem gtoplig chembl_ligand pubchem drugbank
Peptide Agonist endothelin-2 (Mouse), endothelin-2 (Human), endothelin-1 (Human), endothelin-3 (Human) Protein - - 2023-03-22
Gs αs Human Truncated/stabilized miniGs (not chimeric) 59 β1 Human γ2 Human Cryo-EM 8HDO - 2.9 AA2BR ADORA2B A2B Adenosine A (Rhodopsin) Human - Nanobody-35 - BAY 60-6583 pubchem gtoplig chembl_ligand
Small molecule Agonist adenosine Small molecule Cai H, Xu Y, Guo S, He X, Sun J, Li X, Li C, Yin W, Cheng X, Jiang H, Xu HE, Xie X, Jiang Y 10.1038/S41421-022-00503-1 2023-01-18
Gs αs Human MiniGs: 6 point mutations + 3 deletions 61 β1 Human γ2 Human Cryo-EM 8HIX - 3.1 GPR21 GPR21 GPR21 Orphan A (Rhodopsin) Human BRIL Nanobody-35 - - None - - - Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F 10.1038/S41467-023-35882-W 2023-03-15
Gq/11 α15 Human Chimera: Gs body, G15 C-term α5 helix 60 β1 Human γ2 Human Cryo-EM 8HJ0 - 3.1 GPR21 GPR21 GPR21 Orphan A (Rhodopsin) Human - Nanobody-35 - - None - - - Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F 10.1038/S41467-023-35882-W 2023-03-15
Gs αs Human mGs: truncations + 6 point mutations 61 β1 Human γ2 Human Cryo-EM 8HJ1 8HJ1_refined 3.3 GPR21 GPR21 GPR21 Orphan A (Rhodopsin) Human - Nanobody-35 - - None - - - Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F 10.1038/S41467-023-35882-W 2023-12-27
Gq/11 α15 Human miniG15: miniGs+G15 α5; stabilizing muts 60 β1 Human γ2 Human Cryo-EM 8HJ2 8HJ2_refined 3.8 GPR21 GPR21 GPR21 Orphan A (Rhodopsin) Human - Nanobody-35 - - None - - - Lin X, Chen B, Wu Y, Han Y, Qi A, Wang J, Yang Z, Wei X, Zhao T, Wu L, Xie X, Sun J, Zheng J, Zhao S, Xu F 10.1038/S41467-023-35882-W 2023-03-15
Gi/o αi1 Human DN Gαi1 (bovine/human): G203A/A326S 64 β1 Rat γ2 Bovine Cryo-EM 8HK2 - 2.9 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - - C3a anaphylatoxin
Protein Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y 10.1038/S41589-023-01339-W 2023-05-10
Gi/o αi1 Human DN mutant: G203A/A326S, complex stabilizer 63 β1 Rat γ2 Bovine Cryo-EM 8HK3 8HK3_refined 3.2 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - - - None - C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y 10.1038/S41589-023-01339-W 2023-05-10
Gi/o αi1 Human DN Gs: G203A/A326S 64 β1 Human γ2 Human Cryo-EM 8WP1 - 3.2 SUCR1 SUCNR1 succinate Succinate A (Rhodopsin) Human BRIL - - cis-epoxysuccinic acid pubchem gtoplig chembl_ligand
Small molecule Agonist succinic acid Small molecule Liu A, Liu Y, Zhang W, Ye RD 10.1016/J.CELREP.2024.114381 2024-09-11
Gi/o αi1 Human DN Gαi1 (bovine per paper, human/PDB): G203A/A326S 63 β1 Rat γ2 Bovine Cryo-EM 8HK5 8HK5_refined 3.0 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - - [125I]C5a (human) gtoplig
Peptide Agonist C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide Wang Y, Liu W, Xu Y, He X, Yuan Q, Luo P, Fan W, Zhu J, Zhang X, Cheng X, Jiang Y, Xu HE, Zhuang Y 10.1038/S41589-023-01339-W 2023-05-10
Gs αs Human MiniGαs construct 61 β1 Human γ2 Human Cryo-EM 8HMP - 2.8 GPR52 GPR52 GPR52 Orphan A (Rhodopsin) Human - Nanobody-35 - derivative 17 [Nakahata et al., 2018] pubchem gtoplig chembl_ligand
Small molecule Allosteric agonist - - Fan Y, Lin X, Pan B, Chen B, Liu D, Wuthrich K, Xu F 10.1002/MCO2.260 2023-06-21
Gs αs Human DNGαs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 8HMV 8HMV_refined 2.9 GPR21 GPR21 GPR21 Orphan A (Rhodopsin) Human BRIL Nanobody-35 - - None - - - Wong TS, Gao W, Chen G, Qiu C, He G, Ye F, Wu Z, Zeng Z, Du Y 10.1002/MCO2.205 2023-03-01
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 8HN8 - 3.0 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human BRIL - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule - - 2023-12-20
Gi/o αi1 Human DN Gαi1: G203A/A326S; Gβ-HiBiT fusion 62 β1 Human γ2 Human Cryo-EM 8HNK - 3.0 CXCR3 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		[125I]CXCL11 (human) gtoplig
Peptide Agonist CXCL9 (Mouse), CCL20 (Human), CCL19 (Human), CXCL10 (Human), CXCL10 (Mouse), CCL11 (Human), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CXCL12α (Human), CXCL9 (Human), CCL5 (Human), CXCL11 (Human) Peptide Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H 10.1038/S41594-023-01175-5 2023-11-29
Gi/o αi1 Human DN Gαi1: G203A/A326S; Gβ C-term HiBit fusion 62 β1 Human γ2 Human Cryo-EM 8HNL - 3.0 CXCR3 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human BRIL - luci_oplgr (LgBit) PS372424 pubchem
Small molecule Agonist CXCL9 (Mouse), CCL20 (Human), CCL19 (Human), CXCL10 (Human), CXCL10 (Mouse), CCL11 (Human), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CXCL12α (Human), CXCL9 (Human), CCL5 (Human), CXCL11 (Human) Peptide Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H 10.1038/S41594-023-01175-5 2023-11-29
Gi/o αi1 Human DN Gαi1: G203A/A326S; Gβ1-HiBiT fusion 62 β1 Human γ2 Human Cryo-EM 8HNM - 2.9 CXCR3 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		CHEMBL2220409 chembl_ligand pubchem
Small molecule Agonist CXCL9 (Mouse), CCL20 (Human), CCL19 (Human), CXCL10 (Human), CXCL10 (Mouse), CCL11 (Human), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CXCL12α (Human), CXCL9 (Human), CCL5 (Human), CXCL11 (Human) Peptide Jiao H, Pang B, Liu A, Chen Q, Pan Q, Wang X, Xu Y, Chiang YC, Ren R, Hu H 10.1038/S41594-023-01175-5 2023-11-29
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8HQE 8HQE_refined 3.0 GP132 GPR132 GPR132 Proton A (Rhodopsin) Human BRIL - - - None - 9-hydroxyoctadecadienoic acid Small molecule Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X 10.1038/S42255-023-00899-4 2023-10-11
Gi/o αi1 Human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 8HOC - 3.0 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human BRIL - - imetit pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule - - 2023-12-20
Gi/o αo Human Mini-Go: AHD deleted, stabilizing mutations 58 β1 Human γ2 Human Cryo-EM 8HPT - 3.4 C5AR1 C5ar1 C5a1 Complement peptide A (Rhodopsin) Mouse - - - C5apep
Peptide Agonist - - Qiu CH, Wang DF, Xue FS HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αo Human Go heterotrimer 60 β1 Human γ2 Human Cryo-EM 8HQC - 3.9 C5AR1 C5ar1 C5a1 Complement peptide A (Rhodopsin) Mouse - - - [125I]C5a (human) gtoplig
Peptide Agonist - - Qiu CH, Wang DF, Xue FS HTTPS://DOI.ORG/10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αi1 Human DN Gαi1 mutant: S47N/G203A/A326S 62 β1 Human γ2 Human Cryo-EM 8HS3 - 3.1 GPR20 GPR20 GPR20 Orphan A (Rhodopsin) Human BRIL - - - None - - - Lin X, Jiang S, Wu Y, Wei X, Han GW, Wu L, Liu J, Chen B, Zhang Z, Zhao S, Cherezov V, Xu F 10.1038/S41421-023-00520-8 2023-03-08
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S 62 β1 Human γ2 Human Cryo-EM 8HSC - 3.2 GPR20 GPR20 GPR20 Orphan A (Rhodopsin) Human BRIL - - - None - - - Lin X, Jiang S, Wu Y, Wei X, Han GW, Wu L, Liu J, Chen B, Zhang Z, Zhao S, Cherezov V, Xu F 10.1038/S41421-023-00520-8 2023-03-08
Gi/o αi1 Human Human Gi1 heterotrimer 60 β1 Human γ2 Human Cryo-EM 8HVI 8HVI_refined 3.0 GP132 GPR132 GPR132 Proton A (Rhodopsin) Human BRIL - - NOX-6-7 pubchem gtoplig
Small molecule Agonist 9-hydroxyoctadecadienoic acid Small molecule Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X 10.1038/S42255-023-00899-4 2023-10-11
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8HQM 8HQM_refined 3.0 GP132 GPR132 GPR132 Proton A (Rhodopsin) Human BRIL - - N-hexadecanoylglycine pubchem drugbank
Lipid Agonist (partial) 9-hydroxyoctadecadienoic acid Small molecule Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X 10.1038/S42255-023-00899-4 2023-10-11
Gi/o αi1 Human Wild-type Gi heterotrimer 41 β1 Human γ2 Human Cryo-EM 8I7V - 2.8 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - Acipimox pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Park JH, Kawakami K, Ishimoto N, Ikuta T, Ohki M, Ekimoto T, Ikeguchi M, Lee DS, Lee YH, Tame JRH, Inoue A, Park SY 10.1038/S41467-023-42764-8 2024-02-07
Gi/o αi1 Human WT human Gi; expr. as Gγ2-Gαi1 fusion construct 45 β1 Human γ2 Human Cryo-EM 8I7W 8I7W_refined 3.4 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - GSK256073 pubchem gtoplig
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Park JH, Kawakami K, Ishimoto N, Ikuta T, Ohki M, Ekimoto T, Ikeguchi M, Lee DS, Lee YH, Tame JRH, Inoue A, Park SY 10.1038/S41467-023-42764-8 2024-02-07
Gi/o αo Human Mini-Gαo (miniGαo), complex stabilizer 59 β1 Human γ2 Human Cryo-EM 8I95 - 2.9 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - - EP54
Peptide Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αo Human Mini-Go protein fragment 59 β1 Human γ2 Human Cryo-EM 8I97 8I97_refined 3.2 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - - - None - C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αo Human Mini-Gαo protein 59 β1 Human γ2 Human Cryo-EM 8I9L - 3.2 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - - C3a anaphylatoxin
Protein Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αo Human miniGαo: truncated, AHD removed for stability 59 β1 Human γ2 Human Cryo-EM 8I9S 8I9S_refined 3.3 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - - - None - C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αo Human Mini-Go: N-term ScFv16 sequence, truncated 59 β1 Human γ2 Human Cryo-EM 8IA2 8IA2_refined 3.2 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - - [125I]C5a (human) gtoplig
Peptide Agonist C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αi1 Human Wild-type Gi1 heterotrimer for complex formation 61 β1 Human γ2 Human Cryo-EM 8IA8 - 2.9 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - - E7 pubchem gtoplig gtoplig
Peptide Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide - - 2023-05-24
Gi/o αi1 Human Wild-type human Gi heterotrimer 65 β1 Human γ2 Human Cryo-EM 8IC0 - 3.4 CXCR1 CXCR1 CXCR1 Chemokine A (Rhodopsin) Human - - - Interleukin-8
Protein Agonist CXCL6 (Human), CXCL8 (Human), cytokine domain of tyrosyl tRNA synthetase (Human) Peptide Ishimoto N, Park JH, Kawakami K, Tajiri M, Mizutani K, Akashi S, Tame JRH, Inoue A, Park SY 10.1038/S41467-023-39799-2 2023-07-19
Gi/o αi1 Human DN Gi1 protein 64 β1 Human γ2 Human Cryo-EM 8ID3 8ID3_refined 3.1 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - 9-Hydroxyoctadecanoic acid pubchem
Lipid Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gi/o αi1 Human Native human Gi heterotrimer 64 β1 Human γ2 Human Cryo-EM 8ID4 - 3.1 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - linoleic acid pubchem gtoplig chembl_ligand drug_central drugbank
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gi/o αi1 Human Human Gαi1, likely DN muts G203A/A326S (ref 36) 64 β1 Human γ2 Human Cryo-EM 8ID6 - 2.8 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - oleic acid pubchem gtoplig chembl_ligand drug_central pubchem drugbank
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 8HQN 8HQN_refined 3.0 GP132 GPR132 GPR132 Proton A (Rhodopsin) Human BRIL - - 9-hydroxyoctadecadienoic acid pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist 9-hydroxyoctadecadienoic acid Small molecule Wang JL, Dou XD, Cheng J, Gao MX, Xu GF, Ding W, Ding JH, Li Y, Wang SH, Ji ZW, Zhao XY, Huo TY, Zhang CF, Liu YM, Sha XY, Gao JR, Zhang WH, Hao Y, Zhang C, Sun JP, Jiao N, Yu X 10.1038/S42255-023-00899-4 2023-10-11
Gi/o αo Human Mini-Gαo construct 61 β1 Human γ2 Human Cryo-EM 8IED - 3.3 GP156 GPR156 GPR156 Orphan C (Glutamate) Human - - - PC 34:1 pubchem
Lipid Agonist - - - - 2024-02-14
Gi/o αi1 Human DN Gαi1: G203A/A326S; Gβ-SmBiT fusion 62 β1 Mouse γ2 Mouse Cryo-EM 8IHF - 3.0 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - LgBiT MK 6892 pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y 10.1038/S41467-023-41650-7 2023-08-30
Gi/o αi1 Human Gi1 heterotrimer with scFv16 64 β1 Human γ2 Human Cryo-EM 8ID8 - 3.0 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - TUG-891 pubchem gtoplig chembl_ligand
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gi/o αi1 Human DN alpha subunit: G203A/A326S; Gβ-SmBiT 62 β1 Mouse γ2 Mouse Cryo-EM 8IHB - 2.9 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		GSK256073 pubchem gtoplig
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y 10.1038/S41467-023-41650-7 2023-09-13
Gi/o αi1 Human - 56 β1 Human γ2 Human Cryo-EM 8ID9 8ID9_refined 3.0 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - EPA pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Mao C, Xiao P, Tao XN, Qin J, He QT, Zhang C, Guo SC, Du YQ, Chen LN, Shen DD, Yang ZS, Zhang HQ, Huang SM, He YH, Cheng J, Zhong YN, Shang P, Chen J, Zhang DL, Wang QL, Liu MX, Li GY, Guo Y, Xu HE, Wang C, Zhang C, Feng S, Yu X, Zhang Y, Sun JP 10.1126/SCIENCE.ADD6220 2023-03-15
Gi/o αi1 Human DN Gαi1: G203A/A326S 62 β1 Mouse γ2 Mouse Cryo-EM 8IHH - 3.1 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - LgBiT 5-butyl-1H-pyrazole-3-carboxylic acid pubchem gtoplig chembl_ligand
Small molecule Agonist (partial) butyric acid, β-D-hydroxybutyric acid Small molecule Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y 10.1038/S41467-023-41650-7 2023-08-30
Gi/o αi1 Human DN Gαi1: G203A/A326S 62 β1 Mouse γ2 Mouse Cryo-EM 8IHI - 3.1 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		Acifran pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y 10.1038/S41467-023-41650-7 2023-08-30
Gi/o αi1 Human DN Gs: G203A/A326S 61 β1 Human γ2 Human Cryo-EM 8IJB 8IJB_refined 3.2 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - Acipimox pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y 10.1038/S41421-023-00610-7 2024-01-03
Gi/o αi1 Human DN Gαi1 with G203A/A326S mutations 61 β1 Human γ2 Human Cryo-EM 8IJD - 3.3 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - MK 6892 pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y 10.1038/S41421-023-00610-7 2024-01-03
Gi/o αi1 Human Gαi1 (G203A/A326S); Gβ1 C-term SmBiT 62 β1 Mouse γ2 Mouse Cryo-EM 8IHJ 8IHJ_refined 3.1 HCAR3 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - Acifran pubchem
Small molecule Agonist 3-hydroxyoctanoic acid Small molecule Suzuki S, Tanaka K, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y 10.1038/S41467-023-41650-7 2023-08-30
Gi/o αi1 Human DN Gαi1 with G203A/A326S mutations 61 β1 Human γ2 Human Cryo-EM 8IJ3 8IJ3_refined 3.3 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - - None - butyric acid, β-D-hydroxybutyric acid Small molecule Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y 10.1038/S41421-023-00610-7 2024-01-03
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 61 β1 Human γ2 Human Cryo-EM 8IJA - 2.7 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Pan X, Ye F, Ning P, Zhang Z, Li X, Zhang B, Wang Q, Chen G, Gao W, Qiu C, Wu Z, Li J, Zhu L, Xia J, Gong K, Du Y 10.1038/S41421-023-00610-7 2024-01-03
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 8IKG 8IKG_refined 3.4 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - CB-02 pubchem
Small molecule Allosteric agonist anandamide, 2-arachidonoylglycerol Small molecule Shen S, Wu C, Lin G, Yang X, Zhou Y, Zhao C, Miao Z, Tian X, Wang K, Yang Z, Liu Z, Guo N, Li Y, Xia A, Zhou P, Liu J, Yan W, Ke B, Yang S, Shao Z 10.1073/PNAS.2321532121 2024-06-05
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 8IKH 8IKH_refined 3.3 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - CB-05 pubchem
Small molecule Allosteric agonist anandamide, 2-arachidonoylglycerol Small molecule Shen S, Wu C, Lin G, Yang X, Zhou Y, Zhao C, Miao Z, Tian X, Wang K, Yang Z, Liu Z, Guo N, Li Y, Xia A, Zhou P, Liu J, Yan W, Ke B, Yang S, Shao Z 10.1073/PNAS.2321532121 2024-06-05
Gi/o αi1 Human DN Gi protein 62 β1 Human γ2 Human Cryo-EM 9J0I - 2.8 P2Y14 P2RY14 P2Y14 P2Y A (Rhodopsin) Human BRIL - - UDP-glucuronic acid pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist UDP, UDP-galactose, UDP-glucose, UDP N-acetyl-glucosamine, UDP-glucuronic acid Small molecule Gu Q, Lv Z, Wang T, Tang W, Guo X, Huang X, Li F, Wang J 10.1038/S41421-025-00799-9 2025-06-04
G12/13 α13 Human Mini-Gα13, thermostabilized (Gi3/G13 IDs) 56 β1 Human γ2 Human Cryo-EM 8IKL - 2.3 AGRE5 ADGRE5 ADGRE5 ADGRE B2 (Adhesion) Human - - - - - - - - Mao C, Zhao RJ, Dong YJ, Gao M, Chen LN, Zhang C, Xiao P, Guo J, Qin J, Shen DD, Ji SY, Zang SK, Zhang H, Wang WW, Shen Q, Sun JP, Zhang Y 10.1016/J.MOLCEL.2023.12.020 2024-01-24
Gs αs Human Gs/Gi1 chimera; α5 tail from Gs 60 β1 Human γ2 Bovine Cryo-EM 8INR - 2.7 MC5R MC5R MC5 Melanocortin A (Rhodopsin) Human - - LgBiT subunit
HiBiT
HA-signal peptide 		Alpha-MSH pubchem
Calcium pubchem
Small molecule
Small molecule 		Agonist ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC 10.1107/S0907444909042073 2023-09-20
Gs αs Human Gαi1 body + Gαs α5 helix, for Nb35 binding 60 β1 Human γ2 Bovine Cryo-EM 8IOC - 2.9 MC3R MC3R MC3 Melanocortin A (Rhodopsin) Human - Nanobody-35 HA-signal peptide
LgBiT subunit
HiBiT 		γ-MSH (Human) pubchem gtoplig uniprot uniprot uniprot pubchem
Calcium pubchem
Peptide
Small molecule 		Agonist
Cofactor 		ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC 10.1107/S0907444909042073 2023-09-20
Gs αs Human Gs/Gi1 chimera: Gs α5(QRMHLRQYELL), Gi1 core 59 β1 Human γ2 Bovine Cryo-EM 8IOD - 2.6 MC5R MC5R MC5 Melanocortin A (Rhodopsin) Human - Nanobody-35 LgBiT subunit
HiBiT
HA-signal peptide 		PG-901
Peptide Agonist ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Chen VB, Arendall WB 3rd, Headd JJ, Keedy DA, Immormino RM, Kapral GJ, Murray LW, Richardson JS, Richardson DC 10.1107/S0907444909042073 2023-09-20
Gs αs Human Mini-Gs: AHD deleted, G226A/A366S mutations 57 β1 Human γ2 Human Cryo-EM 8IRR - 3.2 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 Beta-2 adrenergic receptor (N-terminal fragment) rotigotine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-21
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 8Y6W - 3.2 FFAR2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - - - AMG7703 pubchem gtoplig chembl_ligand chembl_ligand pubchem
CHEMBL4176503 chembl_ligand pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		butyric acid, propanoic acid, trans-2-methylcrotonic acid, acetic acid Small molecule - - 2025-04-02
Gi/o αi1 Human DN Gi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8IRS - 3.0 DRD2 DRD2 D2 Dopamine A (Rhodopsin) Human BRIL - - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist dopamine Small molecule Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-07
Gi/o αi1 Human DN Gi: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8IRT - 2.7 DRD3 DRD3 D3 Dopamine A (Rhodopsin) Human BRIL - - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist dopamine Small molecule Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-07
Gs αs Human Mini-Gs: AHD deleted, G226A/A366S mutations 60 β1 Human γ2 Human Cryo-EM 8IRV 8IRV_refined 3.1 DRD5 DRD5 D5 Dopamine A (Rhodopsin) Human BRIL - - rotigotine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule Xu P, Huang S, Krumm BE, Zhuang Y, Mao C, Zhang Y, Wang Y, Huang XP, Liu YF, He X, Li H, Yin W, Jiang Y, Zhang Y, Roth BL, Xu HE 10.1038/S41422-023-00808-0 2023-06-07
Gs αs Human modGs: mini-Gs, N-term/AHD from Gi1, scFv16 59 β1 Human γ2 Human Cryo-EM 8ITF - 3.5 TAAR9 Taar9 TAAR9 Orphan A (Rhodopsin) Mouse BRIL Nanobody-35 - N,N-dimethylcyclohexanamine pubchem
Small molecule Agonist - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 59 β1 Human γ2 Bovine Cryo-EM 8IU2 8IU2_refined 3.4 OPSR OPN1LW OPN1LW Opsin (sight) A (Rhodopsin) Human BRIL - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - - - 2024-03-27
Gs αs Human Gαs: N-term & AHD linker from Gi1, scFv16 45 β1 Human γ2 Human Cryo-EM 8IW4 - 3.5 TAAR9 Taar9 TAAR9 Orphan A (Rhodopsin) Mouse BRIL - - SPERMIDINE chembl_ligand pubchem drugbank
Small molecule Agonist - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gi/o αi1 Human WT human Gαi1; Gα-Gγ fusion, NanoBiT tethering 62 β1 Rat γ2 Bovine Cryo-EM 8IY5 - 2.8 EDNRB EDNRB ETB Endothelin A (Rhodopsin) Human - - - endothelin-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Protein Agonist endothelin-2 (Mouse), endothelin-2 (Human), endothelin-1 (Human), endothelin-3 (Human) Protein Sano FK, Akasaka H, Shihoya W, Nureki O 10.7554/ELIFE.85821 2023-08-16
Gq/11 αq Human Gαq with 4A insertion (R332/F333), GDP-locked 99 β1 Human γ2 Human Cryo-EM 8IYS - 3.0 FFAR4 FFAR4 FFA4 Free fatty acid A (Rhodopsin) Human - - - TUG-891 pubchem gtoplig chembl_ligand
Small molecule Agonist linoleic acid, myristic acid, oleic acid, α-linolenic acid Small molecule Yin H, Inoue A, Ma Z, Zhu X, Xia R, Xu Z, Wang N, Duan Y, Zhang A, Guo C, He Y 10.1038/S41422-023-00835-X 2023-06-21
Gi/o αo Human MiniGαo construct (gnao_human based) 57 β1 Human γ2 Human Cryo-EM 8IYW 8IYW_refined 3.5 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - GSK256073 pubchem gtoplig
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Yadav MK, Sarma P, Maharana J, Ganguly M, Mishra S, Zaidi N, Dalal A, Singh V, Saha S, Mahajan G, Sharma S, Chami M, Banerjee R, Shukla AK 10.1038/S41467-024-46239-2 2024-03-06
Gs αs Human mini-Gs: N-term(1-25) & AHD from Gi1, scFv16 59 β1 Human γ2 Human Cryo-EM 8IW7 - 3.0 TAAR9 Taar9 TAAR9 Orphan A (Rhodopsin) Mouse BRIL - - β-phenylethylamine pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist - - Guo L, Cheng J, Lian S, Liu Q, Lu Y, Zheng Y, Zhu K, Zhang M, Kong Y, Zhang C, Rong N, Zhuang Y, Fang G, Jiang J, Zhang T, Han X, Liu Z, Xia M, Liu S, Zhang L, Liberles SD, Yu X, Xu Y, Yang F, Li Q, Sun JP 10.1038/S41586-023-06106-4 2023-05-31
Gi/o αo Human MiniGαo: ΔAHD+muts; receptor N-term fused to M4 59 β1 Human γ2 Human Cryo-EM 8IY9 8IY9_refined 3.4 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Yadav MK, Sarma P, Maharana J, Ganguly M, Mishra S, Zaidi N, Dalal A, Singh V, Saha S, Mahajan G, Sharma S, Chami M, Banerjee R, Shukla AK 10.1038/S41467-024-46239-2 2024-03-06
Gi/o αo Human Mini-Gαo construct (gnao_human based) 58 β1 Human γ2 Human Cryo-EM 8IYH 8IYH_refined 3.3 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - MK 6892 pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Yadav MK, Sarma P, Maharana J, Ganguly M, Mishra S, Zaidi N, Dalal A, Singh V, Saha S, Mahajan G, Sharma S, Chami M, Banerjee R, Shukla AK 10.1038/S41467-024-46239-2 2024-03-06
Gi/o αi1 Human DN Gαi: G203A/A326S 62 β1 Human γ2 Human Cryo-EM 8J1A - 3.2 GPR84 GPR84 GPR84 Orphan A (Rhodopsin) Human BRIL - - - None - - - Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W 10.1038/S41467-023-38985-6 2023-06-21
Gi/o αi1 Human DN Gαi1: G203A/A326S 62 β1 Human γ2 Human Cryo-EM 8J18 - 2.9 GPR84 GPR84 GPR84 Orphan A (Rhodopsin) Human BRIL - - (3R)-3-HYDROXYDODECANOIC ACID pubchem drugbank
Lipid Agonist - - Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W 10.1038/S41467-023-38985-6 2023-06-21
Gi/o αi1 Human DN Gαi: G203A/A326S 62 β1 Human γ2 Human Cryo-EM 8J19 - 3.2 GPR84 GPR84 GPR84 Orphan A (Rhodopsin) Human BRIL - - 6-nonylpyridine-2,4-diol pubchem gtoplig chembl_ligand
Small molecule Agonist - - Liu H, Zhang Q, He X, Jiang M, Wang S, Yan X, Cheng X, Liu Y, Nan FJ, Xu HE, Xie X, Yin W 10.1038/S41467-023-38985-6 2023-06-21
Gi/o αi1 Human Wild-type Gi1/Gβ1/Gγ2 heterotrimer 61 β1 Human γ2 Human Cryo-EM 8J23 8J23_refined 3.2 FFAR2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - - - - None - butyric acid, propanoic acid, trans-2-methylcrotonic acid, acetic acid Small molecule - - 2024-04-17
Gi/o αi1 Human Wild-type human Gi heterotrimer 61 β1 Human γ2 Human Cryo-EM 8J24 8J24_refined 2.6 FFAR2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human BRIL - - acetic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank pubchem drugbank pubchem drugbank pubchem drugbank drugbank drugbank drugbank drugbank drugbank drugbank pubchem
Small molecule Agonist butyric acid, propanoic acid, trans-2-methylcrotonic acid, acetic acid Small molecule Li F, Tai L, Sun X, Lv Z, Tang W, Wang T, Zhao Z, Gong D, Ma S, Tang S, Gu Q, Zhu X, Yu M, Liu X, Wang J 10.1038/S41422-023-00914-Z 2024-01-24
Gi/o αo Human Mini-G: truncated Gαo fragment (1-250) 59 β1 Human γ2 Human Cryo-EM 8J6D 8J6D_refined 3.1 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - - E7 pubchem gtoplig gtoplig
Peptide Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αi1 Human DNGi (Gαi1): S47N/G203A/E345A/A326S 61 β1 Human γ2 Human Cryo-EM 8J6I 8J6I_refined 2.9 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - MK 6892 pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Zhu S, Yuan Q, Li X, He X, Shen S, Wang D, Li J, Cheng X, Duan X, Xu HE, Duan J 10.1016/J.CELREP.2023.113406 2024-04-03
Gi/o αi1 Human DN Gαi1: S47N/G203A/E345A/A326S 61 β1 Human γ2 Human Cryo-EM 8J6J 8J6J_refined 2.8 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - LgBiT GSK256073 pubchem gtoplig
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Zhu S, Yuan Q, Li X, He X, Shen S, Wang D, Li J, Cheng X, Duan X, Xu HE, Duan J 10.1016/J.CELREP.2023.113406 2024-01-10
Gi/o αi1 Human DNGi (Gαi1): S47N/G203A/E345A/A326S 61 β1 Human γ2 Human Cryo-EM 8J6L 8J6L_refined 3.1 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Zhu S, Yuan Q, Li X, He X, Shen S, Wang D, Li J, Cheng X, Duan X, Xu HE, Duan J 10.1016/J.CELREP.2023.113406 2024-04-03
Gi/o αi1 Human DN human Gαi1 (DNGαi1): G203A/A326S 64 β1 Human γ2 Human Cryo-EM 8J6P - 2.6 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - compound 9n [PMID: 18752940] pubchem gtoplig chembl_ligand
nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Small molecule
Small molecule 		Ago-PAM
Agonist 		butyric acid, β-D-hydroxybutyric acid Small molecule Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y 10.1038/S41467-023-43537-Z 2023-12-06
Gi/o αi1 Human DN Gαi1 (DNGαi1), complex stabilizer 64 β1 Human γ2 Human Cryo-EM 8J6R - 2.8 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - MK 6892 pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y 10.1038/S41467-023-43537-Z 2023-12-06
Gi/o αi1 Human Standard human Gi heterotrimer (Gαi1/Gβ1/Gγ2) 63 β1 Human γ2 Human Cryo-EM 8J20 - 3.2 FFAR3 FFAR3 FFA3 Free fatty acid A (Rhodopsin) Human - - - pentanoic acid pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem
AR420626 pubchem
Small molecule
Small molecule 		Agonist
PAM 		butyric acid, propanoic acid Small molecule Li F, Tai L, Sun X, Lv Z, Tang W, Wang T, Zhao Z, Gong D, Ma S, Tang S, Gu Q, Zhu X, Yu M, Liu X, Wang J 10.1038/S41422-023-00914-Z 2024-01-24
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8J21 8J21_refined 3.3 FFAR3 FFAR3 FFA3 Free fatty acid A (Rhodopsin) Human BRIL - - butyric acid pubchem gtoplig chembl_ligand drugbank chembl_ligand pubchem chembl_ligand pubchem
Small molecule Agonist butyric acid, propanoic acid Small molecule Li F, Tai L, Sun X, Lv Z, Tang W, Wang T, Zhao Z, Gong D, Ma S, Tang S, Gu Q, Zhu X, Yu M, Liu X, Wang J 10.1038/S41422-023-00914-Z 2024-01-24
Gi/o αi1 Human G-protein heterotrimer, NanoBiT-stabilized 61 β1 Human γ2 Human Cryo-EM 8J22 8J22_refined 3.2 FFAR2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human BRIL - - CHEMBL4176503 chembl_ligand pubchem
Small molecule Agonist butyric acid, propanoic acid, trans-2-methylcrotonic acid, acetic acid Small molecule Li F, Tai L, Sun X, Lv Z, Tang W, Wang T, Zhao Z, Gong D, Ma S, Tang S, Gu Q, Zhu X, Yu M, Liu X, Wang J 10.1038/S41422-023-00914-Z 2024-01-24
Gi/o αi1 Human DN Gαi1 (DNGαi1) 64 β1 Human γ2 Human Cryo-EM 8J6Q - 2.6 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - compound 9n [PMID: 18752940] pubchem gtoplig chembl_ligand
β-D-hydroxybutyric acid pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Ago-PAM
Agonist 		butyric acid, β-D-hydroxybutyric acid Small molecule Mao C, Gao M, Zang SK, Zhu Y, Shen DD, Chen LN, Yang L, Wang Z, Zhang H, Wang WW, Shen Q, Lu Y, Ma X, Zhang Y 10.1038/S41467-023-43537-Z 2023-12-06
Gi/o αi3 Human DN Gαi3 (P08754): S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8JD6 - 3.4 GRM4 GRM4 mGlu4 Metabotropic glutamate C (Glutamate) Human - - - L-serine-O-phosphate pubchem gtoplig chembl_ligand drugbank drug_central
VU0364770 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		L-serine-O-phosphate, L-glutamic acid Small molecule Wang X, Wang M, Xu T, Feng Y, Shao Q, Han S, Chu X, Xu Y, Lin S, Zhao Q, Wu B 10.1038/S41422-023-00830-2 2023-06-21
Gi/o αo Human Mini-Gαo subunit 58 β1 Human γ2 Human Cryo-EM 8JER 8JER_refined 3.5 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - Acipimox pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Yadav MK, Sarma P, Maharana J, Ganguly M, Mishra S, Zaidi N, Dalal A, Singh V, Saha S, Mahajan G, Sharma S, Chami M, Banerjee R, Shukla AK 10.1038/S41467-024-46239-2 2024-03-06
Gi/o αi1 Human Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 8JGB 8JGB_refined 2.8 MRGX1 MRGPRX1 MRGPRX1 Orphan A (Rhodopsin) Human - - - Conorfamide-Tx2
Peptide Agonist bovine adrenal medulla peptide 8-22 (Human) Peptide Guo L, Zhang Y, Fang G, Tie L, Zhuang Y, Xue C, Liu Q, Zhang M, Zhu K, You C, Xu P, Yuan Q, Zhang C, Liu L, Rong N, Peng S, Liu Y, Wang C, Luo X, Lv Z, Kang D, Yu X, Zhang C, Jiang Y, Dong X, Zhou J, Liu Z, Yang F, Eric Xu H, Sun JP 10.1038/S41467-023-40705-Z 2024-01-10
Gi/o αi1 Human Gi1 heterotrimer used for signaling complex 61 β1 Human γ2 Human Cryo-EM 8JGG 8JGG_refined 3.0 MRGX1 MRGPRX1 MRGPRX1 Orphan A (Rhodopsin) Human - - - bovine adrenal medulla peptide 8-22 (Human) pubchem gtoplig chembl_ligand uniprot
Peptide Agonist bovine adrenal medulla peptide 8-22 (Human) Peptide Guo L, Zhang Y, Fang G, Tie L, Zhuang Y, Xue C, Liu Q, Zhang M, Zhu K, You C, Xu P, Yuan Q, Zhang C, Liu L, Rong N, Peng S, Liu Y, Wang C, Luo X, Lv Z, Kang D, Yu X, Zhang C, Jiang Y, Dong X, Zhou J, Liu Z, Yang F, Eric Xu H, Sun JP 10.1038/S41467-023-40705-Z 2024-01-10
Gi/o αi1 Human DNGai1: G203A/A326S 61 β1 Human γ2 Human Cryo-EM 8JEI - 2.7 HCAR3 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human - - - 4-(n-propyl)amino-3-nitrobenzoic acid pubchem gtoplig chembl_ligand
Small molecule Agonist 3-hydroxyoctanoic acid Small molecule Ye F, Pan X, Zhang Z, Xiang X, Li X, Zhang B, Ning P, Liu A, Wang Q, Gong K, Li J, Zhu L, Qian C, Chen G, Du Y 10.1016/J.CELREP.2024.114895 2024-11-20
Gi/o αo Human MiniGαo construct 58 β1 Human γ2 Human Cryo-EM 8JHN 8JHN_refined 3.8 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - monomethyl fumarate pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Yadav MK, Sarma P, Maharana J, Ganguly M, Mishra S, Zaidi N, Dalal A, Singh V, Saha S, Mahajan G, Sharma S, Chami M, Banerjee R, Shukla AK 10.1038/S41467-024-46239-2 2024-03-06
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 8JHY - 2.9 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - compound 9n [PMID: 18752940] pubchem gtoplig chembl_ligand
Small molecule Ago-PAM butyric acid, β-D-hydroxybutyric acid Small molecule Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z 10.1016/J.MOLCEL.2023.07.030 2023-09-06
Gs αs Human Mini-Gs/Gi chimera, α5 helix from Gs 60 β1 Rat γ2 Bovine Cryo-EM 8JIS 8JIS_refined 2.5 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 15 (P15)
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z 10.1073/PNAS.2303696120 2023-11-08
Gs αs Human DNGs: dominant-negative Gs protein 59 β1 Rat γ2 Bovine Cryo-EM 8JIU 8JIU_refined 2.8 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - SAR425899 pubchem
Peptide Agonist glucagon (Human) Protein Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z 10.1073/PNAS.2303696120 2023-09-13
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 66 β1 Human γ2 Human Cryo-EM 8JJP - 2.9 CML2 CMKLR2 chemerin 2 Chemerin receptor A (Rhodopsin) Human - - - chemerin C-terminal peptide pubchem gtoplig chembl_ligand pubchem
Peptide Agonist chemerin (Human) Peptide - - 2024-08-21
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 8JII - 3.2 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - compound 9n [PMID: 18752940] pubchem gtoplig chembl_ligand
nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Small molecule
Small molecule 		Ago-PAM
Agonist 		butyric acid, β-D-hydroxybutyric acid Small molecule Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z 10.1016/J.MOLCEL.2023.07.030 2023-09-06
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8JIL - 3.5 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z 10.1016/J.MOLCEL.2023.07.030 2023-09-06
Gi/o αi1 Human Gαi1: DN muts S47N/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 8JIM - 3.0 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - monomethyl fumarate pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Zhao C, Wang H, Liu Y, Cheng L, Wang B, Tian X, Fu H, Wu C, Li Z, Shen C, Yu J, Yang S, Hu H, Fu P, Ma L, Wang C, Yan W, Shao Z 10.1016/J.MOLCEL.2023.07.030 2023-09-06
Gs αs Human DNGαs: dominant-negative Gs protein 56 β1 Rat γ2 Bovine Cryo-EM 8JIQ 8JIQ_refined 3.4 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 15 (P15)
Peptide Agonist glucagon (Human) Protein Li Y, Zhou Q, Dai A, Zhao F, Chang R, Ying T, Wu B, Yang D, Wang MW, Cong Z 10.1073/PNAS.2303696120 2023-09-13
Gs αs Human DN Gs: 9 muts incl S54N/G226A/A366S 61 β1 Human γ2 Human Cryo-EM 8JLO - 3.5 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL - - ulotaront pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gs αs Human Dominant-negative Gs (DNGαs) 58 β1 Human γ2 Human Cryo-EM 8JLZ - 3.1 5HT6R HTR6 5-HT6 5-Hydroxytryptamine A (Rhodopsin) Human - Nanobody-35 - CHEMBL365751 chembl_ligand pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule Pei Y, Wen X, Guo SC, Yang ZS, Zhang R, Xiao P, Sun JP 10.1016/J.BBRC.2023.05.126 2023-06-28
Gs αs Human bovine Gs/human Gi chimera, 8 stabilizing muts 59 β1 Human γ2 Human Cryo-EM 8JR9 - 2.6 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - PCO371 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide Zhao LH, He Q, Yuan Q, Gu Y, He X, Shan H, Li J, Wang K, Li Y, Hu W, Wu K, Shen J, Xu HE 10.1038/S41586-023-06467-W 2023-08-02
Gi/o αi1 Human Gi1 heterotrimer, stabilized by scFv16 64 β1 Human γ2 Human Cryo-EM 8JPN - 2.9 SUCR1 SUCNR1 succinate Succinate A (Rhodopsin) Human BRIL - NanoLuc (Oplophorus-luciferin 2-monooxygenase) cis-epoxysuccinic acid pubchem gtoplig chembl_ligand
Small molecule Agonist succinic acid Small molecule Wang T, Tang W, Zhu X, Lv Z, Chen J, Li Y, Sun X, Lv H, Gu Q, Li F, Wang J 10.1038/S41422-024-00968-7 2024-05-22
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 61 β1 Human γ2 Human Cryo-EM 8JEF 8JEF_refined 3.0 HCAR3 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human - - - 3-hydroxyoctanoic acid pubchem gtoplig
Small molecule Agonist 3-hydroxyoctanoic acid Small molecule Ye F, Pan X, Zhang Z, Xiang X, Li X, Zhang B, Ning P, Liu A, Wang Q, Gong K, Li J, Zhu L, Qian C, Chen G, Du Y 10.1016/J.CELREP.2024.114895 2024-12-18
Gi/o αi1 Human WT human Gαi1; Gγ2 human, seq-identical to bovine 61 β1 Human γ2 Human Cryo-EM 8JSP - 3.7 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - ulotaront pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule Xu Z, Guo L, Yu J, Shen S, Wu C, Zhang W, Zhao C, Deng Y, Tian X, Feng Y, Hou H, Su L, Wang H, Guo S, Wang H, Wang K, Chen P, Zhao J, Zhang X, Yong X, Cheng L, Liu L, Yang S, Yang F, Wang X, Yu X, Xu Y, Sun JP, Yan W, Shao Z 10.1038/S41586-023-06804-Z 2023-11-15
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 62 β1 Human γ2 Human Cryo-EM 8JXT 8JXT_refined 3.1 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human - - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule Xia R, Shi S, Xu Z, Vischer HF, Windhorst AD, Qian Y, Duan Y, Liang J, Chen K, Zhang A, Guo C, Leurs R, He Y 10.1038/S41467-024-46840-5 2024-03-20
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S/E245A 62 β1 Human γ2 Human Cryo-EM 8JT6 - 3.0 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - (R)-IHCH-7179 pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule Chen Z, Yu J, Wang H, Xu P, Fan L, Sun F, Huang S, Zhang P, Huang H, Gu S, Zhang B, Zhou Y, Wan X, Pei G, Xu HE, Cheng J, Wang S 10.1016/J.CELL.2024.02.034 2024-02-28
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S/E245A 62 β1 Human γ2 Human Cryo-EM 8JXX 8JXX_refined 3.1 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human - - - clobenpropit pubchem gtoplig chembl_ligand
Small molecule Agonist (partial) CCL16 (Human), histamine Small molecule Xia R, Shi S, Xu Z, Vischer HF, Windhorst AD, Qian Y, Duan Y, Liang J, Chen K, Zhang A, Guo C, Leurs R, He Y 10.1038/S41467-024-46840-5 2024-03-20
Gi/o αi1 Human DN Gi1: S47N/G203A/E245A/A326S 64 β1 Human γ2 Human Cryo-EM 8JZ7 8JZ7_refined 2.6 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - MK 6892 pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Cheng L, Sun S, Wang H, Zhao C, Tian X, Liu Y, Fu P, Shao Z, Chai R, Yan W 10.1038/S41392-023-01625-Y 2023-10-04
Gi/o αo Human Gα subunit identified as Go 59 β1 Human γ2 Human Cryo-EM 8JZP 8JZP_refined 3.5 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - - C5a anaphylatoxin
Protein Agonist C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide - - 2025-01-15
Gi/o αo Human Mini-Go (miniGao1): N-term ScFv16 sequence 59 β1 Human γ2 Human Cryo-EM 8JZZ 8JZZ_refined 3.3 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - - C5a des-Arg (Human) gtoplig
Peptide Agonist (partial) C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide Yadav MK, Maharana J, Yadav R, Saha S, Sarma P, Soni C, Singh V, Saha S, Ganguly M, Li XX, Mohapatra S, Mishra S, Khant HA, Chami M, Woodruff TM, Banerjee R, Shukla AK, Gati C 10.1016/J.CELL.2023.09.020 2023-10-18
Gi/o αi1 Human Gi heterotrimer 61 β1 Human γ2 Human Cryo-EM 8K4N 8K4N_refined 2.8 GPR34 GPR34 GPR34 Orphan A (Rhodopsin) Human - - - (2R)-2-azanyl-3-[oxidanyl-[(2R)-2-oxidanyl-3-tetradec-9-enoyloxy-propoxy]phosphoryl]oxy-propanoic acid
Small molecule Agonist lysophosphatidylserine Lipid - - 2023-10-25
Gi/o αi1 Human DNGai1: DN Gi1 protein 65 β1 Human γ2 Human Cryo-EM 8K4O - 3.0 VGPCR ORF74 ORF74 Unclassified A (Rhodopsin) isolate GK18 BRIL - - CXCL1
Protein Agonist - - - - 2024-07-24
Gi/o αi1 Human Dominant-negative Gαi1 (DNGαi1) 66 β1 Human γ2 Human Cryo-EM 8K4P - 2.8 VGPCR ORF74 ORF74 Unclassified A (Rhodopsin) isolate GK18 BRIL - - - None - - - - - 2024-07-24
Gi/o αi1 Human DN Gαi1 mutant: G203A/A326S 58 β1 Human γ2 Human Cryo-EM 8JXV - 3.2 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human - - - clozapine pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule Xia R, Shi S, Xu Z, Vischer HF, Windhorst AD, Qian Y, Duan Y, Liang J, Chen K, Zhang A, Guo C, Leurs R, He Y 10.1038/S41467-024-46840-5 2024-03-20
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S/E245A 62 β1 Human γ2 Human Cryo-EM 8JXW 8JXW_refined 3.0 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human - - - CHEMBL213912 chembl_ligand pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule Xia R, Shi S, Xu Z, Vischer HF, Windhorst AD, Qian Y, Duan Y, Liang J, Chen K, Zhang A, Guo C, Leurs R, He Y 10.1038/S41467-024-46840-5 2024-03-20
Gi/o αi1 Human DNGi: DN Gi protein for stabilization 62 β1 Human γ2 Human Cryo-EM 8K2X 8K2X_refined 3.2 CXCR3 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human BRIL - NanoBiT (Oplophorus-luciferin 2-monooxygenase catalytic subunit) C-X-C motif chemokine 10
Protein Agonist CXCL9 (Mouse), CCL20 (Human), CCL19 (Human), CXCL10 (Human), CXCL10 (Mouse), CCL11 (Human), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CXCL12α (Human), CXCL9 (Human), CCL5 (Human), CXCL11 (Human) Peptide Jiao H, Pang B, Chiang YC, Chen Q, Pan Q, Ren R, Hu H 10.1038/S41421-023-00617-0 2023-11-29
Gi/o αi3 Rhesus macaque Gαi3 subunit (rhesus macaque) 63 β1 Human γ2 Human Cryo-EM 8K9L - 3.1 OPRM OPRM1 μ Opioid A (Rhodopsin) Human BRIL - - DAMGO pubchem gtoplig chembl_ligand pubchem
BMS-986122 pubchem
Peptide
Small molecule 		Agonist
PAM 		[Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Kaneko S, Imai S, Uchikubo-Kamo T, Hisano T, Asao N, Shirouzu M, Shimada I 10.1038/S41467-024-47792-6 2024-05-29
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S; Gβ1-HiBiT 64 β1 Human γ2 Human Cryo-EM 8KFX 8KFX_refined 3.0 CCR8 CCR8 CCR8 Chemokine A (Rhodopsin) Human - - LgBiT CHEMBL5268017 chembl_ligand pubchem
Small molecule Agonist CCL1 (Human), CCL1 (Mouse), CCL8 (Human) Peptide Jiang S, Lin X, Wu L, Wang L, Wu Y, Xu Z, Xu F 10.1126/SCIADV.ADJ7500 2024-02-07
Gi/o αi2 Human - 63 β1 Human γ2 Human Cryo-EM 8K6M 8K6M_refined 3.3 NPY1R NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human - - - NEUROPEPTIDE-Y chembl_ligand pubchem
Protein Agonist neuropeptide Y (Human), pancreatic polypeptide (Human), peptide YY (Human), pancreatic polypeptide (Mouse), peptide YY (Mouse) Peptide - - 2024-07-31
Gi/o αi2 Human - 63 β1 Human γ2 Human Cryo-EM 8K6N 8K6N_refined 3.2 NPY2R NPY2R Y2 Neuropeptide Y A (Rhodopsin) Human - - - NEUROPEPTIDE-Y chembl_ligand pubchem
Protein Agonist neuropeptide Y (Human), neuropeptide Y-(3-36) (Human), pancreatic polypeptide (Rat), pancreatic polypeptide (Human), peptide YY (Human), pancreatic polypeptide (Mouse), PYY-(3-36) (Human), peptide YY (Mouse) Peptide - - 2024-07-31
Gi/o αi2 Human Gi2 heterotrimer 63 β1 Human γ2 Human Cryo-EM 8K6O 8K6O_refined 3.3 NPY1R NPY1R Y1 Neuropeptide Y A (Rhodopsin) Human - - - [Leu31, Pro34]-NPY pubchem
Peptide Agonist neuropeptide Y (Human), pancreatic polypeptide (Human), peptide YY (Human), pancreatic polypeptide (Mouse), peptide YY (Mouse) Peptide - - 2024-07-31
Gi/o αi1 Human DN Gαi1 mutant: S47N/G203A/A326S 64 β1 Human γ2 Human Cryo-EM 8KFY 8KFY_refined 3.1 CCR8 CCR8 CCR8 Chemokine A (Rhodopsin) Human - - LgBiT
HiBiT 		ZK 756326 pubchem gtoplig chembl_ligand
Small molecule Agonist CCL1 (Human), CCL1 (Mouse), CCL8 (Human) Peptide Jiang S, Lin X, Wu L, Wang L, Wu Y, Xu Z, Xu F 10.1126/SCIADV.ADJ7500 2024-02-07
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S; Gβ1-HiBiT 64 β1 Human γ2 Human Cryo-EM 8KFZ 8KFZ_refined 3.3 CCR8 CCR8 CCR8 Chemokine A (Rhodopsin) Human - - LgBiT - None - CCL1 (Human), CCL1 (Mouse), CCL8 (Human) Peptide Jiang S, Lin X, Wu L, Wang L, Wu Y, Xu Z, Xu F 10.1126/SCIADV.ADJ7500 2024-02-07
Gi/o αi1 Human Human/bovine Gi heterotrimer, no chimeras 59 β1 Bovine γT1 Bovine Cryo-EM 8P12 - 3.2 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - - None - - - - - 2024-11-20
Gi/o αi1 Human Gi: human Gαi1, bovine Gβ1γT1 94 β1 Bovine γT1 Bovine Cryo-EM 8P13 - 5.2 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - - None - - - - - 2024-11-20
Gi/o αi1 Human Human Gαi1, bovine Gβ1, bovine Gγ-T1 96 β1 Bovine γT1 Bovine Cryo-EM 8P15 - 5.9 OPSD RHO Rhodopsin Opsin (sight) A (Rhodopsin) Bovine - - - - None - - - - - 2024-11-20
Gs αs Human Human Gs-short heterotrimer; Gβ1 His-tag/3C 56 β1 Human γ2 Human Cryo-EM 8POK 8POK_refined 3.4 HRH2 HRH2 H2 Histamine A (Rhodopsin) Human - Nanobody-35 - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule Kock Z, Schnelle K, Persechino M, Umbach S, Schihada H, Januliene D, Parey K, Pockes S, Kolb P, Dotsch V, Moller A, Hilger D, Bernhard F 10.1038/S41467-024-46096-Z 2024-03-06
Gs αs Human DNGs: 8 muts for active-state stability 56 β1 Human γ2 Human Cryo-EM 8QJ2 8QJ2_refined 3.4 MC4R MC4R MC4 Melanocortin A (Rhodopsin) Human BRIL Nanobody-35 Red fluorescent protein drFP583 pN162
Protein Agonist ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide - - 2024-09-25
Gs αs Human mini-Gαs399: Gs/Golf chimera, receptor fusion 58 β1 Human γ2 Human Cryo-EM 8KGK 8KGK_refined 3.2 GPR61 GPR61 GPR61 Orphan A (Rhodopsin) Human - Nanobody-35 - - None - - - Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S 10.1038/S41467-023-41654-3 2023-10-11
Gs αs Human Engineered mini-Gs for complex stabilization 58 β1 Human γ2 Human Cryo-EM 8KH4 8KH4_refined 3.1 GP161 GPR161 GPR161 Orphan A (Rhodopsin) Human - Nanobody-35 - - None - - - Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S 10.1038/S41467-023-41654-3 2023-10-11
Gs αs Human Mini-Gs399 fused to receptor C-terminus 58 β1 Human γ2 Human Cryo-EM 8KH5 - 2.8 GP174 GPR174 GPR174 Orphan A (Rhodopsin) Human - Nanobody-35 - Lysophosphotidylserine pubchem drugbank
Lipid Agonist lysophosphatidylserine Lipid Nie Y, Qiu Z, Chen S, Chen Z, Song X, Ma Y, Huang N, Cyster JG, Zheng S 10.1038/S41467-023-41654-3 2023-10-18
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 8PKM - 2.9 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - Befiradol pubchem chembl_ligand pubchem
Phosphatidylinositol-4-phosphate
Small molecule
Small molecule 		Agonist
PAM 		5-hydroxytryptamine Small molecule - - 2024-05-29
Gs αs Human Mini-Gs399 heterotrimer, truncated short Gs 58 β1 Human γ2 Human Cryo-EM 8PM2 - 2.9 TAA7F Taar7f TAAR7F Orphan A (Rhodopsin) Mouse - Nanobody-35 - N,N-dimethylcyclohexanamine pubchem
Small molecule Agonist - - Gusach A, Lee Y, Khoshgrudi AN, Mukhaleva E, Ma N, Koers EJ, Chen Q, Edwards PC, Huang F, Kim J, Mancia F, Verprintsev DB, Vaidehi N, Weyand SN, Tate CG 10.1101/2023.07.07.547762 2023-08-09
Gi/o αo Human Gα subunit with K46E (pinKE) mutation 97 β1 Human γ2 Human Cryo-EM 8U02 8U02_refined 3.3 DRD2 DRD2 D2 Dopamine A (Rhodopsin) Human - - - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist dopamine Small molecule Knight KM, Krumm BE, Kapolka NJ, Ludlam WG, Cui M, Mani S, Prytkova I, Obarow EG, Lefevre TJ, Wei W, Ma N, Huang XP, Fay JF, Vaidehi N, Smrcka AV, Slesinger PA, Logothetis DE, Martemyanov KA, Roth BL, Dohlman HG 10.1038/S41467-024-50964-Z 2024-08-21
Gs αs Human Human Gs heterotrimer; Gα is Gnas-2 variant 50 β1 Human γ2 Human Cryo-EM 8S2T - 3.3 ADRB1 ADRB1 β1 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - LEVISOPRENALINE chembl_ligand pubchem drug_central
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline Small molecule Merino F, Kock Z, Ermel U, Dahlhaus P, Grimm A, Seybert A, Kubicek J, Frangakis AS, Dotsch V, Hilger D, Bernhard F 10.1016/J.STR.2025.07.020 2025-05-21
Gi/o αi1 Human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 8SAI 8SAI_refined 3.3 GPR34 GPR34 GPR34 Orphan A (Rhodopsin) Human BRIL - - LysoPS (18:1) pubchem
Small molecule Agonist lysophosphatidylserine Lipid Xia A, Yong X, Zhang C, Lin G, Jia G, Zhao C, Wang X, Hao Y, Wang Y, Zhou P, Yang X, Deng Y, Wu C, Chen Y, Zhu J, Tang X, Liu J, Zhang S, Zhang J, Xu Z, Hu Q, Zhao J, Yue Y, Yan W, Su Z, Wei Y, Zhou R, Dong H, Shao Z, Yang S 10.1073/PNAS.2308435120 2023-10-04
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 8SG1 - 2.9 CML1 CMKLR1 chemerin Chemerin receptor A (Rhodopsin) Human - - - chemerin C-terminal peptide pubchem gtoplig chembl_ligand pubchem
Peptide Agonist 18R-HEPE, EPA, resolvin E1, chemerin (Human) Peptide Zhang X, Weiss T, Cheng MH, Chen S, Ambrosius CK, Czerniak AS, Li K, Feng M, Bahar I, Beck-Sickinger AG, Zhang C 10.1371/JOURNAL.PBIO.3002188 2023-11-01
Gi/o αo Human GoA K46E (pinKE): blocks GTP binding 62 β1 Human γ2 Human Cryo-EM 8TZQ 8TZQ_refined 3.2 DRD2 DRD2 D2 Dopamine A (Rhodopsin) Human - - - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist dopamine Small molecule Knight KM, Krumm BE, Kapolka NJ, Ludlam WG, Cui M, Mani S, Prytkova I, Obarow EG, Lefevre TJ, Wei W, Ma N, Huang XP, Fay JF, Vaidehi N, Smrcka AV, Slesinger PA, Logothetis DE, Martemyanov KA, Roth BL, Dohlman HG 10.1038/S41467-024-50964-Z 2024-08-21
Gi/o αi1 Human Gi1 heterotrimer 60 β1 Human γ2 Human Cryo-EM 8U1U - 3.1 CCR8 CCR8 CCR8 Chemokine A (Rhodopsin) Human - - eGFP - - - CCL1 (Human), CCL1 (Mouse), CCL8 (Human) Peptide - - 2023-12-20
Gs αs Human MiniGs399, stabilized mini-Gα construct 55 β1 Human γ2 Human Cryo-EM 8U26 8U26_refined 2.5 NK1R TACR1 NK1 Tachykinin A (Rhodopsin) Human - Nanobody-35 - substance P (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist neuropeptide K (Human), substance P (Human), neuropeptide γ (Human), neurokinin B (Human), neurokinin A (Human), hemokinin 1 (Mouse) Peptide Chen M, Schmid MF, Chiu W 10.1038/S41592-023-02082-9 2023-11-15
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 8U4N 8U4N_refined 2.7 CXCR4 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human - - mEGFP - None - CXCL12ε (Human), CXCL12 (Mouse), CXCL12δ (Human), CXCL12α (Human), CXCL12β (Human), CXCL12φ (Human), CXCL12γ (Human) Peptide Saotome K, McGoldrick LL, Ho JH, Ramlall TF, Shah S, Moore MJ, Kim JH, Leidich R, Olson WC, Franklin MC 10.1038/S41594-024-01397-1 2024-03-13
Gs αs Human MiniGs GTPase domain fused to receptor C-term 61 β1 Human γ2 Human Cryo-EM 8SMV 8SMV_refined 2.7 GP161 GPR161 GPR161 Orphan A (Rhodopsin) Human - Nanobody-35 - Cholesterol pubchem drugbank
Small molecule Allosteric agonist - - Hoppe N, Harrison S, Hwang SH, Chen Z, Karelina M, Deshpande I, Suomivuori CM, Palicharla VR, Berry SP, Tschaikner P, Regele D, Covey DF, Stefan E, Marks DS, Reiter J, Dror RO, Evers AS, Mukhopadhyay S, Manglik A 10.1101/2023.05.23.540554 2024-02-21
Gs αs Human DN Gs: 8 muts S54N/G226A/E268A...I285T 60 β1 Human γ2 Human Cryo-EM 8TYW 8TYW_refined 3.4 GPR6 GPR6 GPR6 Orphan A (Rhodopsin) Human - Nanobody-35 - - None - sphingosine 1-phosphate Lipid Barekatain M, Johansson LC, Lam JH, Chang H, Sadybekov AV, Han GW, Russo J, Bliesath J, Brice NL, Carlton MBL, Saikatendu KS, Sun H, Murphy ST, Monenschein H, Schiffer HH, Popov P, Lutomski CA, Robinson CV, Liu ZJ, Hua T, Katritch V, Cherezov V 10.1126/SCISIGNAL.ADO8741 2024-12-04
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 8U4O - 3.3 CXCR4 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human - - monomeric eGFP Stromal cell-derived factor 1
Protein Agonist CXCL12ε (Human), CXCL12 (Mouse), CXCL12δ (Human), CXCL12α (Human), CXCL12β (Human), CXCL12φ (Human), CXCL12γ (Human) Peptide Saotome K, McGoldrick LL, Ho JH, Ramlall TF, Shah S, Moore MJ, Kim JH, Leidich R, Olson WC, Franklin MC 10.1038/S41594-024-01397-1 2024-03-13
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 8U4P - 3.2 CXCR4 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human - - monomeric eGFP plerixafor pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (partial) CXCL12ε (Human), CXCL12 (Mouse), CXCL12δ (Human), CXCL12α (Human), CXCL12β (Human), CXCL12φ (Human), CXCL12γ (Human) Peptide Saotome K, McGoldrick LL, Ho JH, Ramlall TF, Shah S, Moore MJ, Kim JH, Leidich R, Olson WC, Franklin MC 10.1038/S41594-024-01397-1 2024-03-13
Gi/o αi1 Human DN Gi: S47C/G202T/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 8U4Q - 3.4 CXCR4 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human - - GFP REGN7663 Fab (chain H)
REGN7663 Fab (chain L)
Protein
Protein 		Inverse agonist CXCL12ε (Human), CXCL12 (Mouse), CXCL12δ (Human), CXCL12α (Human), CXCL12β (Human), CXCL12φ (Human), CXCL12γ (Human) Peptide Saotome K, McGoldrick LL, Ho JH, Ramlall TF, Shah S, Moore MJ, Kim JH, Leidich R, Olson WC, Franklin MC 10.1038/S41594-024-01397-1 2024-03-13
Gs αs Human DN Gαs subunit 59 β1 Human γ2 Human Cryo-EM 8U8F 8U8F_refined 3.5 GPR3 GPR3 GPR3 Orphan A (Rhodopsin) Human - - - palmitic acid pubchem gtoplig chembl_ligand drugbank
Lipid Agonist sphingosine 1-phosphate Lipid Russell IC, Zhang X, Bumbak F, McNeill SM, Josephs TM, Leeming MG, Christopoulos G, Venugopal H, Flocco MM, Sexton PM, Wootten D, Belousoff MJ 10.1021/ACS.BIOCHEM.3C00647 2024-03-06
Gs αs Human Gs-short splice variant 57 β1 Human γ2 Human Cryo-EM 8UNM - 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs short isoform 59 β1 Human γ2 Human Cryo-EM 8UNN - 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Native human Gs heterotrimer (short isoform) 57 β1 Human γ2 Human Cryo-EM 8UNO - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs short splice variant (isoform 4) 60 β1 Human γ2 Human Cryo-EM 8UNP - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gα subunit: Gs-short splice variant 61 β1 Human γ2 Human Cryo-EM 8UNQ - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs-short splice variant 57 β1 Human γ2 Human Cryo-EM 8UNU - 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gs heterotrimer (α-short isoform) 59 β1 Human γ2 Human Cryo-EM 8UNV - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gαs short splice variant 59 β1 Human γ2 Human Cryo-EM 8UNW - 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gs heterotrimer; Gα short splice variant 62 β1 Human γ2 Human Cryo-EM 8UNX - 3.6 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs-short splice variant (GNAS2) 60 β1 Human γ2 Human Cryo-EM 8UNY - 3.6 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs-short splice variant 85 β1 Human γ2 Human Cryo-EM 8UO1 8UO1_refined 3.6 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs short splice variant 72 β1 Human γ2 Human Cryo-EM 8UO2 8UO2_refined 3.6 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs-short splice variant (isoform 2) 91 β1 Human γ2 Human Cryo-EM 8UO3 8UO3_refined 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs short splice variant (GNAS2) 74 β1 Human γ2 Human Cryo-EM 8UO4 8UO4_refined 4.0 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gi/o αi1 Human DN Gαi1 62 β1 Human γ2 Human Cryo-EM 8UTD 8UTD_refined 3.2 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - CHEMBL2057618 chembl_ligand pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Kang HJ, Krumm BE, Tassou A, Geron M, DiBerto JF, Kapolka NJ, Gumpper RH, Sakamoto K, Dewran Kocak D, Olsen RHJ, Huang XP, Zhang S, Huang KL, Zaidi SA, Nguyen MT, Jo MJ, Katritch V, Fay JF, Scherrer G, Roth BL 10.1016/J.CELL.2024.11.001 2025-02-26
Gs αs Human DN mini-Gs: G226A/A366S mutations 59 β1 Human γ2 Human Cryo-EM 8W87 - 2.8 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - METHAMPHETAMINE chembl_ligand pubchem drugbank drug_central
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F 10.1038/S41586-023-06775-1 2023-11-22
Gs αs Human DN Gs: G226A/A366S 60 β1 Human γ2 Human Cryo-EM 8W88 - 2.6 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - ulotaront pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F 10.1038/S41586-023-06775-1 2023-11-22
Gs αs Human DN mini-Gs: G226A/A366S; Gi2 loop for Nb35; ΔAHD 60 β1 Human γ2 Human Cryo-EM 8W89 - 3.0 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - β-phenylethylamine pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F 10.1038/S41586-023-06775-1 2023-11-22
Gs αs Human mini-Gαs (G226A/A366S); cleaved TAAR1 fusion 60 β1 Human γ2 Human Cryo-EM 8W8A - 2.8 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human - Nanobody-35 - CHEMBL3684869 chembl_ligand pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F 10.1038/S41586-023-06775-1 2023-11-22
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S/E245A 61 β1 Human γ2 Human Cryo-EM 8W8B - 3.0 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - ulotaront pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule Liu H, Zheng Y, Wang Y, Wang Y, He X, Xu P, Huang S, Yuan Q, Zhang X, Wang L, Jiang K, Chen H, Li Z, Liu W, Wang S, Xu HE, Xu F 10.1038/S41586-023-06775-1 2023-11-22
Gs αs Human Native human Gs short isoform heterotrimer 59 β1 Human γ2 Human Cryo-EM 8W8Q 8W8Q_refined 2.9 GP101 GPR101 GPR101 Orphan A (Rhodopsin) Human BRIL Nanobody-35 - - None - - - Yang Z, Wang JY, Yang F, Zhu KK, Wang GP, Guan Y, Ning SL, Lu Y, Li Y, Zhang C, Zheng Y, Zhou SH, Wang XW, Wang MW, Xiao P, Yi F, Zhang C, Zhang PJ, Xu F, Liu BH, Zhang H, Yu X, Gao N, Sun JP 10.1038/S41589-023-01456-6 2024-01-03
Gs αs Human mini-Gs: N-term(1-25) → Gαi1(1-18), scFv16 59 β1 Human γ2 Human Cryo-EM 8WC3 - 3.0 TAAR1 Taar1 TA1 Trace amine A (Rhodopsin) Mouse - - - ulotaront pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine Small molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human mini-Gs: N-term(1-25) replaced by Gαi1, scFv16 59 β1 Human γ2 Human Cryo-EM 8WC4 - 3.1 TAAR1 Taar1 TA1 Trace amine A (Rhodopsin) Mouse BRIL - - CHEMBL476516 chembl_ligand pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine Small molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human modGαs: mini-Gs w/ Gαi1 N-term (1-18), scFv16 58 β1 Human γ2 Human Cryo-EM 8WC5 - 3.3 TAAR1 Taar1 TA1 Trace amine A (Rhodopsin) Mouse - - - Tetramethylammonium pubchem drugbank
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine Small molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human DNGs: 9 muts incl S54N/G226A/A366S 59 β1 Rat γ2 Bovine Cryo-EM 8WG7 8WG7_refined 2.5 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - - None - glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cong Z, Zhao F, Li Y, Luo G, Mai Y, Chen X, Chen Y, Lin S, Cai X, Zhou Q, Yang D, Wang MW 10.1038/S41421-024-00649-0 2024-03-06
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 64 β1 Human γ2 Human Cryo-EM 8WOG - 3.0 SUCR1 SUCNR1 succinate Succinate A (Rhodopsin) Human BRIL - - succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank
Small molecule Agonist succinic acid Small molecule Liu A, Liu Y, Zhang W, Ye RD 10.1016/J.CELREP.2024.114381 2024-09-11
Gi/o αi1 Human DN Gαi1 (DNGαi1): S47N/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 8UGY - 3.3 5HT1E HTR1E 5-HT1E 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - CHEMBL252719 chembl_ligand pubchem
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule Zilberg G, Parpounas AK, Warren AL, Fiorillo B, Provasi D, Filizola M, Wacker D 10.1126/SCIADV.ADK4855 2024-05-01
Gi/o αi1 Human Gαi1, active-state stabilized; DN mutations 61 β1 Human γ2 Human Cryo-EM 8UH3 - 3.3 5HT1E HTR1E 5-HT1E 5-Hydroxytryptamine A (Rhodopsin) Human b562RIL - - SETIPTILINE chembl_ligand pubchem drugbank
Lipid Agonist tryptamine, 5-hydroxytryptamine Small molecule Zilberg G, Parpounas AK, Warren AL, Fiorillo B, Provasi D, Filizola M, Wacker D 10.1126/SCIADV.ADK4855 2024-05-01
Gs αs Human Human Gs heterotrimer; Gα short splice variant 59 β1 Human γ2 Human Cryo-EM 8UNL - 3.3 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs subunit, short isoform (P63092) 61 β1 Human γ2 Human Cryo-EM 8UNR - 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs short splice variant 61 β1 Human γ2 Human Cryo-EM 8UNS - 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Gs α short splice variant (Gnas2) 60 β1 Human γ2 Human Cryo-EM 8UNT - 3.4 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gαs-short splice variant 57 β1 Human γ2 Human Cryo-EM 8UNZ 8UNZ_refined 3.8 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gs αs Human Human Gs heterotrimer: Gαs-short/Gβ1/Gγ2 58 β1 Human γ2 Human Cryo-EM 8UO0 - 3.5 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - c-Epi pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule Papasergi-Scott MM, Perez-Hernandez G, Batebi H, Gao Y, Eskici G, Seven AB, Panova O, Hilger D, Casiraghi M, He F, Maul L, Gmeiner P, Kobilka BK, Hildebrand PW, Skiniotis G 10.1038/S41586-024-07153-1 2024-03-06
Gi/o αi1 Human DN human Gαi1 61 β1 Human γ2 Human Cryo-EM 8UUJ - 2.6 HCAR2 Hcar2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Mouse - - - compound (+)17a [PMID: 20363624] pubchem gtoplig chembl_ligand chembl_ligand pubchem pubchem
Small molecule Agonist β-D-hydroxybutyric acid Small molecule Kang HJ, Krumm BE, Tassou A, Geron M, DiBerto JF, Kapolka NJ, Gumpper RH, Sakamoto K, Dewran Kocak D, Olsen RHJ, Huang XP, Zhang S, Huang KL, Zaidi SA, Nguyen MT, Jo MJ, Katritch V, Fay JF, Scherrer G, Roth BL 10.1016/J.CELL.2024.11.001 2025-02-26
Gs αs Human DNGs: 8 muts; Gβ fused to HiBiT 60 β1 Human γ2 Human Cryo-EM 8VHF 8VHF_refined 3.5 GP119 GPR119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human BRIL Nanobody-35 LgBiT
HiBiT 		MBX-2982 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide Small molecule - - 2024-10-30
Gi/o αi1 Human Wild-type human Gi heterotrimer 63 β1 Human γ2 Human Cryo-EM 8VVE - 3.3 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - nor-binaltorphimine pubchem gtoplig chembl_ligand
Small molecule Inverse agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2025-01-15
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 63 β1 Human γ2 Human Cryo-EM 8VVF 8VVF_refined 3.0 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - JDTic pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem
Small molecule Inverse agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Tyson AS, Khan S, Motiwala Z, Han GW, Zhang Z, Ranjbar M, Styrpejko D, Ramos-Gonzalez N, Woo S, Villers K, Landaker D, Kenakin T, Shenvi R, Majumdar S, Gati C 10.1038/S41589-024-01812-0 2025-01-15
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S; Gβ1-HiBit 63 β1 Human γ2 Human Cryo-EM 8VY7 - 2.7 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human BRIL - LgBiT compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
Cholesterol pubchem drugbank
Small molecule
Small molecule 		Ago-PAM
Agonist 		- - - - 2024-04-03
Gs αs Human Gs heterotrimer 47 β1 Rat γ2 Bovine Cryo-EM 8W8W - 2.9 MC3R MC3R MC3 Melanocortin A (Rhodopsin) Human BRIL Nanobody-35 - Alpha-MSH pubchem
Small molecule Agonist ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide - - 2025-03-19
Gs αs Human Gs protein heterotrimer 47 β1 Rat γ2 Bovine Cryo-EM 8W8Y - 2.9 MC3R MC3R MC3 Melanocortin A (Rhodopsin) Human BRIL Nanobody-35 - γ-MSH (Human) pubchem gtoplig uniprot uniprot uniprot pubchem
Peptide Agonist ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide - - 2025-03-19
Gs αs Human mini-Gs: N-term replaced w/ Gi1, for scFv16 58 β1 Human γ2 Human Cryo-EM 8WC6 - 3.2 TAAR1 Taar1 TA1 Trace amine A (Rhodopsin) Mouse BRIL Nanobody-35 - β-phenylethylamine pubchem gtoplig chembl_ligand drugbank pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine Small molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human mini-Gs/Gi1 chimera: N-term swap for scFv16 58 β1 Human γ2 Human Cryo-EM 8WC7 - 3.1 TAAR1 Taar1 TA1 Trace amine A (Rhodopsin) Mouse - - - CHEMBL4301324 chembl_ligand pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine Small molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gs αs Human mini-Gs: N-term(1-25)->Gi1(1-18), scFv16 56 β1 Human γ2 Human Cryo-EM 8WC8 - 2.9 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human - - - CHEMBL476516 chembl_ligand pubchem
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Shang P, Rong N, Jiang JJ, Cheng J, Zhang MH, Kang D, Qi L, Guo L, Yang GM, Liu Q, Zhou Z, Li XB, Zhu KK, Meng QB, Han X, Yan W, Kong Y, Yang L, Wang X, Lei D, Feng X, Liu X, Yu X, Wang Y, Li Q, Shao ZH, Yang F, Sun JP 10.1016/J.CELL.2023.10.014 2023-12-27
Gi/o αi1 Human Wild-type Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 8X3L 8X3L_refined 3.1 CNR2 CNR2 CB2 Cannabinoid A (Rhodopsin) Human - - - CHEMBL5422946 chembl_ligand pubchem
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Yang X, Zhou P, Shen S, Hu Q, Tian C, Xia A, Wang Y, Yang Z, Nan J, Zhou Y, Chen S, Tian X, Wu C, Lin G, Zhang L, Wang K, Zheng T, Zou J, Yan W, Shao Z, Yang S 10.1073/PNAS.2401091121 2024-11-20
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8WWI 8WWI_refined 3.4 MCHR1 MCHR1 MCH1 Melanin-concentrating hormone A (Rhodopsin) Human - - - - None - melanin-concentrating hormone (Human) Peptide - - 2024-11-13
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 8WWJ - 3.0 MCHR1 MCHR1 MCH1 Melanin-concentrating hormone A (Rhodopsin) Human - - Fusion protein 1
Fusion protein 2 		- None - melanin-concentrating hormone (Human) Peptide - - 2024-11-13
Gi/o αi1 Human Standard human Gi1 heterotrimer 63 β1 Human γ2 Human Cryo-EM 8WWM 8WWM_refined 2.8 MCHR1 MCHR1 MCH1 Melanin-concentrating hormone A (Rhodopsin) Human - - Fusion protein 1
Fusion protein 2 		melanin-concentrating hormone (Human) pubchem gtoplig uniprot uniprot uniprot
Peptide Agonist melanin-concentrating hormone (Human) Peptide Ye X, Liu G, Li X, He B, Tao Y, Guan J, Mu Y, Liu H, Gong W 10.1038/S41421-024-00754-0 2024-11-13
Gi/o αi1 Human Gi1 heterotrimer complex 63 β1 Human γ2 Human Cryo-EM 8WWN 8WWN_refined 2.7 MCHR1 MCHR1 MCH1 Melanin-concentrating hormone A (Rhodopsin) Human - - Fusion protein 1
Fusion protein 2 		melanin-concentrating hormone (Human) pubchem gtoplig uniprot uniprot uniprot
Peptide Agonist melanin-concentrating hormone (Human) Peptide Ye X, Liu G, Li X, He B, Tao Y, Guan J, Mu Y, Liu H, Gong W 10.1038/S41421-024-00754-0 2024-11-13
Gs αs Human MiniGs: receptor-LgBiT, Gβ1-HiBiT/SmBiT fusion 59 β1 Human γ2 Human Cryo-EM 8X79 8X79_refined 2.4 PI2R PTGIR IP Prostanoid A (Rhodopsin) Human BRIL Nanobody-35 - MRE-269 pubchem gtoplig chembl_ligand
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule - - 2024-03-06
Gi/o αi1 Human WT human Gαi1, rat Gβ1, bovine Gγ2 62 β1 Rat γ2 Bovine Cryo-EM 8XBH 8XBH_refined 2.8 GPR34 GPR34 GPR34 Orphan A (Rhodopsin) Human - - - CHEMBL4758243 chembl_ligand pubchem
Small molecule Agonist lysophosphatidylserine Lipid - - 2023-12-27
Gi/o αi1 Human DN Gi: G203A/A326S 60 β1 Human γ2 Human Cryo-EM 8XGU - 3.0 KISSR KISS1R kisspeptin Kisspeptin A (Rhodopsin) Human - - - TAK448
Peptide Agonist kisspeptin-10 (Mouse), kisspeptin-52 (Mouse), kisspeptin-13 (Human), kisspeptin-14 (Human), kisspeptin-54 (Human), kisspeptin-10 (Human), kisspeptin-52 (Rat) Peptide Wu Z, Chen G, Qiu C, Yan X, Xu L, Jiang S, Xu J, Han R, Shi T, Liu Y, Gao W, Wang Q, Li J, Ye F, Pan X, Zhang Z, Ning P, Zhang B, Chen J, Du Y 10.1126/SCIADV.ADN7771 2024-10-30
Gi/o αi1 Human DNGαi1: S47C/G202T/G203A/E245A/A326S; Gβ1-HiBiT 62 β1 Human γ2 Human Cryo-EM 8XML - 2.6 CCR8 CCR8 CCR8 Chemokine A (Rhodopsin) Human BRIL - HiBiT - None - CCL1 (Human), CCL1 (Mouse), CCL8 (Human) Peptide - - 2025-01-01
Gi/o αi1 Human DN Gαi1: G203A/A326S 61 β1 Rat γ2 Bovine Cryo-EM 8XOS - 3.2 PAR1 F2R PAR1 Proteinase-activated A (Rhodopsin) Human - - LgBiT - - - thrombin (Human), thrombin (Rat), thrombin (Mouse) Peptide - - 2024-09-18
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326A 62 β1 Human γ2 Human Cryo-EM 8XWP 8XWP_refined 3.2 EDNRB EDNRB ETB Endothelin A (Rhodopsin) Human - - - endothelin-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Protein Agonist endothelin-2 (Mouse), endothelin-2 (Human), endothelin-1 (Human), endothelin-3 (Human) Protein Tani K, Maki-Yonekura S, Kanno R, Negami T, Hamaguchi T, Hall M, Mizoguchi A, Humbel BM, Terada T, Yonekura K, Doi T 10.1038/S42003-024-06905-Z 2024-10-02
Gi/o αi1 Human WT Gi heterotrimer (Table 1); receptor R124Y mut 62 β1 Human γ2 Human Cryo-EM 8XWQ - 4.6 EDNRB EDNRB ETB Endothelin A (Rhodopsin) Human - - - endothelin-1 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Protein Agonist endothelin-2 (Mouse), endothelin-2 (Human), endothelin-1 (Human), endothelin-3 (Human) Protein Tani K, Maki-Yonekura S, Kanno R, Negami T, Hamaguchi T, Hall M, Mizoguchi A, Humbel BM, Terada T, Yonekura K, Doi T 10.1038/S42003-024-06905-Z 2024-10-02
Gi/o αo Human MiniGαoA construct 61 β1 Human γ2 Human Cryo-EM 8XXH 8XXH_refined 2.8 CXCR2 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - - - CXCL2
Protein Agonist CXCL5 (Rat), CXCL5 (Mouse), CXCL1 (Rat), CXCL7 (Human), CXCL1 (Mouse), CXCL2 (Mouse), CXCL3 (Human), CXCL2 (Human), CXCL5 (Human), CXCL6 (Human), CXCL2 (Rat), CXCL3 (Rat), CXCL3 (Mouse), CXCL1 (Human), CXCL8 (Human) Peptide Saha S, Sano FK, Sharma S, Ganguly M, Mishra S, Dalal A, Akasaka H, Kobayashi TA, Zaidi N, Tiwari D, Roy N, Yadav MK, Banerjee N, Saha S, Mohapatra S, Itoh Y, Chevigne A, Banerjee R, Shihoya W, Nureki O, Shukla AK 10.1016/J.MOLCEL.2025.01.024 2025-01-15
Gi/o αo Human MiniGαoA: truncated Gαo GTPase domain 59 β1 Human γ2 Human Cryo-EM 8XXR - 3.2 CXCR2 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - - - - None - CXCL5 (Rat), CXCL5 (Mouse), CXCL1 (Rat), CXCL7 (Human), CXCL1 (Mouse), CXCL2 (Mouse), CXCL3 (Human), CXCL2 (Human), CXCL5 (Human), CXCL6 (Human), CXCL2 (Rat), CXCL3 (Rat), CXCL3 (Mouse), CXCL1 (Human), CXCL8 (Human) Peptide Saha S, Sano FK, Sharma S, Ganguly M, Mishra S, Dalal A, Akasaka H, Kobayashi TA, Zaidi N, Tiwari D, Roy N, Yadav MK, Banerjee N, Saha S, Mohapatra S, Itoh Y, Chevigne A, Banerjee R, Shihoya W, Nureki O, Shukla AK 10.1016/J.MOLCEL.2025.01.024 2025-01-15
Gi/o αo Human Mini-GaoA protein, stabilizer 60 β1 Human γ2 Human Cryo-EM 8XXX 8XXX_refined 3.2 CXCR2 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - - - CXCL6
Protein Agonist CXCL5 (Rat), CXCL5 (Mouse), CXCL1 (Rat), CXCL7 (Human), CXCL1 (Mouse), CXCL2 (Mouse), CXCL3 (Human), CXCL2 (Human), CXCL5 (Human), CXCL6 (Human), CXCL2 (Rat), CXCL3 (Rat), CXCL3 (Mouse), CXCL1 (Human), CXCL8 (Human) Peptide Saha S, Sano FK, Sharma S, Ganguly M, Mishra S, Dalal A, Akasaka H, Kobayashi TA, Zaidi N, Tiwari D, Roy N, Yadav MK, Banerjee N, Saha S, Mohapatra S, Itoh Y, Chevigne A, Banerjee R, Shihoya W, Nureki O, Shukla AK 10.1016/J.MOLCEL.2025.01.024 2025-01-15
Gi/o αi1 Human Gi: G203A/A326S mutations; AHD not modeled 61 β1 Human γ2 Human Cryo-EM 8XYD 8XYD_refined 2.9 PTAFR PTAFR PAF Platelet-activating factor A (Rhodopsin) Human - - - PAF pubchem gtoplig chembl_ligand drugbank
Lipid Agonist PAF Lipid Fan W, Xu Y, He X, Luo P, Zhu J, Li J, Wang R, Yuan Q, Wu K, Hu W, Zhao Y, Xu S, Cheng X, Wang Y, Xu HE, Zhuang Y 10.1016/J.CELREP.2024.114422 2024-11-13
Gi/o αi1 Human DN Gαi1 muts reduce nucleotide affinity 61 β1 Human γ2 Human Cryo-EM 8XZF 8XZF_refined 3.0 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - WN561
Peptide Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Wang WW, Ji SY, Zhang W, Zhang J, Cai C, Hu R, Zang SK, Miao L, Xu H, Chen LN, Yang Z, Guo J, Qin J, Shen DD, Liang P, Zhang Y, Zhang Y 10.1016/J.CELL.2024.02.004 2024-03-20
Gi/o αi1 Human DN Gαi1 mutant for stabilization 61 β1 Human γ2 Human Cryo-EM 8XZG 8XZG_refined 3.2 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - apelin-13 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Wang WW, Ji SY, Zhang W, Zhang J, Cai C, Hu R, Zang SK, Miao L, Xu H, Chen LN, Yang Z, Guo J, Qin J, Shen DD, Liang P, Zhang Y, Zhang Y 10.1016/J.CELL.2024.02.004 2024-03-27
Gi/o αi1 Human DN Gαi1 via mutagenesis, lower GDP affinity 62 β1 Human γ2 Human Cryo-EM 8XZH 8XZH_refined 2.6 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - MM07 pubchem gtoplig chembl_ligand
Peptide Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Wang WW, Ji SY, Zhang W, Zhang J, Cai C, Hu R, Zang SK, Miao L, Xu H, Chen LN, Yang Z, Guo J, Qin J, Shen DD, Liang P, Zhang Y, Zhang Y 10.1016/J.CELL.2024.02.004 2024-03-20
Gi/o αi2 Human DN Gαi2: S47N/G204A/E246A/A327S 63 β1 Human γ2 Human Cryo-EM 8Y45 8Y45_refined 3.5 OPRD OPRD1 δ Opioid A (Rhodopsin) Human BRIL - - ADL5859 pubchem gtoplig chembl_ligand
Small molecule Agonist [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2024-11-27
Gq/11 αq Human - 60 β1 Human γ2 Human Cryo-EM 8Y51 8Y51_refined 3.3 BRS3 BRS3 BB3 Bombesin A (Rhodopsin) Human - - - - None - - - - - 2025-02-12
Gi/o αi1 Human Human Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 8Y62 - 3.2 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - C16:0 ceramide pubchem
Small molecule Agonist (partial) LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide Lin H, Ma C, Cai K, Guo L, Wang X, Lv L, Zhang C, Lin J, Zhang D, Ye C, Wang T, Huang S, Han J, Zhang Z, Gao J, Zhang M, Pu Z, Li F, Guo Y, Zhou X, Qin C, Yi F, Yu X, Kong W, Jiang C, Sun JP 10.1126/SCIENCE.ADO4188 2025-02-05
Gi/o αi1 Human Human Gi1 heterotrimer; Gβ1 His-tag/3C site 60 β1 Human γ2 Human Cryo-EM 8Y63 8Y63_refined 3.2 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - - - Cer(d18:0/20:0) pubchem
Small molecule Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide - - 2025-02-05
Gi/o αi1 Human DN Gi1: G203A/A326S 63 β1 Rat γ2 Bovine Cryo-EM 8Y73 - 2.8 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - DAMGO pubchem gtoplig chembl_ligand pubchem
MPAM-15 pubchem
Peptide
Small molecule 		Agonist
PAM 		[Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2025-08-06
Gs αs Human Gs heterotrimer; α5 tail QRMHLRQYELL = Gnas2 60 β1 Human γ2 Human Cryo-EM 8YFO - 2.7 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - Ac-LA-PTH
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide - - 2025-09-03
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 8YG4 - 2.6 PTH1R PTH1R PTH1 Parathyroid hormone B1 (Secretin) Human - Nanobody-35 - LA-PTH-R1
Peptide Agonist PTHrP-(1-36) (Human), PTHrP (Human), TIP39 (Human), PTH (Human), PTH (Mouse), PTH (Rat) Peptide - - 2025-09-03
Gs αs Human MiniGs: G226A/A366S, only α5 fragment modeled 60 β1 Human γ2 Human Cryo-EM 8YN3 - 2.6 HRH2 HRH2 H2 Histamine A (Rhodopsin) Human - Nanobody-35 - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W 10.1038/S41467-024-52585-Y 2024-10-09
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8YN5 - 2.7 HRH3 HRH3 H3 Histamine A (Rhodopsin) Human - - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W 10.1038/S41467-024-52585-Y 2024-10-09
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8YN6 - 2.8 HRH3 HRH3 H3 Histamine A (Rhodopsin) Human - - - imetit pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist histamine Small molecule Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W 10.1038/S41467-024-52585-Y 2024-10-09
Gi/o αo Human MiniGo (miniGαo49), truncated Gαo 61 β1 Human γ2 Human Cryo-EM 8YN7 - 2.8 HRH3 HRH3 H3 Histamine A (Rhodopsin) Human - - - immethridine pubchem gtoplig chembl_ligand
Small molecule Agonist histamine Small molecule - - 2024-10-16
Gs αs Human DN bovine Gs (confirmed via α5 tail seq) 58 β1 Human γ2 Human Cryo-EM 8YUT - 2.7 HRH2 HRH2 H2 Histamine A (Rhodopsin) Human - Nanobody-35 - amthamine pubchem gtoplig chembl_ligand
Small molecule Agonist histamine Small molecule - - 2024-06-05
Gi/o αi1 Human DN human Gi1 (DNGi1), stabilizing mutations 64 β1 Human γ2 Human Cryo-EM 8YUV - 3.0 HRH3 HRH3 H3 Histamine A (Rhodopsin) Human - - - immepip pubchem gtoplig chembl_ligand
Small molecule Agonist histamine Small molecule - - 2024-06-05
Gs αs Human Gs α subunit, short isoform, native human 57 β1 Human γ2 Human Cryo-EM 8YW5 8YW5_refined 2.8 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - retatrutide pubchem gtoplig
Protein Agonist glucagon (Human) Protein Li W, Zhou Q, Cong Z, Yuan Q, Li W, Zhao F, Xu HE, Zhao LH, Yang D, Wang MW 10.1038/S41421-024-00700-0 2024-08-07
Gs αs Human Gα chimera: Gi1 UniProt but Gs α5 tail 60 β1 Human γ2 Human Cryo-EM 8YWF - 2.7 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - retatrutide pubchem gtoplig
Protein Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein - - 2025-04-16
Gs αs Human Gs α subunit, short isoform 60 β1 Human γ2 Human Cryo-EM 8Z68 - 2.6 GPR68 GPR68 GPR68 Proton A (Rhodopsin) Human - - - - None - - - - - 2025-04-23
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S 64 β1 Human γ2 Human Cryo-EM 8Z7J 8Z7J_refined 3.1 APJ APLNR apelin Apelin A (Rhodopsin) Human BRIL - - JN241-9
Protein Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Yue Y, Liu L, Wu L, Xu C, Na M, Liu S, Liu Y, Li F, Liu J, Shi S, Lei H, Zhao M, Yang T, Ji W, Wang A, Hanson MA, Stevens RC, Liu J, Xu F 10.1038/S41467-024-55555-6 2025-01-22
Gi/o αi1 Human DN Gαi1 (DNGαi1) 64 β1 Human γ2 Human Cryo-EM 8Z87 - 2.7 HCAR1 HCAR1 HCA1 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - CHEMBL2146910 chembl_ligand pubchem
Small molecule Agonist D-lactic acid Small molecule - - 2025-11-05
Gi/o αi1 Human DNGαi1: DN Gi1 w/ stabilizing muts 64 β1 Human γ2 Human Cryo-EM 8Z8A - 2.8 HCAR1 HCAR1 HCA1 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - D-lactic acid pubchem gtoplig chembl_ligand drugbank pubchem gtoplig chembl_ligand pubchem drugbank pubchem drugbank drugbank pubchem drugbank drugbank drugbank
Small molecule Agonist D-lactic acid Small molecule Gao M, Zang S, Zhu Y, Xi K, Du Y, Cheng S, Miao L, Lu Y, Mao C, Zhang Y, Ma X 10.1126/SCISIGNAL.ADW1483 2025-10-29
Gi/o αi1 Human DN Gαi1: G203A/A326S, stabilizes trimer 64 β1 Human γ2 Human Cryo-EM 8Z8B - 2.7 HCAR1 HCAR1 HCA1 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - - None - D-lactic acid Small molecule Gao M, Zang S, Zhu Y, Xi K, Du Y, Cheng S, Miao L, Lu Y, Mao C, Zhang Y, Ma X 10.1126/SCISIGNAL.ADW1483 2025-10-29
Gs αs Human DN Gs: G226A mutation 60 β1 Human γ2 Human Cryo-EM 8ZD1 - 2.6 GPR4 gpr4 GPR4 Proton A (Rhodopsin) Western clawed frog BRIL - - - None - - - Wen X, Shang P, Chen H, Guo L, Rong N, Jiang X, Li X, Liu J, Yang G, Zhang J, Zhu K, Meng Q, He X, Wang Z, Liu Z, Cheng H, Zheng Y, Zhang B, Pang J, Liu Z, Xiao P, Chen Y, Liu L, Luo F, Yu X, Yi F, Zhang P, Yang F, Deng C, Sun JP 10.1016/J.CELL.2024.12.001 2025-02-26
G12/13 α13 Human MiniGα13 construct 56 β1 Human γ2 Human Cryo-EM 8ZX5 - 3.0 GPR55 GPR55 GPR55 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - - LgBiT
HiBiT 		AM251 pubchem gtoplig chembl_ligand
Small molecule Agonist N-palmitoylethanolamine, lysophosphatidylinositol, anandamide, 2-arachidonoylglycerolphosphoinositol, 2-arachidonoylglycerol Small molecule - - 2024-11-13
G12/13 α13 Human Mini-Gαi/13: Gαi2 N-term + Gα13 core 56 β1 Human γ2 Human Cryo-EM 8ZME - 3.2 PAR2 F2RL1 PAR2 Proteinase-activated A (Rhodopsin) Human - - - - - - - - Zhu X, Xia R, Zhang A, Guo C, Xu Z, He Y 10.1038/S41421-025-00851-8 2025-05-28
Gs αs Human Gs heterotrimer 60 β1 Human γ2 Human Cryo-EM 8ZR5 - 3.3 GP119 GPR119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - DS-8500a pubchem gtoplig chembl_ligand
Small molecule Agonist SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide Small molecule - - 2024-06-19
Gs αs Human Gs α subunit, short isoform 60 β1 Human γ2 Human Cryo-EM 8ZRK - 2.8 GP119 GPR119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - GSK-1292263 chembl_ligand pubchem drugbank
Small molecule Agonist SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide Small molecule - - 2024-06-19
Gs αs Human Mini-Gs (mini-Gas): Gαi2 body + Gs α5 helix 58 β1 Human γ2 Human Cryo-EM 8ZSJ - 2.8 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - - None - 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Jiang K, Zheng Y, Zeng L, Wang L, Li F, Pu J, Lu Y, Zhao S, Xu F 10.1016/J.CELREP.2024.114505 2024-07-24
Gs αs Human DN Gs: G226A mutation 59 β1 Human γ2 Human Cryo-EM 9AUC - 2.4 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- Calcitonin gene-related peptide 1
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Danev R, Christopoulos A, Wootten D, Sexton PM 10.1021/ACS.BIOCHEM.4C00114 2024-04-24
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 9B65 9B65_refined 3.0 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - MDMB-Fubinaca pubchem gtoplig
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Rangari VA, O'Brien ES, Powers AS, Slivicki RA, Bertels Z, Appourchaux K, Aydin D, Ramos-Gonzalez N, Mwirigi J, Lin L, Mangutov E, Sobecks BL, Awad-Agbaria Y, Uphade MB, Aguilar J, Peddada TN, Shiimura Y, Huang XP, Folarin-Hines J, Payne M, Kalathil A, Varga BR, Kobilka BK, Pradhan AA, Cameron MD, Kumar KK, Dror RO, Gereau RW 4th, Majumdar S 10.1038/S41586-025-08618-7 2025-03-05
Gs αs Human MiniGs399, stabilizes active-state complex 61 β1 Human γ2 Human Cryo-EM 9BIP 9BIP_refined 2.8 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 - - None - - - Howard MK, Hoppe N, Huang XP, Mitrovic D, Billesbolle CB, Macdonald CB, Mehrotra E, Rockefeller Grimes P, Trinidad DD, Delemotte L, English JG, Coyote-Maestas W, Manglik A 10.1016/J.CELL.2024.11.036 2025-01-15
Gi/o αi1 Human Wild-type Gi1 heterotrimer for complex formation 61 β1 Human γ2 Human Cryo-EM 9BQJ - 3.3 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - RO-76 pubchem
Small molecule Agonist (partial) - - - - 2024-09-11
Gi/o αo Human Mini-GoA: truncated mini-G of Gnao1 60 β1 Human γ2 Human Cryo-EM 9BSB - 2.3 DRD2 DRD2 D2 Dopamine A (Rhodopsin) Human BRIL - - (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist dopamine Small molecule Jain MK, Gumpper RH, Slocum ST, Schmitz GP, Madsen JS, Tummino TA, Suomivuori CM, Huang XP, Shub L, DiBerto JF, Kim K, DeLeon C, Krumm BE, Fay JF, Keiser M, Hauser AS, Dror RO, Shoichet B, Gloriam DE, Nichols DE, Roth BL 10.1016/J.NEURON.2025.06.012 2025-09-17
Gs αs Human DNGs: dominant-negative Gs protein 59 β1 Human γ2 Human Cryo-EM 9BTW - 3.0 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP3 		- cagrilintide pubchem gtoplig drugbank
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Johnson RM, Keov P, Mariam Z, Deganutti G, Christopoulos G, Hick CA, Reedtz-Runge S, Glendorf T, Ballarin-Gonzalez B, Raun K, Bayly-Jones C, Wootten D, Sexton PM 10.1038/S41467-025-58680-Y 2025-04-16
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 9BUC - 3.4 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - cagrilintide pubchem gtoplig drugbank
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide - - 2025-04-23
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 9BUD - 2.5 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - cagrilintide pubchem gtoplig drugbank
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide - - 2025-04-23
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 9BUE - 3.6 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - cagrilintide pubchem gtoplig drugbank
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Johnson RM, Keov P, Mariam Z, Deganutti G, Christopoulos G, Hick CA, Reedtz-Runge S, Glendorf T, Ballarin-Gonzalez B, Raun K, Bayly-Jones C, Wootten D, Sexton PM 10.1038/S41467-025-58680-Y 2025-04-16
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 9BUY - 2.9 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - - - LM189 pubchem
compound-6FA pubchem
Small molecule
Small molecule 		Agonist
PAM 		(-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule - - 2025-05-28
Gs αs Human Gs heterotrimer 60 β1 Human γ2 Human Cryo-EM 9BYO - 2.3 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Exendin-asp3
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein - - 2025-06-11
Gs αs Human - 51 β1 Human γ2 Human Cryo-EM 9C0K - 2.7 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Exendin-phe1
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein - - 2025-06-11
Gi/o αo Human DN Gαo: S47N/G204A/E246A/M249K/A326S 61 β1 Rat γ2 Human Cryo-EM 9F33 - 3.1 DRD3 DRD3 D3 Dopamine A (Rhodopsin) Human - - Green fluorescent protein CHEMBL4551160 chembl_ligand pubchem
Small molecule Agonist dopamine Small molecule - - 2024-09-18
Gi/o αi1 Human DN Gαi1 62 β1 Human γ2 Human Cryo-EM 9CGJ - 2.8 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - - - C6-Quino pubchem
Small molecule Agonist (partial) [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2025-04-02
Gi/o αi1 Human DN Gi1 protein, likely G203A/A326S 61 β1 Human γ2 Human Cryo-EM 9CGK - 2.6 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - - - C5-Quino pubchem
Small molecule Agonist [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2025-04-02
Gi/o αi1 Human DN Gαi1 protein: G203A/A326S mutations 63 β1 Human γ2 Human Cryo-EM 9CM7 - 3.3 FFAR2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - - - AZ-1729 pubchem
CHEMBL4176503 chembl_ligand pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		butyric acid, propanoic acid, trans-2-methylcrotonic acid, acetic acid Small molecule - - 2025-06-25
Gi/o αi1 Human WT human Gi1 heterotrimer (Gαi1/Gβ1/Gγ2) 63 β1 Human γ2 Human Cryo-EM 9D61 9D61_refined 3.6 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - JDTic pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem
Small molecule Inverse agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Tyson AS, Khan S, Motiwala Z, Han GW, Zhang Z, Ranjbar M, Styrpejko D, Ramos-Gonzalez N, Woo S, Villers K, Landaker D, Kenakin T, Shenvi R, Majumdar S, Gati C 10.1038/S41589-024-01812-0 2025-01-15
Gi/o αo Human Gγ2(oa)-Gαo fusion via GSAGSAGSA linker 61 β1 Human γ2 Human Cryo-EM 9DYE - 2.9 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - buspirone pubchem gtoplig chembl_ligand drugbank drug_central pubchem
PtdIns4P pubchem
Small molecule
Small molecule 		Agonist
PAM 		5-hydroxytryptamine Small molecule Warren AL, Zilberg G, Abbassi A, Abraham A, Yang S, Wacker D 10.1126/SCIADV.ADU9851 2025-08-13
Gi/o αi1 Human G protein: S47N/G203A/E245A/A326S mutations 65 β1 Human γ2 Human Cryo-EM 9DYF - 2.7 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - (3aS,12bR)-asenapine pubchem
PtdIns4P pubchem
Small molecule
Small molecule 		Agonist (partial)
PAM 		5-hydroxytryptamine Small molecule - - 2025-08-13
Gs αs Human Dominant-negative Gs heterotrimer 60 β1 Human γ2 Human Cryo-EM 9E2A - 3.3 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - GLP-1(7-36)NH2 pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein El Eid L, Manchanda Y, Austin G, Deane-Alder K, Rujan RM, Mariam Z, Oqua AI, Belousoff MJ, de la Serna JB, Sloop KW, Rutter GA, Montoya A, Withers DJ, Millership SJ, Bouzakri K, Jones B, Reynolds CA, Sexton PM, Wootten D, Deganutti G, Tomas A 10.1126/SCIADV.ADW0899 2025-10-29
G12/13 α13 Human MiniGα13: ΔAHD + stabilizing mutations 57 β1 Human γ2 Human Cryo-EM 9E51 - 2.9 AGRL2 ADGRL2 ADGRL2 ADGRL B2 (Adhesion) Human - - - - None - - - Yang X, He F, Lopez-Pajares V, Porter DF, Garbett K, Siprashvili Z, Ducoli L, Meyers RM, Reynolds DL, Lan Huong Bui D, Hong A, Nguyen DT, Jing Y, Mondal S, Ko L, Tao S, Singal B, Sando R, Skiniotis G, Khavari PA 10.1073/PNAS.2508436122 2025-11-12
Gs αs Human DNGs: dominant-negative Gs protein 59 β1 Human γ2 Human Cryo-EM 9EBN - 3.4 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - - None - glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cary BP, Hager MV, Mariam Z, Morris RK, Belousoff MJ, Deganutti G, Sexton PM, Wootten D, Gellman SH 10.1073/PNAS.2407574122 2025-03-26
Gs αs Human DN Gs protein 60 β1 Human γ2 Human Cryo-EM 9E9S - 2.7 PD2R PTGDR DP1 Prostanoid A (Rhodopsin) Human - Nanobody-35 - PGD2 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist PGF2α, PGE1, Δ12-PGJ2, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Davoudinasab B, Raskovalov A, Lee W, Kim D, Kim H, Lam JH, Han GW, Katritch V, Cherezov V 10.1038/S41467-025-64002-Z 2025-09-03
Gi/o αi1 Human DN Gαi1 (DNGαi1) with stabilizing mutations 60 β1 Human γ2 Human Cryo-EM 9EBH - 3.6 AA3R ADORA3 A3 Adenosine A (Rhodopsin) Human - - - adenosine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist adenosine Small molecule Zhang L, Mobbs JI, Bennetts FM, Venugopal H, Nguyen ATN, Christopoulos A, van der Es D, Heitman LH, May LT, Glukhova A, Thal DM 10.1038/S41467-025-62872-X 2025-08-20
Gs αs Human DN Gs protein 58 β1 Human γ2 Human Cryo-EM 9EBO - 3.1 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - GLP-1 (ACPC18)
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Cary BP, Hager MV, Mariam Z, Morris RK, Belousoff MJ, Deganutti G, Sexton PM, Wootten D, Gellman SH 10.1073/PNAS.2407574122 2025-03-26
G12/13 α13 Human miniG13 protein 51 β1 Human - - Cryo-EM 9ECJ - 2.9 P2RY8 P2RY8 P2RY8 Orphan A (Rhodopsin) Human - - - S-geranylgeranyl-L-glutathione pubchem
Small molecule Agonist - - - - 2025-11-05
Gs αs Human mini-Gαs399 heterotrimer stabilizes complex 59 β1 Human γ2 Human Cryo-EM 9EE8 - 2.6 AA2AR ADORA2A A2A Adenosine A (Rhodopsin) Human - Nanobody-35 - adenosine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist adenosine Small molecule Bi M, Wang X, Wang J, Xu J, Sun W, Adediwura VA, Miao Y, Cheng Y, Ye L 10.1038/S41467-025-56434-4 2025-04-09
Gs αs Human mini-Gαs399 (truncated Gs) aids complex 58 β1 Human γ2 Human Cryo-EM 9EE9 - 3.2 AA2AR ADORA2A A2A Adenosine A (Rhodopsin) Human - Nanobody-35 - adenosine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist adenosine Small molecule Bi M, Wang X, Wang J, Xu J, Sun W, Adediwura VA, Miao Y, Cheng Y, Ye L 10.1038/S41467-025-56434-4 2025-04-09
Gs αs Human Mini-Gαs399, truncated for stability 58 β1 Human γ2 Human Cryo-EM 9EEA - 3.4 AA2AR ADORA2A A2A Adenosine A (Rhodopsin) Human - Nanobody-35 - adenosine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist adenosine Small molecule Bi M, Wang X, Wang J, Xu J, Sun W, Adediwura VA, Miao Y, Cheng Y, Ye L 10.1038/S41467-025-56434-4 2025-04-09
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 9EGO - 3.2 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - methyl (2R)-2-({(1M)-5-methyl-1-[3-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonyl}amino)-2-(thiophen-2-yl)propanoate pubchem
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule Tummino TA, Iliopoulos-Tsoutsouvas C, Braz JM, O'Brien ES, Stein RM, Craik V, Tran NK, Ganapathy S, Liu F, Shiimura Y, Tong F, Ho TC, Radchenko DS, Moroz YS, Rosado SR, Bhardwaj K, Benitez J, Liu Y, Kandasamy H, Normand C, Semache M, Sabbagh L, Glenn I, Irwin JJ, Kumar KK, Makriyannis A, Basbaum AI, Shoichet BK 10.1038/S41467-025-57136-7 2025-04-30
Gi/o αi1 Human Recombinant human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 9EJC - 3.0 VGPCR ORF74 ORF74 Unclassified A (Rhodopsin) isolate GK18 - - - CXCL1
Protein Agonist - - Park JB, Sahoo B, Sahoo AR, Kim D, Seo HD, Bowman J, Kwak MJ, Suh S, Buck M, Dai X, Jung JU 10.1038/S41467-025-63457-4 2025-09-03
Gi/o αi1 Human WT human Gαi1 + bovine Gβ1γ1 60 β1 Bovine γT1 Bovine Cryo-EM 9EPR - 4.9 B1B1U5 HaRh1 Rhodopsin Opsin (sight) A (Rhodopsin) Hasarius adansoni - - - all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Tejero O, Pamula F, Koyanagi M, Nagata T, Afanasyev P, Das I, Deupi X, Sheves M, Terakita A, Schertler GFX, Rodrigues MJ, Tsai CJ 10.1038/S41467-024-53208-2 2024-10-30
Gi/o αi1 Human DN mutant: G203A/A326S mutations 63 β1 Human γ2 Human Cryo-EM 9ERX 9ERX_refined 2.9 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - HU-210 pubchem gtoplig chembl_ligand
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule - - 2024-06-26
Gs αs Human Engineered miniGs (mutated/truncated Gαs) 59 β1 Human γ2 Human Cryo-EM 9EW2 - 3.2 FZD7 FZD7 FZD7 WNT F (Frizzled) Human - Nanobody-35 - - None - - - - - 2024-10-02
G12/13 α13 Human Mini-Gα13/Ni2: Gαi2 N-term(1-30), scFv16 56 β1 Human γ2 Human Cryo-EM 9GE3 - 2.9 GPR55 GPR55 GPR55 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - - Green fluorescent protein 1-palmitoyl-2-lysophosphatidylinositol
Small molecule Agonist N-palmitoylethanolamine, lysophosphatidylinositol, anandamide, 2-arachidonoylglycerolphosphoinositol, 2-arachidonoylglycerol Small molecule - - 2025-03-05
Gi/o αo Human DN Gαo: S47N/G204A/E246A/M249K/A326S 61 β1 Rat γ2 Human Cryo-EM 9F34 - 3.1 DRD3 DRD3 D3 Dopamine A (Rhodopsin) Human - - eGFP CHEMBL4551160 chembl_ligand pubchem
Small molecule Agonist dopamine Small molecule - - 2024-09-18
Gi/o αi1 Human Gi1 heterotrimer complex 61 β1 Human γ2 Human Cryo-EM 9HYI - 2.3 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - DP81 pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule - - 2026-01-21
Gs αs Human Gs heterotrimer (short isoform) 60 β1 Human γ2 Human Cryo-EM 9I52 - 2.8 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - - Beta-2 adrenergic receptor 19B
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule - - 2025-07-16
Gs αs Human Gs heterotrimer, short α isoform 60 β1 Human γ2 Human Cryo-EM 9I54 - 2.7 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - - Beta-2 adrenergic receptor fusion segment Compound 24 pubchem
Small molecule Agonist 5-hydroxytryptamine, noradrenaline, dopamine Small molecule - - 2025-07-16
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 62 β1 Human γ2 Human Cryo-EM 9IJ9 - 2.7 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human - - - compound 28.1 [PMID: 36847646] pubchem gtoplig chembl_ligand
Small molecule Allosteric agonist - - - - 2024-07-24
Gi/o αi1 Human Dominant-negative human Gαi1 (DNGi) 61 β1 Human γ2 Human Cryo-EM 9IK8 - 2.8 SSR1 SSTR1 SST1 Somatostatin A (Rhodopsin) Human BRIL - - pasireotide pubchem gtoplig drugbank chembl_ligand drug_central
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide - - 2025-04-30
Gi/o αi1 Human DNGi: DN Gαi1 subunit 61 β1 Human γ2 Human Cryo-EM 9IK9 - 3.4 SSR1 SSTR1 SST1 Somatostatin A (Rhodopsin) Human BRIL - - LANREOTIDE chembl_ligand pubchem pubchem drugbank
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Zeng Z, Liao Q, Gan S, Li X, Xiong T, Xu L, Li D, Jiang Y, Chen J, Ye R, Du Y, Wong T 10.1016/J.APSB.2025.03.043 2025-04-30
Gi/o αi1 Human DN G protein for complex assembly 61 β1 Human γ2 Human Cryo-EM 9J0F - 2.8 P2Y14 P2RY14 P2Y14 P2Y A (Rhodopsin) Human BRIL - - NADH pubchem drugbank
Small molecule Agonist UDP, UDP-galactose, UDP-glucose, UDP N-acetyl-glucosamine, UDP-glucuronic acid Small molecule Gu Q, Lv Z, Wang T, Tang W, Guo X, Huang X, Li F, Wang J 10.1038/S41421-025-00799-9 2025-06-04
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 9IPV - 2.5 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - - JR14a pubchem gtoplig chembl_ligand
Small molecule Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide - - 2025-04-23
Gs αs Human Human Gs, engineered for thermal stability 58 β1 Human γ2 Human Cryo-EM 9IV1 - 3.0 AGRD1 ADGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - - - dihydrotestosterone pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist dihydrotestosterone Small molecule Yang Z, Ping YQ, Wang MW, Zhang C, Zhou SH, Xi YT, Zhu KK, Ding W, Zhang QY, Song ZC, Zhao RJ, He ZL, Wang MX, Qi L, Ullmann C, Ricken A, Schoneberg T, Gan ZJ, Yu X, Xiao P, Yi F, Liebscher I, Sun JP 10.1016/J.CELL.2025.01.006 2025-02-12
Gs αs Human Gs-short isoform, tail seq QRMHLRQYELL 60 β1 Human γ2 Human Cryo-EM 9IV6 - 2.7 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - - - - None - - - - - 2025-07-30
Gs αs Human Gs/Gi1 chimera; α5 tail is Gs-type 62 β1 Human γ2 Human Cryo-EM 9IVG 9IVG_refined 3.0 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - glucagon-like peptide 1-(9-36) pubchem
Small molecule Agonist (partial) glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Li J, Li G, Mai Y, Liu X, Yang D, Zhou Q, Wang MW 10.1016/J.APSB.2024.09.002 2024-11-27
Gs αs Human Gαs/Gαi1 chimera (per UniProt metadata) 62 β1 Human γ2 Human Cryo-EM 9IVM - 3.2 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - glucagon-like peptide 1-(9-36) pubchem
LSN3318839 pubchem gtoplig chembl_ligand chembl_ligand pubchem
Small molecule
Small molecule 		Agonist (partial)
PAM 		glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein - - 2024-11-13
Gs αs Human Engineered Gs alpha subunit 59 β1 Human γ2 Human Cryo-EM 9IXJ - 2.9 HRH2 HRH2 H2 Histamine A (Rhodopsin) Human - Nanobody-35 - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule - - 2025-07-30
G12/13 α13 Human MiniGαi/13: Gα13 α5 helix fragment 57 β1 Human γ2 Human Cryo-EM 9IY8 9IY8_refined 3.0 GPR55 GPR55 GPR55 GPR18, GPR55 and GPR119 A (Rhodopsin) Human BRIL - - - None - N-palmitoylethanolamine, lysophosphatidylinositol, anandamide, 2-arachidonoylglycerolphosphoinositol, 2-arachidonoylglycerol Small molecule Chang H, Li X, Shen L, Ge X, Hao S, Wu L, Liu S, Liu J, Cherezov V, Hua T 10.1038/S41422-024-01046-8 2025-01-01
Gi/o αi1 Human DN Gαi1: G203A/A326S; NanoBiT fusion peptide 60 β1 Human γ2 Human Cryo-EM 9IZA - 3.1 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - SCH 900271 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule - - 2025-04-02
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 61 β1 Human γ2 Human Cryo-EM 9IZC - 2.7 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - CHEMBL2057618 chembl_ligand pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Pan X, Ye F, Ning P, Yu Y, Zhang Z, Wang J, Chen G, Wu Z, Qiu C, Li J, Chen B, Zhu L, Qian C, Gong K, Du Y 10.1371/JOURNAL.PBIO.3003126 2025-04-02
Gi/o αi1 Human DN Gαi1: G203A/A326S; WT human Gβ1/Gγ2 60 β1 Human γ2 Human Cryo-EM 9IZD - 3.2 HCAR1 HCAR1 HCA1 Hydroxycarboxylic acid A (Rhodopsin) Human - - - CHEMBL2146910 chembl_ligand pubchem
Small molecule Agonist D-lactic acid Small molecule - - 2025-04-02
Gi/o αi1 Human Gαi1 (G203A/A326S); Gβ1 C-term HiBiT tag 61 β1 Human γ2 Mouse Cryo-EM 9IZF - 3.1 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human BRIL - LgBiT tag LPA pubchem
Lipid Agonist LPA Small molecule - - 2025-01-01
G12/13 α13 Human Gi2-mini-G13 chimera: ΔAHD, G13 specificity 56 β1 Human γ2 Mouse Cryo-EM 9IZH - 3.0 LPAR1 LPAR1 LPA1 Lysophospholipid (LPA) A (Rhodopsin) Human BRIL - LgBiT LPA pubchem
Lipid Agonist LPA Small molecule Suzuki S, Tanaka K, Kamegawa A, Nishikawa K, Suzuki H, Oshima A, Fujiyoshi Y 10.1016/J.JSB.2024.108164 2025-01-01
Gi/o αi1 Human DN Gi subunit 62 β1 Human γ2 Human Cryo-EM 9J0B - 2.9 P2Y14 P2RY14 P2Y14 P2Y A (Rhodopsin) Human BRIL - - UDP-glucose pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist UDP, UDP-galactose, UDP-glucose, UDP N-acetyl-glucosamine, UDP-glucuronic acid Small molecule Gu Q, Lv Z, Wang T, Tang W, Guo X, Huang X, Li F, Wang J 10.1038/S41421-025-00799-9 2025-06-04
Gs αs Human Gs/Gi1 chimera for nanobody stabilization 60 β1 Rat γ2 Bovine Cryo-EM 9J1P 9J1P_refined 3.0 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - g1:Ox
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Fan S, Li J, Zhuang J, Zhou Q, Mai Y, Lin B, Wang MW, Wu C 10.1021/JACS.4C12808 2025-02-26
Gi/o αi1 Human DN Gαi1: G203A/A326S 61 β1 Human γ2 Human Cryo-EM 9J8Z - 3.4 HCAR1 HCAR1 HCA1 Hydroxycarboxylic acid A (Rhodopsin) Human - - - - None - D-lactic acid Small molecule Pan X, Ye F, Ning P, Yu Y, Zhang Z, Wang J, Chen G, Wu Z, Qiu C, Li J, Chen B, Zhu L, Qian C, Gong K, Du Y 10.1371/JOURNAL.PBIO.3003126 2025-04-02
Gs αs Human Engineered Gs protein for improved stability 59 β1 Human γ2 Human Cryo-EM 9JCQ - 2.6 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 - Lysophosphatidylcholine (LPC) pubchem
Small molecule PAM - - - - 2025-07-09
Gi/o αi1 Human DN Gαi1: G203A/A326S 64 β1 Human γ2 Human Cryo-EM 9JED - 2.6 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human BRIL - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule Jin SS, Zhang H, Yan JH, Wu CR, Cai XQ, Wu K, Wang MW, Xu HE, Yang DH, Jiang Y 10.1038/S41401-025-01633-4 2025-09-10
Gi/o αi1 Human Gαi1 (G203A/A326S); Gβ1 C-term HiBiT fusion 64 β1 Human γ2 Bovine Cryo-EM 9JEQ - 3.1 HRH3 HRH3 H3 Histamine A (Rhodopsin) Human BRIL - LgBiT histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule Jin SS, Zhang H, Yan JH, Wu CR, Cai XQ, Wu K, Wang MW, Xu HE, Yang DH, Jiang Y 10.1038/S41401-025-01633-4 2025-09-24
Gs αs Human DNGs short isoform: 8 mutations 57 β1 Human γ2 Human Cryo-EM 9JFW - 3.1 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 Endoglucanase H - None - - - Yue X, Peng L, Liu S, Zhang B, Zhang X, Chang H, Pei Y, Li X, Liu J, Shui W, Wu L, Xu H, Liu ZJ, Hua T 10.1038/S41422-025-01092-W 2025-04-23
Gi/o αi1 Human Human Gi1 heterotrimer 58 β1 Human γ2 Human Cryo-EM 9JFY - 3.2 NPFF2 NPFFR2 NPFF2 Neuropeptide FF/neuropeptide AF A (Rhodopsin) Human - - - Neuropeptide SF pubchem
Peptide Agonist QRFP43 (43RFa) (Human), neuropeptide AF (Rat), neuropeptide AF (Human), RFRP-3 (Human), neuropeptide SF (Human), PrRP-31 (Human), neuropeptide AF (Mouse), neuropeptide FF (Human), RFRP-1 (Human) Peptide Kim J, Hong S, Lee H, Lee HS, Park C, Kim J, Im W, Choi HJ 10.1038/S44319-025-00428-2 2025-04-09
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 9JH3 - 2.9 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - CMF-019 pubchem gtoplig chembl_ligand
Small molecule Agonist (partial) apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide - - 2025-04-23
Gi/o αi1 Human Gi1 heterotrimer; Gβ1 has His-tag/3C site 61 β1 Human γ2 Human Cryo-EM 9JHJ - 3.2 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human BRIL - - C18 Ceramide pubchem
Small molecule Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide Lin H, Ma C, Cai K, Guo L, Wang X, Lv L, Zhang C, Lin J, Zhang D, Ye C, Wang T, Huang S, Han J, Zhang Z, Gao J, Zhang M, Pu Z, Li F, Guo Y, Zhou X, Qin C, Yi F, Yu X, Kong W, Jiang C, Sun JP 10.1126/SCIENCE.ADO4188 2025-03-19
Gi/o αi1 Human DN Gαi1: G203A/A326S 60 β1 Human γ2 Human Cryo-EM 9JIC - 3.4 HCAR3 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human - - - - None - 3-hydroxyoctanoic acid Small molecule Ye F, Pan X, Zhang Z, Xiang X, Li X, Zhang B, Ning P, Liu A, Wang Q, Gong K, Li J, Zhu L, Qian C, Chen G, Du Y 10.1016/J.CELREP.2024.114895 2025-12-17
Gi/o αi1 Human DN Gi1: G203A/A326S 61 β1 Human γ2 Human Cryo-EM 9JID - 2.8 HCAR3 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human - - - nicotinic acid pubchem gtoplig chembl_ligand drugbank drug_central drugbank drugbank
Small molecule Agonist 3-hydroxyoctanoic acid Small molecule Ye F, Pan X, Zhang Z, Xiang X, Li X, Zhang B, Ning P, Liu A, Wang Q, Gong K, Li J, Zhu L, Qian C, Chen G, Du Y 10.1016/J.CELREP.2024.114895 2025-12-17
Gi/o αi1 Human DNGai1: G203A/A326S 60 β1 Human γ2 Human Cryo-EM 9JKV - 3.3 HCAR3 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human - - - IBC 293 pubchem gtoplig chembl_ligand
Small molecule Agonist 3-hydroxyoctanoic acid Small molecule - - 2025-10-29
Gs αs Human DNGs: 8 muts to enhance stability 60 β1 Human γ2 Human Cryo-EM 9JKQ 9JKQ_refined 2.7 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - METHAMPHETAMINE chembl_ligand pubchem drugbank drug_central
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Lin Y, Wang J, Shi F, Yang L, Wu S, Qiao A, Ye S 10.1021/ACS.JMEDCHEM.4C01961 2024-10-16
Gi/o αi1 Human DN Gαi1 (DNGαi1): G203A/A326S mutations 60 β1 Human γ2 Human Cryo-EM 9JKS - 3.3 HCAR3 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human - - - compound 6o [PMID: 19524438] pubchem gtoplig chembl_ligand
Small molecule Agonist 3-hydroxyoctanoic acid Small molecule - - 2025-10-29
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 61 β1 Human γ2 Human Cryo-EM 9JKT - 3.1 HCAR3 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human - - - D-phenyllactic acid pubchem gtoplig drugbank pubchem
Small molecule Agonist 3-hydroxyoctanoic acid Small molecule Ye F, Zhang Z, Zhang B, Li X, Deng J, Miao Q, Ning P, Chi Y, Chen G, Wu Z, Wang Q, Xu L, Gong N, Cheng B, Ma Z, Qian C, Zhu L, Pan X, Du Y 10.1371/JOURNAL.PBIO.3003480 2025-10-29
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 61 β1 Human γ2 Human Cryo-EM 9JKX - 3.2 HCAR3 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human - - - Acifran pubchem
Small molecule Agonist 3-hydroxyoctanoic acid Small molecule Ye F, Zhang Z, Zhang B, Li X, Deng J, Miao Q, Ning P, Chi Y, Chen G, Wu Z, Wang Q, Xu L, Gong N, Cheng B, Ma Z, Qian C, Zhu L, Pan X, Du Y 10.1371/JOURNAL.PBIO.3003480 2025-10-29
Gi/o αi1 Human DN Gαi1: G203A/A326S 61 β1 Human γ2 Human Cryo-EM 9JKY - 2.7 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human - - - Acifran pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Ye F, Zhang Z, Zhang B, Li X, Deng J, Miao Q, Ning P, Chi Y, Chen G, Wu Z, Wang Q, Xu L, Gong N, Cheng B, Ma Z, Qian C, Zhu L, Pan X, Du Y 10.1371/JOURNAL.PBIO.3003480 2025-10-29
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 9JLC - 3.0 MAS MAS1 MAS1 Orphan A (Rhodopsin) Human - - - AVE 0991 pubchem gtoplig chembl_ligand
Small molecule Agonist - - - - 2025-09-24
Gi/o αi1 Human Gαi1: DN muts S47N/G203A/A326S/E245A 61 β1 Human γ2 Human Cryo-EM 8WSS 8WSS_refined 3.0 MCHR1 MCHR1 MCH1 Melanin-concentrating hormone A (Rhodopsin) Human BRIL - - melanin-concentrating hormone (Human) pubchem gtoplig uniprot uniprot uniprot
Peptide Agonist melanin-concentrating hormone (Human) Peptide He Q, Yuan Q, Shan H, Wu C, Gu Y, Wu K, Hu W, Zhang Y, He X, Xu HE, Zhao LH 10.1038/S41421-024-00679-8 2024-06-19
Gi/o αi1 Human Gi1 heterotrimer 63 β1 Human γ2 Human Cryo-EM 8WWK 8WWK_refined 2.6 MCHR1 MCHR1 MCH1 Melanin-concentrating hormone A (Rhodopsin) Human - - Fusion protein 1
Fusion protein 2 		melanin-concentrating hormone (Human) pubchem gtoplig uniprot uniprot uniprot
Peptide Agonist melanin-concentrating hormone (Human) Peptide Ye X, Liu G, Li X, He B, Tao Y, Guan J, Mu Y, Liu H, Gong W 10.1038/S41421-024-00754-0 2024-11-13
Gi/o αi1 Human Gi1 heterotrimer complex 63 β1 Human γ2 Human Cryo-EM 8WWL 8WWL_refined 2.8 MCHR1 MCHR1 MCH1 Melanin-concentrating hormone A (Rhodopsin) Human - - Fusion protein melanin-concentrating hormone (Human) pubchem gtoplig uniprot uniprot uniprot
Peptide Agonist melanin-concentrating hormone (Human) Peptide Ye X, Liu G, Li X, He B, Tao Y, Guan J, Mu Y, Liu H, Gong W 10.1038/S41421-024-00754-0 2024-11-13
Gs αs Human Wild-type Gs heterotrimer 55 β1 Human γ2 Human Cryo-EM 8X2K - 3.0 GPR3 GPR3 GPR3 Orphan A (Rhodopsin) Human BRIL - - N-oleoylethanolamide pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist sphingosine 1-phosphate Lipid Chen G, Staffen N, Wu Z, Xu X, Pan J, Inoue A, Shi T, Gmeiner P, Du Y, Xu J 10.1038/S41422-023-00919-8 2024-04-03
Gs αs Human MiniGαs-short, ΔAHD; Gβ1-SmBiT fusion 60 β1 Human γ2 Human Cryo-EM 8X7A 8X7A_refined 2.6 PI2R PTGIR IP Prostanoid A (Rhodopsin) Human BRIL Nanobody-35 LgBiT treprostinil pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist PGF2α, PGE1, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Wang JJ, Jin S, Zhang H, Xu Y, Hu W, Jiang Y, Chen C, Wang DW, Xu HE, Wu C 10.1126/SCIADV.ADK5184 2024-03-06
Gi/o αi1 Human Wild-type human Gi1 complex 62 β1 Rat γ2 Bovine Cryo-EM 8XBE 8XBE_refined 3.4 GPR34 GPR34 GPR34 Orphan A (Rhodopsin) Human - - - CHEMBL4782438 chembl_ligand pubchem
Small molecule Agonist lysophosphatidylserine Lipid Izume T, Kawahara R, Uwamizu A, Chen L, Yaginuma S, Omi J, Kawana H, Hou F, Sano FK, Tanaka T, Kobayashi K, Okamoto HH, Kise Y, Ohwada T, Aoki J, Shihoya W, Nureki O 10.1038/S41467-024-45046-Z 2024-05-15
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 66 β1 Human γ2 Human Cryo-EM 8XGM - 3.3 CML2 CMKLR2 chemerin 2 Chemerin receptor A (Rhodopsin) Human - - - Chemerin
Protein Agonist chemerin (Human) Peptide - - 2024-08-21
Gi/o αi1 Human DN Gαi1: S47N/G203A/A326S 63 β1 Human γ2 Human Cryo-EM 8XQE 8XQE_refined 3.5 APJ APLNR apelin Apelin A (Rhodopsin) Human BRIL - - apelin-13 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Yue Y, Liu L, Wu L, Xu C, Na M, Liu S, Liu Y, Li F, Liu J, Shi S, Lei H, Zhao M, Yang T, Ji W, Wang A, Hanson MA, Stevens RC, Liu J, Xu F 10.1038/S41467-024-55555-6 2025-01-22
Gi/o αi1 Human DN G protein: S47N/G203A/A326S mutations 63 β1 Human γ2 Human Cryo-EM 8XQF 8XQF_refined 3.1 APJ APLNR apelin Apelin A (Rhodopsin) Human BRIL - - apelin-13 (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Yue Y, Liu L, Wu L, Xu C, Na M, Liu S, Liu Y, Li F, Liu J, Shi S, Lei H, Zhao M, Yang T, Ji W, Wang A, Hanson MA, Stevens RC, Liu J, Xu F 10.1038/S41467-024-55555-6 2025-01-22
Gi/o αo Human MiniGαo GTPase domain (res 1-240) 58 β1 Human γ2 Human Cryo-EM 8XWV 8XWV_refined 3.1 CXCR2 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - - - CXCL1
Protein Agonist CXCL5 (Rat), CXCL5 (Mouse), CXCL1 (Rat), CXCL7 (Human), CXCL1 (Mouse), CXCL2 (Mouse), CXCL3 (Human), CXCL2 (Human), CXCL5 (Human), CXCL6 (Human), CXCL2 (Rat), CXCL3 (Rat), CXCL3 (Mouse), CXCL1 (Human), CXCL8 (Human) Peptide Saha S, Sano FK, Sharma S, Ganguly M, Mishra S, Dalal A, Akasaka H, Kobayashi TA, Zaidi N, Tiwari D, Roy N, Yadav MK, Banerjee N, Saha S, Mohapatra S, Itoh Y, Chevigne A, Banerjee R, Shihoya W, Nureki O, Shukla AK 10.1016/J.MOLCEL.2025.01.024 2025-01-22
Gi/o αo Human Mini-Gαo subunit (miniGaoA) 61 β1 Human γ2 Human Cryo-EM 8XX3 - 3.4 CXCR2 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - - - CXCL3
Protein Agonist CXCL5 (Rat), CXCL5 (Mouse), CXCL1 (Rat), CXCL7 (Human), CXCL1 (Mouse), CXCL2 (Mouse), CXCL3 (Human), CXCL2 (Human), CXCL5 (Human), CXCL6 (Human), CXCL2 (Rat), CXCL3 (Rat), CXCL3 (Mouse), CXCL1 (Human), CXCL8 (Human) Peptide Saha S, Sano FK, Sharma S, Ganguly M, Mishra S, Dalal A, Akasaka H, Kobayashi TA, Zaidi N, Tiwari D, Roy N, Yadav MK, Banerjee N, Saha S, Mohapatra S, Itoh Y, Chevigne A, Banerjee R, Shihoya W, Nureki O, Shukla AK 10.1016/J.MOLCEL.2025.01.024 2025-01-15
Gi/o αo Human MiniGαoA, truncated GTPase domain 61 β1 Human γ2 Human Cryo-EM 8XX6 8XX6_refined 3.0 CXCR2 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - - - CXCL8
Protein Agonist CXCL5 (Rat), CXCL5 (Mouse), CXCL1 (Rat), CXCL7 (Human), CXCL1 (Mouse), CXCL2 (Mouse), CXCL3 (Human), CXCL2 (Human), CXCL5 (Human), CXCL6 (Human), CXCL2 (Rat), CXCL3 (Rat), CXCL3 (Mouse), CXCL1 (Human), CXCL8 (Human) Peptide Saha S, Sano FK, Sharma S, Ganguly M, Mishra S, Dalal A, Akasaka H, Kobayashi TA, Zaidi N, Tiwari D, Roy N, Yadav MK, Banerjee N, Saha S, Mohapatra S, Itoh Y, Chevigne A, Banerjee R, Shihoya W, Nureki O, Shukla AK 10.1016/J.MOLCEL.2025.01.024 2025-01-15
Gi/o αo Human Mini-Gαo protein (miniGaoA) 61 β1 Human γ2 Human Cryo-EM 8XX7 8XX7_refined 3.3 CXCR2 CXCR2 CXCR2 Chemokine A (Rhodopsin) Human - - - CXCL5
Protein Agonist CXCL5 (Rat), CXCL5 (Mouse), CXCL1 (Rat), CXCL7 (Human), CXCL1 (Mouse), CXCL2 (Mouse), CXCL3 (Human), CXCL2 (Human), CXCL5 (Human), CXCL6 (Human), CXCL2 (Rat), CXCL3 (Rat), CXCL3 (Mouse), CXCL1 (Human), CXCL8 (Human) Peptide Saha S, Sano FK, Sharma S, Ganguly M, Mishra S, Dalal A, Akasaka H, Kobayashi TA, Zaidi N, Tiwari D, Roy N, Yadav MK, Banerjee N, Saha S, Mohapatra S, Itoh Y, Chevigne A, Banerjee R, Shihoya W, Nureki O, Shukla AK 10.1016/J.MOLCEL.2025.01.024 2025-01-15
Gi/o αi1 Human Gαi1: 4 DN mutations (S47N/G203A/+2 more) 64 β1 Human γ2 Human Cryo-EM 8XXV - 2.3 PD2R2 PTGDR2 DP2 Prostanoid A (Rhodopsin) Human BRIL - LgBiT indomethacin pubchem gtoplig chembl_ligand drugbank drug_central
Phosphatidylinositol (16:0/18:1)
Small molecule
Small molecule 		Agonist
PAM 		PGF2α, Δ12-PGJ2, PGE2, PGD2, PGI2, PGD3, thromboxane A2 Small molecule - - 2024-12-04
Gi/o αo Human MiniGαo GTPase domain only 61 β1 Human γ2 Human Cryo-EM 8XXZ 8XXZ_refined 3.3 CXCR3 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human - - - - None - CXCL9 (Mouse), CCL20 (Human), CCL19 (Human), CXCL10 (Human), CXCL10 (Mouse), CCL11 (Human), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CXCL12α (Human), CXCL9 (Human), CCL5 (Human), CXCL11 (Human) Peptide Saha S, Sano FK, Sharma S, Ganguly M, Dalal A, Mishra S, Tiwari D, Akasaka H, Kobayashi TA, Roy N, Zaidi N, Itoh Y, Leurs R, Banerjee R, Shihoya W, Nureki O, Shukla AK 10.1038/S41467-025-58264-W 2025-02-26
Gi/o αo Human MiniGαo: GTPase domain, AHD→linker 61 β1 Human γ2 Human Cryo-EM 8XYK - 3.0 CXCR3 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human - - - CHEMBL2181467 chembl_ligand pubchem chembl_ligand pubchem
Small molecule Agonist CXCL9 (Mouse), CCL20 (Human), CCL19 (Human), CXCL10 (Human), CXCL10 (Mouse), CCL11 (Human), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CXCL12α (Human), CXCL9 (Human), CCL5 (Human), CXCL11 (Human) Peptide - - 2025-02-26
Gi/o αi1 Human DNGi (Gαi1) muts reduce nucl. affinity 62 β1 Human γ2 Human Cryo-EM 8XZI 8XZI_refined 2.7 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - CMF-019 pubchem gtoplig chembl_ligand
Small molecule Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide - - 2024-03-20
Gi/o αi1 Human DN Gαi1 for stabilization 62 β1 Human γ2 Human Cryo-EM 8XZJ 8XZJ_refined 3.0 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - WN353
Peptide Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide Wang WW, Ji SY, Zhang W, Zhang J, Cai C, Hu R, Zang SK, Miao L, Xu H, Chen LN, Yang Z, Guo J, Qin J, Shen DD, Liang P, Zhang Y, Zhang Y 10.1016/J.CELL.2024.02.004 2024-03-20
Gi/o αi1 Human DN Gαi1 (5 muts); Gβ1 C-term HiBiT tag 58 β1 Human γ2 Bovine Cryo-EM 8Y01 8Y01_refined 2.5 OPSG OPN1MW OPN1MW Opsin (sight) A (Rhodopsin) Human BRIL - LgBiT subunit
HiBiT tag 		all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - - - 2025-02-12
Gi/o αi1 Human DN Gαi1 mutant: S47C/G202T +3 more mutations 61 β1 Human γ2 Bovine Cryo-EM 8Y02 - 2.6 OPSB OPN1SW OPN1SW Opsin (sight) A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		all-trans-retinal pubchem gtoplig chembl_ligand
Small molecule Agonist - - Peng Q, Li J, Jiang H, Cheng X, Nag P, Kleinau G, Lamb TD, Busche L, Lu Q, Zhou S, Liu Y, Zhang Y, Lv S, Wan S, Yang T, Chen Y, Zhang W, Nan W, Fu Y, Che T, Li Y, Liao H, Duan J, Schapiro I, Scheerer P, Zhang J 10.1126/SCIENCE.ADZ8141 2025-06-11
Gi/o αo Human MiniGαo: GTPase domain only 61 β1 Human γ2 Human Cryo-EM 8Y0N 8Y0N_refined 3.1 CXCR3 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human - - - CHEMBL2221034 chembl_ligand pubchem
Small molecule Agonist CXCL9 (Mouse), CCL20 (Human), CCL19 (Human), CXCL10 (Human), CXCL10 (Mouse), CCL11 (Human), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CXCL12α (Human), CXCL9 (Human), CCL5 (Human), CXCL11 (Human) Peptide - - 2025-02-26
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 62 β1 Rat γ2 Bovine Cryo-EM 8Y71 - 3.0 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - - LgBiT SNC80 pubchem
BMS-986187 pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		[Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-01-07
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 64 β1 Rat γ2 Bovine Cryo-EM 8Y72 - 2.7 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - DAMGO pubchem gtoplig chembl_ligand pubchem
BMS-986122 pubchem
Peptide
Small molecule 		Agonist
PAM 		[Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Wang Y, Luo P, Xu H, Zhan L, Sakamoto K, Li M, Wang J, Huang XP, Zhou J, Liu T, Suo Y, Fan W, He X, Xu Y, Cai Y, Wang C, Zhao Y, Dai A, Lai Y, Yuan Q, Hu W, Wu K, Yang D, Cheng X, Lu X, Krumm B, Kenakin T, Zhang J, Roth BL, Gao Z, Xu HE, Zhuang Y 10.1126/SCIADV.AEA9832 2025-08-06
Gi/o αi1 Human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 8YIC 8YIC_refined 3.5 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human Endolysin - - SAR247799 pubchem gtoplig chembl_ligand
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid - - 2024-12-11
Gi/o αi1 Human Engineered Gi protein for stabilization 60 β1 Rat γ2 Bovine Cryo-EM 8YKV - 2.5 SUCR1 SUCNR1 succinate Succinate A (Rhodopsin) Human - - - compound 31 [PMID: 29968758] pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist succinic acid Small molecule - - 2024-05-29
Gi/o αi1 Human Engineered Gi protein with DN mutations 60 β1 Rat γ2 Bovine Cryo-EM 8YKW 8YKW_refined 2.8 SUCR1 SUCNR1 succinate Succinate A (Rhodopsin) Human - - - succinic acid pubchem gtoplig chembl_ligand drugbank drug_central pubchem drugbank drugbank
Small molecule Agonist succinic acid Small molecule Li C, Liu H, Li J, He X, Zhu H, Fu W, Xu HE 10.1038/S41422-024-00984-7 2024-05-29
Gi/o αi1 Human Engineered Gi protein 60 β1 Rat γ2 Bovine Cryo-EM 8YKX 8YKX_refined 2.7 SUCR1 SUCNR1 succinate Succinate A (Rhodopsin) Human - - - maleic acid pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist succinic acid Small molecule Li C, Liu H, Li J, He X, Zhu H, Fu W, Xu HE 10.1038/S41422-024-00984-7 2024-05-29
Gi/o αo Human MiniGo: stabilizing mutations + truncations 61 β1 Human γ2 Human Cryo-EM 8YN8 - 2.8 HRH3 HRH3 H3 Histamine A (Rhodopsin) Human - - - proxyfan pubchem gtoplig chembl_ligand
Small molecule Agonist histamine Small molecule - - 2024-10-16
Gi/o αi1 Human DN Gi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8YN9 - 2.3 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human - - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule Zhang X, Liu G, Zhong YN, Zhang R, Yang CC, Niu C, Pu X, Sun J, Zhang T, Yang L, Zhang C, Li X, Shen X, Xiao P, Sun JP, Gong W 10.1038/S41467-024-52585-Y 2024-10-09
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 8YNA - 2.6 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human - - - immepip pubchem gtoplig chembl_ligand
Small molecule Agonist CCL16 (Human), histamine Small molecule - - 2024-10-09
Gs αs Human Gαs (short isoform) subunit 57 β1 Human γ2 Human Cryo-EM 8YW3 8YW3_refined 2.7 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - retatrutide pubchem gtoplig
Protein Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Li W, Zhou Q, Cong Z, Yuan Q, Li W, Zhao F, Xu HE, Zhao LH, Yang D, Wang MW 10.1038/S41421-024-00700-0 2024-09-18
Gs αs Human Engineered mini-Gs protein 60 β1 Human γ2 Human Cryo-EM 8YW4 8YW4_refined 3.3 GIPR GIPR GIP Glucagon B1 (Secretin) Human - Nanobody-35 - retatrutide pubchem gtoplig
Protein Agonist gastric inhibitory polypeptide (Mouse), gastric inhibitory polypeptide (Human) Peptide Li W, Zhou Q, Cong Z, Yuan Q, Li W, Zhao F, Xu HE, Zhao LH, Yang D, Wang MW 10.1038/S41421-024-00700-0 2024-09-18
Gs αs Human Short isoform of Gs alpha subunit 60 β1 Human γ2 Human Cryo-EM 8Z3Q - 2.8 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - - - - None - - - - - 2025-04-23
Gs αs Human modGαs: Gi1 N-term added for scFv16 binding 60 β1 Human γ2 Human Cryo-EM 8Z3Y - 3.2 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human BRIL - - - None - - - Guo L, Zhu K, Zhong YN, Gao M, Liu J, Qi Z, Liu Z, Rong N, Zhang M, Li D, Zhang Q, Yang G, Zhang X, Zhang M, Ding N, Ping YQ, Yang Z, Xiao P, Xia M, Yu X, Gaole A, Sun JP, Yang F 10.1016/J.MOLCEL.2025.03.018 2025-06-04
Gs αs Human Gs heterotrimer 60 β1 Human γ2 Human Cryo-EM 8Z5H - 3.3 GPR68 GPR68 GPR68 Proton A (Rhodopsin) Human - - - - None - - - - - 2025-04-23
Gs αs Human Gs α subunit, short isoform 60 β1 Human γ2 Human Cryo-EM 8Z65 - 3.0 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - - - - None - - - - - 2025-04-23
Gi/o αi1 Human Gi1 heterotrimer complex 32 β1 Human γ2 Human Cryo-EM 8ZBI - 2.8 SSR3 SSTR3 SST3 Somatostatin A (Rhodopsin) Human BRIL - - SOMATOSTATIN chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide - - 2025-04-30
Gi/o αi1 Human Wild-type Gi1 heterotrimer 47 β1 Human γ2 Human Cryo-EM 8ZBJ - 2.9 SSR5 SSTR5 SST5 Somatostatin A (Rhodopsin) Human BRIL - - SOMATOSTATIN chembl_ligand pubchem drugbank drug_central pubchem
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide - - 2025-04-30
Gi/o αi2 Human DN Gαi2: S47N/G203A/A326S/E245A; Gβ1-HiBiT 61 β1 Human γ2 Human Cryo-EM 8ZBW - 2.6 FPR2 FPR2 FPR2/ALX Formylpeptide A (Rhodopsin) Human - - - Quin-C1 pubchem
Small molecule Agonist LXA4, 15-deoxy-LXA4, LL-37 (Human), annexin I-(2-26) (Human), LTD4, resolvin D1, PrP106-126 (Human), annexin I (Rat), annexin I (Mouse), LTC4, aspirin triggered lipoxin A4, aspirin-triggered resolvin D1, serum amyloid A (Human), humanin (Human), annexin I (Human) Peptide - - 2025-09-10
Gs αs Human DN human Gs (DNGas): 8 stabilizing mutations 57 β1 Human γ2 Human Cryo-EM 8ZCE - 3.1 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 Endoglucanase H - None - - - Yue X, Peng L, Liu S, Zhang B, Zhang X, Chang H, Pei Y, Li X, Liu J, Shui W, Wu L, Xu H, Liu ZJ, Hua T 10.1038/S41422-025-01092-W 2025-04-23
Gs αs Human DNGs: 8 muts incl S54N/G226A/E268A 57 β1 Human γ2 Human Cryo-EM 8ZCF - 2.9 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 Endoglucanase H - None - - - Yue X, Peng L, Liu S, Zhang B, Zhang X, Chang H, Pei Y, Li X, Liu J, Shui W, Wu L, Xu H, Liu ZJ, Hua T 10.1038/S41422-025-01092-W 2025-04-23
Gi/o αi1 Human DN Gαi1: G203A/A326S; Gβ1 C-term HiBit 63 β1 Rat γ2 Bovine Cryo-EM 8ZCJ 8ZCJ_refined 3.1 SSR5 SSTR5 SST5 Somatostatin A (Rhodopsin) Human - - LgBiT
beta2AR-N-terminal-segment
HiBiT 		pasireotide pubchem gtoplig drugbank chembl_ligand drug_central
Peptide Agonist cortistatin-14 (Mouse), SRIF-14 (Human), SRIF-28 (Human), CST-17 (Human) Peptide Li YG, Meng XY, Yang X, Ling SL, Shi P, Tian CL, Yang F 10.1038/S41401-024-01314-8 2024-07-10
Gs αs Human Engineered Gαs (modGas) w/ stabilizing muts 60 β1 Human γ2 Human Cryo-EM 8ZF6 - 3.0 GPR4 gpr4 GPR4 Proton A (Rhodopsin) Western clawed frog - - - - None - - - Wen X, Shang P, Chen H, Guo L, Rong N, Jiang X, Li X, Liu J, Yang G, Zhang J, Zhu K, Meng Q, He X, Wang Z, Liu Z, Cheng H, Zheng Y, Zhang B, Pang J, Liu Z, Xiao P, Chen Y, Liu L, Luo F, Yu X, Yi F, Zhang P, Yang F, Deng C, Sun JP 10.1016/J.CELL.2024.12.001 2025-02-26
Gs αs Human mGs: Gs AHD replaced with Gi1 AHD 60 β1 Human γ2 Human Cryo-EM 8ZF9 - 2.6 GPR4 Gpr4 GPR4 Proton A (Rhodopsin) Mouse - Nanobody-35 - - None - - - Wen X, Shang P, Chen H, Guo L, Rong N, Jiang X, Li X, Liu J, Yang G, Zhang J, Zhu K, Meng Q, He X, Wang Z, Liu Z, Cheng H, Zheng Y, Zhang B, Pang J, Liu Z, Xiao P, Chen Y, Liu L, Luo F, Yu X, Yi F, Zhang P, Yang F, Deng C, Sun JP 10.1016/J.CELL.2024.12.001 2025-02-26
Gs αs Human modGαs chimera, engineered to stabilize complex 60 β1 Human γ2 Human Cryo-EM 8ZFC - 2.7 GPR4 Gpr4 GPR4 Proton A (Rhodopsin) Mouse - - - - None - - - Wen X, Shang P, Chen H, Guo L, Rong N, Jiang X, Li X, Liu J, Yang G, Zhang J, Zhu K, Meng Q, He X, Wang Z, Liu Z, Cheng H, Zheng Y, Zhang B, Pang J, Liu Z, Xiao P, Chen Y, Liu L, Luo F, Yu X, Yi F, Zhang P, Yang F, Deng C, Sun JP 10.1016/J.CELL.2024.12.001 2025-02-26
Gs αs Human Mini-Gs (mini-GαsIN): αN from Gαi, scFv16 60 β1 Human γ2 Human Cryo-EM 8ZFZ - 3.3 GPR4 gpr4 GPR4 Proton A (Rhodopsin) Zebrafish BRIL - LgBiT
HiBiT 		- None - - - Ma Y, Wang Y, Tang M, Weng Y, Chen Y, Xu Y, An S, Wu Y, Zhao S, Xu H, Li D, Liu M, Lu W, Ru H, Song G 10.1038/S41467-025-55901-2 2025-01-22
Gi/o αi1 Human DN Gαi1: G203A/A326S mutations 63 β1 Human γ2 Human Cryo-EM 8ZJG - 3.2 CML1 CMKLR1 chemerin Chemerin receptor A (Rhodopsin) Human - - - Chemerin
Protein Agonist 18R-HEPE, EPA, resolvin E1, chemerin (Human) Peptide Liu A, Liu Y, Wang J, Ye RD 10.1038/S42003-024-07228-9 2025-01-22
Gi/o αi1 Human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 8ZQE 8ZQE_refined 2.9 GPR15 GPR15 GPR15 Orphan A (Rhodopsin) Human BRIL - Maltose-binding protein (MBP) GPR15LC11
Peptide Agonist - - Zhang Z, Zheng Y, Xu L, Yue Y, Xu K, Li F, Xu F 10.1038/S41421-024-00698-5 2024-07-10
Gs αs Human Mini-Gs: Gi2/Gs chimera (dual accessions) 58 β1 Human γ2 Human Cryo-EM 8ZSP - 3.1 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - (+)-LSD pubchem gtoplig pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule Jiang K, Zheng Y, Zeng L, Wang L, Li F, Pu J, Lu Y, Zhao S, Xu F 10.1016/J.CELREP.2024.114505 2024-07-24
Gs αs Human Mini-Gs/Gi2 chimera (dual UniProt IDs) 58 β1 Human γ2 Human Cryo-EM 8ZSS - 3.1 TAAR1 TAAR1 TA1 Trace amine A (Rhodopsin) Human BRIL Nanobody-35 - RO5256390 pubchem gtoplig chembl_ligand
Small molecule Agonist (partial) 3-iodothyronamine, β-phenylethylamine, tyramine, octopamine, dopamine Small molecule - - 2024-07-24
Gs αs Human Mini-Gs/Gi2 chimera (metadata IDs) 58 β1 Human γ2 Human Cryo-EM 8ZSV - 3.0 TAAR1 Taar1 TA1 Trace amine A (Rhodopsin) Mouse BRIL Nanobody-35 - RO5256390 pubchem gtoplig chembl_ligand
Small molecule Agonist (partial) 3-iodothyronamine, β-phenylethylamine, tyramine Small molecule - - 2024-07-24
Gs αs Human DN Gs: 8 muts; NanoBiT HiBiT-Gβ fusion 60 β1 Human γ2 Human Cryo-EM 8ZVZ - 2.4 PD2R PTGDR DP1 Prostanoid A (Rhodopsin) Human BRIL Nanobody-35 - CHEMBL1591294 chembl_ligand pubchem pubchem
Small molecule Agonist PGF2α, PGE1, Δ12-PGJ2, PGE2, PGD2, PGI2, thromboxane A2 Small molecule - - 2025-05-28
Gs αs Human DN Gs: 8 muts S54N/G226A/E268A...I285T 60 β1 Human γ2 Human Cryo-EM 8ZW0 - 2.7 PD2R PTGDR DP1 Prostanoid A (Rhodopsin) Human BRIL Nanobody-35 - PGD2 pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist PGF2α, PGE1, Δ12-PGJ2, PGE2, PGD2, PGI2, thromboxane A2 Small molecule Xu J, Wu Y, Xu Y, Li Y, He X, Zhang H, Wang JJ, Hou J, Li J, Hu W, Wu K, Yuan Q, Wu C, Xu HE 10.1073/PNAS.2501902122 2025-05-28
Gi/o αi1 Human - 63 β1 Rat γ Western European hedgehog Cryo-EM 8ZWG - 2.9 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - Beta-2 adrenergic receptor fusion segment JR14a pubchem gtoplig chembl_ligand
Small molecule Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide - - 2025-05-14
G12/13 α13 Human MiniGα13 construct 56 β1 Human γ2 Human Cryo-EM 8ZX4 - 2.9 GPR55 GPR55 GPR55 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - - LgBiT
HiBiT 		L-alpha-lysophosphatidylinositol (16:0)
Small molecule Agonist N-palmitoylethanolamine, lysophosphatidylinositol, anandamide, 2-arachidonoylglycerolphosphoinositol, 2-arachidonoylglycerol Small molecule - - 2024-11-13
Gi/o αi1 Human Standard Gi1 heterotrimer (Gαi1/Gβ1/Gγ2) 62 β1 Human γ2 Human Cryo-EM 9B54 9B54_refined 2.9 CNR1 CNR1 CB1 Cannabinoid A (Rhodopsin) Human - - - VIP36 pubchem gtoplig
Small molecule Agonist anandamide, 2-arachidonoylglycerol Small molecule - - 2025-03-05
Gs αs Human MiniGs399 (no Gγ subunit present) 61 β1 Human - - Cryo-EM 9BHL - 2.8 GPR65 GPR65 GPR65 Proton A (Rhodopsin) Human - Nanobody-35 - - None - - - Howard MK, Hoppe N, Huang XP, Mitrovic D, Billesbolle CB, Macdonald CB, Mehrotra E, Rockefeller Grimes P, Trinidad DD, Delemotte L, English JG, Coyote-Maestas W, Manglik A 10.1016/J.CELL.2024.11.036 2025-01-22
Gs αs Human MiniGs construct 53 β1 Human - - Cryo-EM 9BHM - 2.9 GPR68 GPR68 GPR68 Proton A (Rhodopsin) Human - Nanobody-35 - - None - - - Howard MK, Hoppe N, Huang XP, Mitrovic D, Billesbolle CB, Macdonald CB, Mehrotra E, Rockefeller Grimes P, Trinidad DD, Delemotte L, English JG, Coyote-Maestas W, Manglik A 10.1016/J.CELL.2024.11.036 2025-01-22
Gs αs Human DNGs: dominant-negative Gs protein 57 β1 Human γ2 Human Cryo-EM 9BLB - 3.2 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Cagrilintide backbone (non-acylated)
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Johnson RM, Keov P, Mariam Z, Deganutti G, Christopoulos G, Hick CA, Reedtz-Runge S, Glendorf T, Ballarin-Gonzalez B, Raun K, Bayly-Jones C, Wootten D, Sexton PM 10.1038/S41467-025-58680-Y 2025-04-16
Gs αs Human DN Gs protein 58 β1 Human γ2 Human Cryo-EM 9BLC - 3.3 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35 - Cagrilintide backbone (non-acylated)
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Johnson RM, Keov P, Mariam Z, Deganutti G, Christopoulos G, Hick CA, Reedtz-Runge S, Glendorf T, Ballarin-Gonzalez B, Raun K, Bayly-Jones C, Wootten D, Sexton PM 10.1038/S41467-025-58680-Y 2025-04-16
Gs αs Human DNGs: dominant-negative Gs protein 58 β1 Human γ2 Human Cryo-EM 9BLW - 3.2 CALCR CALCR CT Calcitonin B1 (Secretin) Human - Nanobody-35
RAMP1 		- Cagrilintide backbone (non-acylated)
Peptide Agonist adrenomedullin 2/intermedin (Human), β-CGRP (Mouse), amylin (Mouse), α-CGRP (Human), calcitonin (Human), β-CGRP (Human), β-CGRP (Rat), α-CGRP (Mouse), calcitonin (Mouse), adrenomedullin (Human), amylin (Human) Peptide Cao J, Belousoff MJ, Johnson RM, Keov P, Mariam Z, Deganutti G, Christopoulos G, Hick CA, Reedtz-Runge S, Glendorf T, Ballarin-Gonzalez B, Raun K, Bayly-Jones C, Wootten D, Sexton PM 10.1038/S41467-025-58680-Y 2025-04-16
Gs αs Human Mini-Gs (G112): Gi1-derived stabilizing mods 59 β1 Human γ2 Bovine Cryo-EM 9K3F - 2.8 MC3R MC3R MC3 Melanocortin A (Rhodopsin) Human - - LgBiT
HiBiT 		- None - ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Feng W, Zhou Q, Zheng C, Yang D, Wang MW 10.1016/J.STR.2025.03.004 2025-08-06
Gs αs Human G112: mini-Gs w/ Gs+Gi1 segments 59 β1 Human γ2 Bovine Cryo-EM 9K3H - 2.9 MC5R MC5R MC5 Melanocortin A (Rhodopsin) Human - - LgBiT
HiBiT 		- None - ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Feng W, Zhou Q, Zheng C, Yang D, Wang MW 10.1016/J.STR.2025.03.004 2025-08-06
Gs αs Human Gs heterotrimer: Gs/Gi1 chimera (G112) 59 β1 Human γ2 Bovine Cryo-EM 9K3K - 3.1 MC4R MC4R MC4 Melanocortin A (Rhodopsin) Human - Nanobody-35 LgBiT
HiBiT 		- None - ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat), agouti-related protein (Human) Peptide Feng W, Zhou Q, Zheng C, Yang D, Wang MW 10.1016/J.STR.2025.03.004 2025-08-06
Gi/o αi2 Human Gα mutant: S47N/G203A/A327S 64 β1 Human γ2 Human Cryo-EM 9K6L - 2.8 T2R16 TAS2R16 TAS2R16 Taste 2 T2 (Taste 2) Human - - exo-alpha-sialidase NanA
LgBiT 		salicin pubchem gtoplig
Small molecule Agonist - - Wang X, Zhou C, Ao W, Wu L, Wu Y, Xu W, Liu S, Tan Q, Wang L, Zhao F, Liu J, Pei Y, Zhao S, Hua T 10.1016/J.CELREP.2025.115604 2025-04-02
Gi/o αi2 Human DN Gαi2: S47N/G204A/E246A/A327S 62 β1 Human γ2 Human Cryo-EM 9KFI - 2.9 RL3R1 RXFP3 RXFP3 Relaxin family peptide A (Rhodopsin) Human BRIL - LgBiT Relaxin-3 (chain A)
Relaxin-3 (chain B)
Peptide
Peptide 		Agonist INSL5 (Human), relaxin-3 (B chain) (Human), relaxin-3 (Human), relaxin (Human) Peptide Chen Y, Zhou Q, Yan S, Yan J, Yang D, Chen J, Wang MW 10.1038/S42003-025-08220-7 2025-08-13
Gi/o αi2 Human DN human Gαi2 (DNGi2): 4 point mutations 63 β1 Human γ2 Human Cryo-EM 9KFJ - 3.1 RL3R1 RXFP3 RXFP3 Relaxin family peptide A (Rhodopsin) Human BRIL - LgBiT CHEMBL4522365 chembl_ligand pubchem
Small molecule Agonist INSL5 (Human), relaxin-3 (B chain) (Human), relaxin-3 (Human), relaxin (Human) Peptide Chen Y, Zhou Q, Yan S, Yan J, Yang D, Chen J, Wang MW 10.1038/S42003-025-08220-7 2025-08-13
Gi/o αi1 Human Gαi1 heterotrimer 61 β1 Human - - Cryo-EM 9KO2 - 3.0 CCR7 CCR7 CCR7 Chemokine A (Rhodopsin) Human - - - CCL19
Protein Agonist CCL21 (Human), CCL19 (Human) Peptide - - 2025-11-26
Gi/o αi1 Human Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 9KO4 - 3.3 CCR7 CCR7 CCR7 Chemokine A (Rhodopsin) Human - - - CCL21
Protein Agonist CCL21 (Human), CCL19 (Human) Peptide - - 2025-11-26
Gi/o αo Human MiniGαo, N-term scFv16 binding sequence 59 β1 Human γ2 Human Cryo-EM 9KUG - 3.1 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - N-terminal M4-fusion tag EP67
Peptide Agonist C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide Dalal A, Yadav MK, Ganguly M, Mishra S, Yadav R, Sinha S, Roy N, Tiwari D, Mukherjee D, Reyaz A, Dsouza CA, Nigam A, Banerjee N, Li XX, Clark RJ, Woodruff TM, Banerjee R, Gati C, Shukla AK 10.1073/PNAS.2614459123 2025-11-26
Gi/o αo Human Mini-Gαo: N-term ScFv16 binding sequence 58 β1 Human γ2 Human Cryo-EM 9KUT - 3.3 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - Muscarinic acetylcholine receptor M4 N-terminal fragment JR14a pubchem gtoplig chembl_ligand
Small molecule Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide - - 2025-11-26
Gi/o αo Human MiniGαo1 with N-term scFv16 sequence 59 β1 Human γ2 Human Cryo-EM 9KV6 - 2.9 C3AR C3ar1 C3a Complement peptide A (Rhodopsin) Mouse - - M4 receptor N-terminal fragment TLQP-21 (Human) pubchem gtoplig uniprot
Peptide Agonist - - Mishra S, Yadav MK, Dalal A, Ganguly M, Yadav R, Sawada K, Tiwari D, Roy N, Banerjee N, Fung JN, Marallag J, Cui CS, Li XX, Lee JD, Dsouza CA, Saha S, Sarma P, Rawat G, Zhu H, Khant HA, Clark RJ, Sano FK, Banerjee R, Woodruff TM, Nureki O, Gati C, Shukla AK 10.1101/2025.05.26.656101 2025-11-26
Gi/o αo Human Mini-Gαo (miniGao): N-term ScFv16 sequence 59 β1 Human γ2 Human Cryo-EM 9KV8 - 3.2 C3AR C3ar1 C3a Complement peptide A (Rhodopsin) Mouse - - - TLQP-21 (Human) pubchem gtoplig uniprot
Peptide Agonist - - Mishra S, Yadav MK, Dalal A, Ganguly M, Yadav R, Sawada K, Tiwari D, Roy N, Banerjee N, Fung JN, Marallag J, Cui CS, Li XX, Lee JD, Dsouza CA, Saha S, Sarma P, Rawat G, Zhu H, Khant HA, Clark RJ, Sano FK, Banerjee R, Woodruff TM, Nureki O, Gati C, Shukla AK 10.1101/2025.05.26.656101 2025-11-26
Gi/o αi1 Human DN human Gαi1: S47N/G203A/A326S/E245A 63 β1 Human γ2 Human Cryo-EM 9KVG - 2.6 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - 5-MeO-DMT pubchem gtoplig chembl_ligand drugbank
PtdIns4P pubchem
Small molecule
Small molecule 		Agonist
PAM 		5-hydroxytryptamine Small molecule Li SJ, Yuan QN, Wu WY, Chen ZH, Chen D, Shan H, Chu QY, Hu W, Wu K, Liu T, Zhu YY, Hou L, Zhou J, Duan J, Duan JA, Xu HE, Ma HY 10.34133/RESEARCH.0987 2025-12-03
Gi/o αi1 Human DN human Gαi1 variant: S47N/G203A/A326S/E245A 63 β1 Human γ2 Human Cryo-EM 9KVH - 2.6 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - Cinobufotenine
PtdIns4P pubchem
Small molecule
Small molecule 		Agonist
PAM 		5-hydroxytryptamine Small molecule - - 2025-12-03
Gi/o αi1 Human DN human Gαi1 variant: S47N/G203A/A326S/E245A 63 β1 Human γ2 Human Cryo-EM 9KVI - 2.5 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - bufotenine pubchem gtoplig chembl_ligand drugbank
PtdIns4P pubchem
Small molecule
Small molecule 		Agonist
PAM 		5-hydroxytryptamine Small molecule - - 2025-12-03
Gi/o αo Human MiniGαo, N-term scFv16 binding sequence 59 β1 Human γ2 Human Cryo-EM 9KX6 - 3.1 C5AR1 C5ar1 C5a1 Complement peptide A (Rhodopsin) Mouse - - M4 receptor N-terminal region (residues 2-23) C5a des-Arg (Human) gtoplig
Peptide Agonist - - Mishra S, Yadav MK, Dalal A, Ganguly M, Yadav R, Sawada K, Tiwari D, Roy N, Banerjee N, Fung JN, Marallag J, Cui CS, Li XX, Lee JD, Dsouza CA, Saha S, Sarma P, Rawat G, Zhu H, Khant HA, Clark RJ, Sano FK, Banerjee R, Woodruff TM, Nureki O, Gati C, Shukla AK 10.1101/2025.05.26.656101 2025-11-26
Gi/o αo Human MiniGαo with N-term scFv16 site 58 β1 Human γ2 Human Cryo-EM 9KXS - 3.3 C5AR1 C5ar1 C5a1 Complement peptide A (Rhodopsin) Mouse - - Muscarinic acetylcholine receptor M4 (residues 2-23) EP67
Peptide Agonist - - Dalal A, Yadav MK, Ganguly M, Mishra S, Yadav R, Sinha S, Roy N, Tiwari D, Mukherjee D, Reyaz A, Dsouza CA, Nigam A, Banerjee N, Li XX, Clark RJ, Woodruff TM, Banerjee R, Gati C, Shukla AK 10.1073/PNAS.2614459123 2025-11-26
Gi/o αo Human MiniGαo with N-term scFv16 sequence 59 β1 Human γ2 Human Cryo-EM 9KZ2 - 3.4 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - M4 receptor N-terminal tag EP67
Peptide Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide Dalal A, Yadav MK, Ganguly M, Mishra S, Yadav R, Sinha S, Roy N, Tiwari D, Mukherjee D, Reyaz A, Dsouza CA, Nigam A, Banerjee N, Li XX, Clark RJ, Woodruff TM, Banerjee R, Gati C, Shukla AK 10.1073/PNAS.2614459123 2025-11-26
Gi/o αo Human MiniGαo with N-term scFv16 sequence 59 β1 Human γ2 Human Cryo-EM 9KZ8 - 3.3 C3AR C3ar1 C3a Complement peptide A (Rhodopsin) Mouse - - Muscarinic acetylcholine receptor M4 (N-terminal tag) EP67
Peptide Agonist - - Dalal A, Yadav MK, Ganguly M, Mishra S, Yadav R, Sinha S, Roy N, Tiwari D, Mukherjee D, Reyaz A, Dsouza CA, Nigam A, Banerjee N, Li XX, Clark RJ, Woodruff TM, Banerjee R, Gati C, Shukla AK 10.1073/PNAS.2614459123 2025-11-26
Gi/o αi1 Human DN Gαi1: G203A/A326S 64 β1 Rat γ2 Bovine Cryo-EM 9L60 - 2.9 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - Dynorphin A13 pubchem
MPAM-15 pubchem
Small molecule
Small molecule 		Agonist
PAM 		[Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2025-12-31
Gs αs Human Cross-species Gs heterotrimer, engineered α 56 β1 Rat γ2 Bovine Cryo-EM 9L79 - 3.0 GP119 GPR119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - AR231453 pubchem gtoplig chembl_ligand
Small molecule Agonist SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide Small molecule - - 2025-12-31
Gs αs Human MiniGs (labeled miniGsiN, confirmed Gs tail) 57 β1 Rat γ2 Bovine Cryo-EM 9L80 - 3.3 GP119 GPR119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - ATAZANAVIR chembl_ligand pubchem drugbank
Small molecule Ago-PAM SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide Small molecule He G, Sun Q, Xu X, Kong F, Zhang S, Ye K, Sun X, Lin B, Chen X, Yan C, Liu X 10.1016/J.CELL.2025.12.023 2025-12-31
Gs αs Human modGs: mini-Gs399 based, Gγ not modeled 53 β1 Human - - Cryo-EM 9LKB - 3.7 A2RT31 Or5v1 OR5V1 Olfactory family 5 O2 (Olfactory/extra-nasal 2) Mouse BRIL - MBP PL45 pubchem
Small molecule Agonist - - - - 2026-01-21
Gi/o αi1 Human Gαi1 w/ 4 DN muts: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 9LL7 - 2.8 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - LgBiT (R)-DOI pubchem gtoplig chembl_ligand
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule - - 2026-01-14
Gi/o αi1 Human Gαi1: 4 DN muts (S47N/G203A/E245A/A326S) 64 β1 Human γ2 Human Cryo-EM 9LL8 - 2.6 5HT2A HTR2A 5-HT2A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - LgBiT (NanoBiT) psilocin pubchem gtoplig chembl_ligand
Small molecule Agonist tryptamine, 5-hydroxytryptamine Small molecule Xu Z, Wang H, Yu J, Deng Y, Tian X, Ni R, Xia F, Yang L, Xu C, Zhang L, Luo R, Chen P, Zhang X, Liu Y, Hou J, Zhang M, Chen S, Su L, Sun H, He Y, Chen D, Chen X, Miao Z, Xie J, Liu X, Zhao J, Ke B, Tian X, Zeng L, Zhang L, Tang X, Yang S, Liu J, Wang X, Yan W, Shao Z 10.1038/S41586-025-10061-7 2026-01-14
Gs αs Human Gs-alpha short isoform Gnas-2 57 β1 Human γ2 Human Cryo-EM 9LLE - 2.9 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
GEM targeting TM1/2/4
Small molecule
Protein 		Agonist
Allosteric agonist 		5-hydroxytryptamine, noradrenaline, dopamine Small molecule - - 2026-03-04
Gs αs Human Gs heterotrimer; Gα is short isoform Gnas-2 57 β1 Human γ2 Human Cryo-EM 9LLF - 2.6 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 LgBiT dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
De novo designed GPCR exoframe modulator (GEM)
Small molecule
Protein 		Agonist
PAM 		5-hydroxytryptamine, noradrenaline, dopamine Small molecule - - 2026-03-04
Gi/o αi1 Human Gi: human Gαi1, rat Gβ1, bovine Gγ2 62 β1 Rat γ2 Bovine Cryo-EM 9LRD - 3.2 HRH1 HRH1 H1 Histamine A (Rhodopsin) Human - - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule Matsuzaki Y, Sano FK, Oshima HS, Akasaka H, Kobayashi K, Tanaka T, Itoh Y, Shihoya W, Kise Y, Kusakizako T, Inoue A, Nureki O 10.1038/S42003-025-08363-7 2025-06-11
Gi/o αi1 Human dnGi: dominant-negative Gi for stabilization 59 β1 Rat γ2 Bovine Cryo-EM 9LRE - 2.8 HRH4 HRH4 H4 Histamine A (Rhodopsin) Human - - - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist CCL16 (Human), histamine Small molecule Matsuzaki Y, Sano FK, Oshima HS, Akasaka H, Kobayashi K, Tanaka T, Itoh Y, Shihoya W, Kise Y, Kusakizako T, Inoue A, Nureki O 10.1038/S42003-025-08363-7 2025-06-11
Gs αs Human MiniGs (short isoform) α subunit 59 β1 Human γ2 Human Cryo-EM 9LW5 - 2.9 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule - - 2026-02-18
Gs αs Human Human Gs heterotrimer; β1/γ2 species unclear 54 β1 Human γ2 Human Cryo-EM 9M8V - 3.8 GPR3 GPR3 GPR3 Orphan A (Rhodopsin) Human BRIL - - AF64394 pubchem
Small molecule NAM sphingosine 1-phosphate Lipid - - 2025-09-24
Gs αs Human DNGs: 8 stabilizing mutations 61 β1 Human γ2 Human Cryo-EM 9LYB - 3.2 GPR3 GPR3 GPR3 Orphan A (Rhodopsin) Human BRIL Nanobody-35 - - None - sphingosine 1-phosphate Lipid Chang H, Li X, Tu H, Wu L, Yu Y, Liu J, Chen N, Shen WL, Hua T 10.1016/J.CELREP.2025.115478 2025-04-09
Gi/o αi1 Human DN Gi1: G203A/A326S; NanoBiT LgBiT/HiBiT 64 β1 Rat γ2 Bovine Cryo-EM 9M1O - 2.5 NPFF2 NPFFR2 NPFF2 Neuropeptide FF/neuropeptide AF A (Rhodopsin) Human BRIL - - neuropeptide FF (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist QRFP43 (43RFa) (Human), neuropeptide AF (Rat), neuropeptide AF (Human), RFRP-3 (Human), neuropeptide SF (Human), PrRP-31 (Human), neuropeptide AF (Mouse), neuropeptide FF (Human), RFRP-1 (Human) Peptide Li X, Zhang H, Hu W, Wu K, Li S, Jin S, Yin Y, Yuan Q, Xu HE, Pan B, Jiang Y 10.1016/J.CELREP.2025.116160 2025-07-23
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 9M1P - 2.8 Q5QNQ1 taar13d taar13d Unclassified A (Rhodopsin) Zebrafish - Nanobody-35 - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist - - - - 2026-03-04
Gi/o αi1 Human DN Gαi1: G203A/A326S, low GDP affinity 64 β1 Rat γ2 Bovine Cryo-EM 9M2F - 2.9 NPFF1 NPFFR1 NPFF1 Neuropeptide FF/neuropeptide AF A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		neuropeptide FF
Peptide Agonist QRFP43 (43RFa) (Human), neuropeptide AF (Rat), neuropeptide AF (Human), neuropeptide SF (Mouse), RFRP-3 (Human), neuropeptide SF (Human), PrRP-31 (Human), neuropeptide AF (Mouse), neuropeptide FF (Human), RFRP-1 (Human), neuropeptide SF (Rat) Peptide Li X, Zhang H, Hu W, Wu K, Li S, Jin S, Yin Y, Yuan Q, Xu HE, Pan B, Jiang Y 10.1016/J.CELREP.2025.116160 2025-07-23
Gs αs Human Gαs (short isoform) subunit 59 β1 Human γ2 Human Cryo-EM 9M2O - 2.6 Q5QNQ1 taar13d taar13d Unclassified A (Rhodopsin) Zebrafish - Nanobody-35 - Putrescine pubchem drugbank
Small molecule Agonist - - - - 2026-03-04
Gs αs Human Gs α subunit, short isoform 59 β1 Human γ2 Human Cryo-EM 9M2S - 2.8 TA13C taar13c taar13c Orphan A (Rhodopsin) Zebrafish - Nanobody-35 - Cadaverine pubchem drugbank
Small molecule Agonist - - - - 2026-03-04
Gs αs Human Gs α subunit, short isoform 59 β1 Human γ2 Human Cryo-EM 9M3Q - 2.7 TA13C taar13c taar13c Orphan A (Rhodopsin) Zebrafish - Nanobody-35 - SPERMIDINE chembl_ligand pubchem drugbank
Small molecule Agonist - - - - 2026-03-11
Gs αs Human Gs heterotrimer 59 β1 Human γ2 Human Cryo-EM 9M3S - 2.8 Q5QNP9 taar13a taar13a Unclassified A (Rhodopsin) Zebrafish - Nanobody-35 - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist - - - - 2026-03-11
Gi/o αi1 Human DN Gαi1: S47N/G203A/E245A/A326S 63 β1 Human γ2 Human Cryo-EM 9MB9 - 3.0 GRM8 GRM8 mGlu8 Metabotropic glutamate C (Glutamate) Human - - - VU0422288 pubchem gtoplig chembl_ligand
(S)-3,4-DCPG pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Ago-PAM
Agonist 		L-serine-O-phosphate, L-glutamic acid Small molecule - - 2025-10-01
Gs αs Human Gs heterotrimer 59 β1 Human γ2 Human Cryo-EM 9MZG - 3.0 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Glucagon pubchem
Small molecule Agonist glucagon (Human) Protein - - 2026-04-22
Gs αs Human Gs heterotrimer stabilized by Nb35 59 β1 Human γ2 Human Cryo-EM 9N04 - 2.3 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 15
Peptide Agonist glucagon (Human) Protein - - 2026-04-22
Gs αs Human Human Gs heterotrimer: Gαs-short/Gβ1/Gγ2 58 β1 Human γ2 Human Cryo-EM 9N05 - 2.2 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - SRB103Q
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein - - 2026-04-22
Gs αs Human Wild-type Gs heterotrimer 58 β1 Human γ2 Human Cryo-EM 9N0E - 2.3 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - Oxyntomodulin pubchem pubchem
Small molecule Agonist glucagon (Human) Protein - - 2026-04-22
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 9N1P - 2.9 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - SRB103H
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein - - 2026-04-22
Gs αs Human - 58 β1 Human γ2 Human Cryo-EM 9N1Q - 3.0 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - SRB103H
Peptide Agonist glucagon (Human) Protein - - 2026-04-22
Gi/o αi1 Human DN Gαi1 with G203A/A326S mutations 63 β1 Human γ2 Human Cryo-EM 9NS9 - 3.3 FFAR2 FFAR2 FFA2 Free fatty acid A (Rhodopsin) Human - - - CHEMBL5965059 chembl_ligand pubchem
CHEMBL4176503 chembl_ligand pubchem
Small molecule
Small molecule 		Ago-PAM
Agonist 		butyric acid, propanoic acid, trans-2-methylcrotonic acid, acetic acid Small molecule - - 2025-06-25
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 9O36 - 2.3 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - Fluornitrazene pubchem
Small molecule Agonist - - - - 2026-04-01
Gi/o αi1 Human Wild-type Gi1 heterotrimer 98 β1 Human γ2 Human Cryo-EM 9ODL - 3.6 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - Mitragynine pseudoindoxyl
Small molecule Agonist (partial) - - Robertson MJ, Modak A, Papasergi-Scott MM, Hu M, Peroto MC, Varga BR, Majumdar S, Kalathur R, Blanchard SC, Skiniotis G 10.1038/S41586-025-10056-4 2026-01-07
Gi/o αi1 Human Nucleotide-free Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 9ODM - 2.8 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - DAMGO pubchem gtoplig chembl_ligand pubchem
Peptide Agonist - - - - 2026-03-04
Gi/o αi1 Human Gαi1 heterotrimer, GTP-bound G-primed state 62 β1 Human γ2 Human Cryo-EM 9ODN - 2.4 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - DAMGO pubchem gtoplig chembl_ligand pubchem
Peptide Agonist - - - - 2026-03-04
Gi/o αi1 Human Human Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 9P0K - 3.5 CXCR3 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human - - FP506 CXCL9
Protein Agonist (partial) CXCL9 (Mouse), CCL20 (Human), CCL19 (Human), CXCL10 (Human), CXCL10 (Mouse), CCL11 (Human), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CXCL12α (Human), CXCL9 (Human), CCL5 (Human), CXCL11 (Human) Peptide Bouyssou A, Sun D, Zhou T, Smith S, Ho H, Johnson M, Azumaya C, Noreng S, Liu P, Ti S, Joshi P, Tam C, Yang Y, Janezic E, Comps-Agrar L, Masureel M 10.1126/SCIADV.ADZ3767 2026-04-29
Gi/o αi1 Human Wild-type Gi1 heterotrimer 60 β1 Human γ2 Human Cryo-EM 9P0L - 3.1 CXCR3 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human - - GFP-like fluorescent chromoprotein FP506 CXCL10
Protein Agonist (partial) CXCL9 (Mouse), CCL20 (Human), CCL19 (Human), CXCL10 (Human), CXCL10 (Mouse), CCL11 (Human), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CXCL12α (Human), CXCL9 (Human), CCL5 (Human), CXCL11 (Human) Peptide Bouyssou A, Sun D, Zhou T, Smith S, Ho H, Johnson M, Azumaya C, Noreng S, Liu P, Ti S, Joshi P, Tam C, Yang Y, Janezic E, Comps-Agrar L, Masureel M 10.1126/SCIADV.ADZ3767 2026-04-29
Gi/o αi1 Human Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 9P0M - 3.0 CXCR3 CXCR3 CXCR3 Chemokine A (Rhodopsin) Human - - GFP-like fluorescent chromoprotein FP506 CXCL11
Protein Agonist CXCL9 (Mouse), CCL20 (Human), CCL19 (Human), CXCL10 (Human), CXCL10 (Mouse), CCL11 (Human), CCL7 (Human), CXCL10 (Rat), CXCL11 (Mouse), CCL13 (Human), CXCL12α (Human), CXCL9 (Human), CCL5 (Human), CXCL11 (Human) Peptide Bouyssou A, Sun D, Zhou T, Smith S, Ho H, Johnson M, Azumaya C, Noreng S, Liu P, Ti S, Joshi P, Tam C, Yang Y, Janezic E, Comps-Agrar L, Masureel M 10.1126/SCIADV.ADZ3767 2026-04-29
Gi/o αi1 Human WT G protein heterotrimer, apo (nucleotide-free) 62 β1 Human γ2 Human Cryo-EM 9P7Z - 2.1 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 96 β1 Human γ2 Human Cryo-EM 9P84 - 2.7 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gq/11 α11 Human WT Gα11 heterotrimer, nucleotide-free (apo) 61 β1 Human γ2 Human Cryo-EM 9P86 - 2.9 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gq/11 α11 Human Nucleotide-free state, AHD partially closed 61 β1 Human γ2 Human Cryo-EM 9P87 - 2.8 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gq/11 α11 Human Wild-type Gα11 heterotrimer 61 β1 Human γ2 Human Cryo-EM 9P88 - 2.9 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gq/11 α11 Human WT Gα11 heterotrimer, expressed in Tni cells 97 β1 Human γ2 Human Cryo-EM 9P89 - 3.9 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gs αs Human DNGs: dominant-negative Gs protein 57 β1 Human γ2 Human Cryo-EM 9P92 - 3.8 PACR ADCYAP1R1 PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - Vasoactive intestinal polypeptide pubchem
Small molecule Agonist PHV (Rat), VIP (Human), PHV (Human), PHM (Human), PHI (Mouse), PACAP-38 (Human), PACAP-27 (Human) Protein Lu JJ, Deganutti G, Li M, Humphrys LJ, Li Y, Nettleton TJ, Venugopal H, Julita V, Christopoulos G, Reynolds CA, Sexton PM, Wootten D, Zhao P, Piper SJ 10.1073/PNAS.2521157122 2025-11-19
Gs αs Human DNGs: dominant-negative Gs protein 57 β1 Human γ2 Human Cryo-EM 9P93 - 3.2 PACR ADCYAP1R1 PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - Vasoactive intestinal polypeptide pubchem
Small molecule Agonist PHV (Rat), VIP (Human), PHV (Human), PHM (Human), PHI (Mouse), PACAP-38 (Human), PACAP-27 (Human) Protein Lu JJ, Deganutti G, Li M, Humphrys LJ, Li Y, Nettleton TJ, Venugopal H, Julita V, Christopoulos G, Reynolds CA, Sexton PM, Wootten D, Zhao P, Piper SJ 10.1073/PNAS.2521157122 2025-11-19
Gs αs Human DNGs: G226A/S285E mutations 58 β1 Human γ2 Human Cryo-EM 9P94 - 3.0 PACR ADCYAP1R1 PAC1 VIP and PACAP B1 (Secretin) Human - Nanobody-35 - PACAP-27 (Human) pubchem gtoplig uniprot uniprot uniprot uniprot pubchem
Protein Agonist PHV (Rat), VIP (Human), PHV (Human), PHM (Human), PHI (Mouse), PACAP-38 (Human), PACAP-27 (Human) Protein Lu JJ, Deganutti G, Li M, Humphrys LJ, Li Y, Nettleton TJ, Venugopal H, Julita V, Christopoulos G, Reynolds CA, Sexton PM, Wootten D, Zhao P, Piper SJ 10.1073/PNAS.2521157122 2025-11-19
Gi/o αi1 Human DN human Gαi1: S47N/E245A/G203A/A326S 62 β1 Human γ2 Human Cryo-EM 9PA4 - 2.5 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - ESKETAMINE chembl_ligand pubchem drugbank
Small molecule Agonist (partial) [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Jiang Q, Han J, Fine EJ, Ramos-Gonzalez N, Rangari VA, Ruiz MV, Critz ML, Suomivuori CM, Wang J, Albert TL, Whiddon K, Li K, Robertson MJ, Huang XP, Land BB, Majumdar S, Fay JF, Dror RO, Che T 10.1038/S41594-026-01839-Y 2026-07-01
Gi/o αi1 Human DN Gαi1: S47N/E245A/G203A/A326S 64 β1 Human γ2 Human Cryo-EM 9PA5 - 2.9 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - ESKETAMINE chembl_ligand pubchem drugbank
Small molecule Agonist (partial) [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Jiang Q, Han J, Fine EJ, Ramos-Gonzalez N, Rangari VA, Ruiz MV, Critz ML, Suomivuori CM, Wang J, Albert TL, Whiddon K, Li K, Robertson MJ, Huang XP, Land BB, Majumdar S, Fay JF, Dror RO, Che T 10.1038/S41594-026-01839-Y 2026-07-01
Gi/o αi1 Human DN human Gαi1: S47N/E245A/G203A/A326S 62 β1 Human γ2 Human Cryo-EM 9PA6 - 3.4 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - - None - [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Jiang Q, Han J, Fine EJ, Ramos-Gonzalez N, Rangari VA, Ruiz MV, Critz ML, Suomivuori CM, Wang J, Albert TL, Whiddon K, Li K, Robertson MJ, Huang XP, Land BB, Majumdar S, Fay JF, Dror RO, Che T 10.1038/S41594-026-01839-Y 2026-07-01
Gi/o αo Human Go heterotrimer (Gαo1β1γ2) 63 β1 Human γ2 Human Cryo-EM 9PLO - 2.8 ADA2A ADRA2A α2A Adrenoceptors A (Rhodopsin) Human - - - N-(5-methylnaphthalen-1-yl)pyridin-4-amine pubchem
Small molecule Agonist (-)-noradrenaline, (-)-adrenaline Small molecule - - 2025-07-30
Gi/o αi1 Human Wild-type Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 9PXV - 3.0 OPRM OPRM1 μ Opioid A (Rhodopsin) Human BRIL - - naloxone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem
Small molecule Agonist (partial) [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2025-11-12
Gi/o αi1 Human Wild-type human Gi heterotrimer 99 β1 Human γ2 Human Cryo-EM 9PXW - 3.8 OPRM OPRM1 μ Opioid A (Rhodopsin) Human BRIL - - naloxone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem
Small molecule Agonist (partial) [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2025-11-12
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 9PXX - 3.1 OPRM OPRM1 μ Opioid A (Rhodopsin) Human BRIL - - naloxone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem
Small molecule Agonist (partial) [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2025-11-12
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 97 β1 Human γ2 Human Cryo-EM 9PXY - 3.0 OPRM OPRM1 μ Opioid A (Rhodopsin) Human BRIL - - naloxone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem
Small molecule Agonist (partial) [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2025-11-12
Gi/o αi1 Human Gi1 heterotrimer, GDPβS-bound unlatched state 64 β1 Human γ2 Human Cryo-EM 9PY3 - 3.2 OPRM OPRM1 μ Opioid A (Rhodopsin) Human BRIL - - loperamide pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2025-11-12
Gi/o αi1 Human WT human Gi heterotrimer, GDPβS-primed state 97 β1 Human γ2 Human Cryo-EM 9PY4 - 2.8 OPRM OPRM1 μ Opioid A (Rhodopsin) Human BRIL - - loperamide pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2025-11-12
Gi/o αi1 Human Gi1 heterotrimer 66 β1 Human γ2 Human Cryo-EM 9JR0 - 3.1 Q9BML6 GABA-B-R2 GABA-B-R2 Unclassified C (Glutamate) Fruit fly - - - GABA pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist - - - - 2025-10-22
Gi/o αi1 Human DNGai1: S47C/G202T/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 9K1C 9K1C_refined 3.2 FFAR1 FFAR1 FFA1 Free fatty acid A (Rhodopsin) Human - - - docosahexaenoic acid pubchem gtoplig chembl_ligand drug_central drugbank
Small molecule Agonist oleic acid, docosahexaenoic acid, α-linolenic acid, myristic acid Small molecule Ke Y, Huang Y, Yi C, Ma L, Chu X, Wu B, Zhao Q, Han S 10.1016/J.CELREP.2024.115024 2024-12-11
Gi/o αo Human Mini-Go/Gαi1 N-term chimera for scFv16 binding 60 β1 Human γ2 Human Cryo-EM 9K20 - 2.7 P2RY2 P2RY2 P2Y2 P2Y A (Rhodopsin) Human - - - ATP pubchem gtoplig chembl_ligand drugbank drug_central
Small molecule Agonist UTP, ATP Small molecule Lan B, Zhang S, Chen K, Dai S, Fei J, Gao K, Sun X, Lin B, Liu X 10.1038/S41421-025-00797-X 2025-06-11
Gi/o αi1 Human Gi1 heterotrimer, stabilized by scFv16 58 β1 Human γ2 Human Cryo-EM 9K26 - 3.0 PRLHR PRLHR PrRP Prolactin-releasing peptide A (Rhodopsin) Human - - - PrRP31 pubchem
Peptide Agonist PrRP-20 (Human), PrRP-20 (Rat), neuropeptide Y (Human), PTHrP (Human), PrRP-31 (Rat), PrRP-31 (Human) Peptide - - 2025-01-29
Gq/11 αq Human Native Gq heterotrimer 64 β1 Human γ2 Human Cryo-EM 9K27 9K27_refined 2.7 PRLHR PRLHR PrRP Prolactin-releasing peptide A (Rhodopsin) Human - - - PrRP31 pubchem
Peptide Agonist PrRP-20 (Human), PrRP-20 (Rat), neuropeptide Y (Human), PTHrP (Human), PrRP-31 (Rat), PrRP-31 (Human) Peptide - - 2025-01-29
Gs αs Human Mini-Gs (G112): Gs/Gi1 chimera segments 58 β1 Human γ2 Bovine Cryo-EM 9K3L - 3.0 ACTHR MC2R MC2 Melanocortin A (Rhodopsin) Human - Nanobody-35 LgBiT subunit
HiBiT 		- None - ACTH (Human), ACTH (Mouse) Peptide Feng W, Zhou Q, Zheng C, Yang D, Wang MW 10.1016/J.STR.2025.03.004 2025-08-06
Gs αs Human G112: Gs/Gi1 chimera; α5 tail=Gs 59 β1 Human γ2 Bovine Cryo-EM 9K3P - 3.0 MSHR MC1R MC1 Melanocortin A (Rhodopsin) Human - Nanobody-35 LgBiT subunit
HiBiT subunit 		- None - ACTH (Human), ACTH (Mouse), β-MSH (Human), α-MSH (Human), β-MSH (Mouse), γ-MSH (Human), β-MSH (Rat) Peptide Feng W, Zhou Q, Zheng C, Yang D, Wang MW 10.1016/J.STR.2025.03.004 2025-08-06
Gi/o αi2 Human DN human Gαi2 (DNGi2): S47N/G204A/E246A/A327S 62 β1 Human γ2 Bovine Cryo-EM 9KFK - 3.0 RL3R2 RXFP4 RXFP4 Relaxin family peptide A (Rhodopsin) Human BRIL - LgBiT Relaxin-3 (chain A)
Relaxin-3 (chain B)
Peptide
Peptide 		Agonist relaxin-3 (B chain) (Human), relaxin-3 (Human), INSL5 (Human) Peptide Chen Y, Zhou Q, Yan S, Yan J, Yang D, Chen J, Wang MW 10.1038/S42003-025-08220-7 2025-08-13
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 9KFT - 3.1 FPR1 FPR1 FPR1 Formylpeptide A (Rhodopsin) Human - - - fMLFC peptide
Peptide Agonist spinorphin (Human), cathepsin G (Rat), fMet-Leu-Phe-Ile-Ile, annexin I-(2-26) (Human), mitochondrial peptde fMMYALF, mitochondrial peptide fMFADRW, fMet-Leu-Phe, annexin I (Rat), annexin I (Mouse), cathepsin G (Mouse), cathepsin G (Human), annexin I (Human) Peptide - - 2025-11-12
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 9KPF - 3.2 T2R16 TAS2R16 TAS2R16 Taste 2 T2 (Taste 2) Human - - exo-alpha-sialidase NanA
LgBiT 		salicin pubchem gtoplig
Small molecule Agonist - - Wang X, Zhou C, Ao W, Wu L, Wu Y, Xu W, Liu S, Tan Q, Wang L, Zhao F, Liu J, Pei Y, Zhao S, Hua T 10.1016/J.CELREP.2025.115604 2025-04-02
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 9KT6 - 3.0 HCAR3 HCAR3 HCA3 Hydroxycarboxylic acid A (Rhodopsin) Human - - - Acifran pubchem
Small molecule Agonist 3-hydroxyoctanoic acid Small molecule Wang J, Qian Y, Han Z, Wang Y, Liu Y, Li J, Duanmu Q, Ye S, Qiao A, Wu S 10.1021/ACS.JMEDCHEM.4C02567 2025-12-10
Gi/o αi1 Human Gi1 heterotrimer complex 64 β1 Human γ2 Human Cryo-EM 9KT7 - 2.8 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - MK 6892 pubchem gtoplig chembl_ligand pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Wang J, Qian Y, Han Z, Wang Y, Liu Y, Li J, Duanmu Q, Ye S, Qiao A, Wu S 10.1021/ACS.JMEDCHEM.4C02567 2025-12-10
Gi/o αi1 Human Recombinant human Gi heterotrimer 64 β1 Human γ2 Human Cryo-EM 9KT8 - 2.7 HCAR2 HCAR2 HCA2 Hydroxycarboxylic acid A (Rhodopsin) Human BRIL - - Acifran pubchem
Small molecule Agonist butyric acid, β-D-hydroxybutyric acid Small molecule Wang J, Qian Y, Han Z, Wang Y, Liu Y, Li J, Duanmu Q, Ye S, Qiao A, Wu S 10.1021/ACS.JMEDCHEM.4C02567 2025-12-10
Gi/o αi1 Human Gi heterotrimer 64 β1 Human γ2 Human Cryo-EM 9KT9 - 2.7 HCAR1 HCAR1 HCA1 Hydroxycarboxylic acid A (Rhodopsin) Human - - - 3,5-dihydroxybenzoic acid pubchem gtoplig chembl_ligand
Small molecule Agonist D-lactic acid Small molecule Wang J, Qian Y, Han Z, Wang Y, Liu Y, Li J, Duanmu Q, Ye S, Qiao A, Wu S 10.1021/ACS.JMEDCHEM.4C02567 2025-12-10
Gi/o αo Human Mini-Go: N-term ScFv16 binding sequence 58 β1 Human γ2 Human Cryo-EM 9KVP - 2.8 C3AR C3AR1 C3a Complement peptide A (Rhodopsin) Human - - M4 N-terminal region fusion SB290157 pubchem gtoplig chembl_ligand
Small molecule Agonist C5a (Rat), C3a (Mouse), C5a (Mouse), C3a (Human), C5a (Human), C3a (Rat) Peptide - - 2025-11-26
Gi/o αo Human MiniGαo: stabilizing muts + N-term scFv16 59 β1 Human γ2 Human Cryo-EM 9KWG - 3.2 C5AR1 C5ar1 C5a1 Complement peptide A (Rhodopsin) Mouse - - M4 N-terminal tag C5A pubchem
Small molecule Agonist - - Mishra S, Yadav MK, Dalal A, Ganguly M, Yadav R, Sawada K, Tiwari D, Roy N, Banerjee N, Fung JN, Marallag J, Cui CS, Li XX, Lee JD, Dsouza CA, Saha S, Sarma P, Rawat G, Zhu H, Khant HA, Clark RJ, Sano FK, Banerjee R, Woodruff TM, Nureki O, Gati C, Shukla AK 10.1101/2025.05.26.656101 2025-11-26
Gi/o αo Human MiniGαo(1-240) + N-term scFv16 sequence 59 β1 Human γ2 Human Cryo-EM 9KWX - 3.1 C5AR1 C5ar1 C5a1 Complement peptide A (Rhodopsin) Mouse - - Muscarinic acetylcholine receptor M4 (residues 2-23) C5a-desArg
Peptide Agonist - - Mishra S, Yadav MK, Dalal A, Ganguly M, Yadav R, Sawada K, Tiwari D, Roy N, Banerjee N, Fung JN, Marallag J, Cui CS, Li XX, Lee JD, Dsouza CA, Saha S, Sarma P, Rawat G, Zhu H, Khant HA, Clark RJ, Sano FK, Banerjee R, Woodruff TM, Nureki O, Gati C, Shukla AK 10.1101/2025.05.26.656101 2025-11-26
Gi/o αo Human MiniGαo1 with N-term scFv16 binding site 58 β1 Human γ2 Human Cryo-EM 9L0H - 3.6 C3AR C3ar1 C3a Complement peptide A (Rhodopsin) Mouse - - Muscarinic acetylcholine receptor M4 N-terminal segment JR14a pubchem gtoplig chembl_ligand
Small molecule Agonist - - - - 2025-11-26
Gi/o αi1 Human Wild-type Gi1 heterotrimer 58 β1 Human γ2 Human Cryo-EM 9L3W - 3.5 CML1 CMKLR1 chemerin Chemerin receptor A (Rhodopsin) Human - - - Chemerin
Protein Agonist 18R-HEPE, EPA, resolvin E1, chemerin (Human) Peptide Lin X, Zhao L, Cai H, Chang X, Tang Y, Luo T, Wu M, Yi C, Ma L, Chu X, Han S, Zhao Q, Wu B, He M, Zhu Y 10.1093/PROCEL/PWAE073 2025-03-12
Gi/o αi1 Human Wild-type human Gi1 protein 60 β1 Human γ2 Human Cryo-EM 9L3Y - 3.6 CML2 CMKLR2 chemerin 2 Chemerin receptor A (Rhodopsin) Human - - - Chemerin
Protein Agonist chemerin (Human) Peptide Lin X, Zhao L, Cai H, Chang X, Tang Y, Luo T, Wu M, Yi C, Ma L, Chu X, Han S, Zhao Q, Wu B, He M, Zhu Y 10.1093/PROCEL/PWAE073 2025-03-12
Gs αs Human DNGs: 8 muts incl S54N/G226A/E268A 61 β1 Human γ2 Human Cryo-EM 9LGM - 2.8 GPR4 GPR4 GPR4 Proton A (Rhodopsin) Human - Nanobody-35 Endoglucanase H - None - - - Yue X, Peng L, Liu S, Zhang B, Zhang X, Chang H, Pei Y, Li X, Liu J, Shui W, Wu L, Xu H, Liu ZJ, Hua T 10.1038/S41422-025-01092-W 2025-04-23
Gs αs Human Gs heterotrimer 56 β1 Human γ2 Human Cryo-EM 9LLH - 2.7 DRD1 DRD1 D1 Dopamine A (Rhodopsin) Human - Nanobody-35 LgBiT Agonist-positive allosteric GEM targeting TM5/6/7
dopamine pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Protein
Small molecule 		Ago-PAM
Agonist 		5-hydroxytryptamine, noradrenaline, dopamine Small molecule - - 2026-03-04
Gi/o αi1 Human Human Gi heterotrimer (Gαi1/Gβ1/Gγ2) 62 β1 Human γ2 Human Cryo-EM 9LR2 - 3.1 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - JN241-9
Protein Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide - - 2026-02-04
Gi/o αi1 Human - 62 β1 Human γ2 Human Cryo-EM 9LR3 - 2.8 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - azelaprag pubchem gtoplig chembl_ligand chembl_ligand pubchem
Small molecule Agonist apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide - - 2026-02-04
Gs αs Human Mini-Gαs construct 59 β1 Rat γ2 Bovine Cryo-EM 9LRB - 2.8 HRH1 HRH1 H1 Histamine A (Rhodopsin) Human - Nanobody-35 - histamine pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist histamine Small molecule Matsuzaki Y, Sano FK, Oshima HS, Akasaka H, Kobayashi K, Tanaka T, Itoh Y, Shihoya W, Kise Y, Kusakizako T, Inoue A, Nureki O 10.1038/S42003-025-08363-7 2025-06-11
Gs αs Human DN Gs: 8 mutations to improve stability 60 β1 Human γ2 Human Cryo-EM 9LYC - 3.1 GPR3 GPR3 GPR3 Orphan A (Rhodopsin) Human - Nanobody-35 - - None - sphingosine 1-phosphate Lipid Chang H, Li X, Tu H, Wu L, Yu Y, Liu J, Chen N, Shen WL, Hua T 10.1016/J.CELREP.2025.115478 2025-04-09
Gi/o αi1 Human DN Gαi1: G203A/A326S 64 β1 Rat γ2 Bovine Cryo-EM 9M0R - 2.5 NPFF1 NPFFR1 NPFF1 Neuropeptide FF/neuropeptide AF A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		Neuropeptide VF pubchem
Peptide Agonist QRFP43 (43RFa) (Human), neuropeptide AF (Rat), neuropeptide AF (Human), neuropeptide SF (Mouse), RFRP-3 (Human), neuropeptide SF (Human), PrRP-31 (Human), neuropeptide AF (Mouse), neuropeptide FF (Human), RFRP-1 (Human), neuropeptide SF (Rat) Peptide Li X, Zhang H, Hu W, Wu K, Li S, Jin S, Yin Y, Yuan Q, Xu HE, Pan B, Jiang Y 10.1016/J.CELREP.2025.116160 2025-07-23
Gs αs Human Gs α subunit, short isoform 59 β1 Human γ2 Human Cryo-EM 9M0Z - 2.7 Q5QNQ1 taar13d taar13d Unclassified A (Rhodopsin) Zebrafish - Nanobody-35 - Cadaverine pubchem drugbank
Small molecule Agonist - - - - 2026-03-04
Gs αs Human Gs α subunit, short isoform 60 β1 Human γ2 Human Cryo-EM 9M40 - 2.7 Q5QNP8 taar13e taar13e Unclassified A (Rhodopsin) Zebrafish - Nanobody-35 - Agmatine pubchem drugbank
Small molecule Agonist - - - - 2026-03-11
Gs αs Human Gαs (short isoform) subunit 58 β1 Human γ2 Human Cryo-EM 9MZE - 2.2 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Oxyntomodulin pubchem pubchem
Small molecule Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein - - 2026-04-22
Gs αs Human - 59 β1 Human γ2 Human Cryo-EM 9MZF - 2.5 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - Nanobody-35 - Peptide 15
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein - - 2026-04-22
Gs αs Human Gs heterotrimer 58 β1 Human γ2 Human Cryo-EM 9N2I - 3.0 GLR GCGR glucagon Glucagon B1 (Secretin) Human - Nanobody-35 - SRB103Q
Peptide Agonist glucagon (Human) Protein - - 2026-04-22
Gi/o αi1 Human WT Gi heterotrimer, no antibody fragments 61 β1 Human γ2 Human Cryo-EM 9ODE - 2.5 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - LOFENTANIL chembl_ligand pubchem drugbank
Small molecule Agonist - - Robertson MJ, Modak A, Papasergi-Scott MM, Hu M, Peroto MC, Varga BR, Majumdar S, Kalathur R, Blanchard SC, Skiniotis G 10.1038/S41586-025-10056-4 2026-03-04
Gi/o αi1 Human WT Gi1 heterotrimer, no antibody fragments 62 β1 Human γ2 Human Cryo-EM 9ODF - 2.4 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - LOFENTANIL chembl_ligand pubchem drugbank
Small molecule Agonist - - Robertson MJ, Modak A, Papasergi-Scott MM, Hu M, Peroto MC, Varga BR, Majumdar S, Kalathur R, Blanchard SC, Skiniotis G 10.1038/S41586-025-10056-4 2026-03-04
Gi/o αi1 Human GTP-bound G-ACT-2 activation intermediate 97 β1 Human γ2 Human Cryo-EM 9ODK - 3.9 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - - None - - - Robertson MJ, Modak A, Papasergi-Scott MM, Hu M, Peroto MC, Varga BR, Majumdar S, Kalathur R, Blanchard SC, Skiniotis G 10.1038/S41586-025-10056-4 2026-01-07
Gi/o αi1 Human DN Gs protein; NanoBiT tethering used 62 β1 Human γ2 Human Cryo-EM 9OXA - 2.9 T2R43 TAS2R43 TAS2R43 Taste 2 T2 (Taste 2) Human BRIL - - aristolochic acid pubchem gtoplig chembl_ligand
Small molecule Agonist - - Kim Y, Gumpper RH, Zhuang Y, Dror RO, Roth BL 10.1038/S41594-026-01776-W 2026-04-22
Gi/o αi1 Human Wild-type Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 9P80 - 2.3 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gi/o αi1 Human Wild-type Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 9P81 - 2.6 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gi/o αi1 Human WT Gi1, GTP-bound closed-AHD intermediate 99 β1 Human γ2 Human Cryo-EM 9P82 - 2.4 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gi/o αi1 Human Wild-type Gi1 heterotrimer 60 β1 Human γ2 Human Cryo-EM 9P83 - 3.2 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - NTS8–13 pubchem
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 10.1038/S41586-026-10120-7 2026-03-25
Gi/o αi1 Human DN Gαi1: S47N/E245A/G203A/A326S 63 β1 Human γ2 Human Cryo-EM 9PA1 - 2.6 OPRK OPRK1 κ Opioid A (Rhodopsin) Human BRIL - - PHENCYCLIDINE chembl_ligand pubchem drugbank pubchem drug_central
Small molecule Agonist (partial) [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Jiang Q, Han J, Fine EJ, Ramos-Gonzalez N, Rangari VA, Ruiz MV, Critz ML, Suomivuori CM, Wang J, Albert TL, Whiddon K, Li K, Robertson MJ, Huang XP, Land BB, Majumdar S, Fay JF, Dror RO, Che T 10.1038/S41594-026-01839-Y 2026-07-01
Gi/o αi1 Human DN Gαi1 (4 muts) fused to Gγ2 via linker 64 β1 Human γ2 Human Cryo-EM 9PA2 - 2.9 OPRM OPRM1 μ Opioid A (Rhodopsin) Human BRIL - - PHENCYCLIDINE chembl_ligand pubchem drugbank pubchem drug_central
Small molecule Agonist (partial) [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide Jiang Q, Han J, Fine EJ, Ramos-Gonzalez N, Rangari VA, Ruiz MV, Critz ML, Suomivuori CM, Wang J, Albert TL, Whiddon K, Li K, Robertson MJ, Huang XP, Land BB, Majumdar S, Fay JF, Dror RO, Che T 10.1038/S41594-026-01839-Y 2026-07-01
Gi/o αi1 Human DN Gαi1: S47N/E245A/G203A/A326S; Gα-Gγ linker 64 β1 Human γ2 Human Cryo-EM 9PA3 - 3.1 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - - 3-OH-PCP pubchem
Small molecule Agonist (partial) [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2026-07-01
Gi/o αi1 Human DN Gi1: S47N/E245A/G203A/A326S 56 β1 Human γ2 Human Cryo-EM 9PPW - 3.3 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - - - naltrindole pubchem gtoplig chembl_ligand
Small molecule Antagonist [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Bernhard SM, Roy Chowdhury S, Murata T, Reinl EL, Ramos-Gonzalez N, Denn E, Appourchaux K, Inoue A, England SK, Fay JF, Majumdar S, Chanda B, Che T 10.1126/SCIADV.AEB6737 2026-03-04
Gi/o αi1 Human DN Gαi1: S47N/E245A/G203A/A326S 31 β1 Human γ2 Human Cryo-EM 9PPX - 3.0 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - - - naltrexone pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem
Small molecule Antagonist [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-03-04
Gi/o αi1 Human DN Gαi1: S47N/E245A/G203A/A326S 56 β1 Human γ2 Human Cryo-EM 9PPY - 3.1 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - - - Met-enkephalin
Peptide Agonist [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Bernhard SM, Roy Chowdhury S, Murata T, Reinl EL, Ramos-Gonzalez N, Denn E, Appourchaux K, Inoue A, England SK, Fay JF, Majumdar S, Chanda B, Che T 10.1126/SCIADV.AEB6737 2026-03-04
Gi/o αi1 Human DN Gi1: S47N/E245A/G203A/A326S 58 β1 Human γ2 Human Cryo-EM 9PPZ - 3.2 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - - - SNC80 pubchem gtoplig chembl_ligand
Small molecule Agonist [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-03-04
Gi/o αi1 Human DN Gi1: S47N/E245A/G203A/A326S 57 β1 Human γ2 Human Cryo-EM 9PQ0 - 3.1 OPRD OPRD1 δ Opioid A (Rhodopsin) Human - - - ADL5859 pubchem gtoplig chembl_ligand
Small molecule Agonist [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-03-04
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 9R41 - 3.8 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human - - - buspirone pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (partial) 5-hydroxytryptamine Small molecule - - 2026-05-20
Gs αs Human Gs α subunit, short isoform 60 β1 Human γ2 Human Cryo-EM 9U9V - 2.9 ADRB2 ADRB2 β2 Adrenoceptors A (Rhodopsin) Human - Nanobody-35 - METHAMPHETAMINE chembl_ligand pubchem drugbank drug_central
Small molecule Agonist (-)-noradrenaline, noradrenaline, (-)-adrenaline, Zn2+ Small molecule - - 2025-09-03
Gi/o αo Human MiniGαo, N-term scFv16 binding sequence 59 β1 Human γ2 Human Cryo-EM 9UMJ - 3.4 C3AR C3ar1 C3a Complement peptide A (Rhodopsin) Mouse - - M4 N-terminus EP54
Peptide Agonist - - Mishra S, Yadav MK, Dalal A, Ganguly M, Yadav R, Sawada K, Tiwari D, Roy N, Banerjee N, Fung JN, Marallag J, Cui CS, Li XX, Lee JD, Dsouza CA, Saha S, Sarma P, Rawat G, Zhu H, Khant HA, Clark RJ, Sano FK, Banerjee R, Woodruff TM, Nureki O, Gati C, Shukla AK 10.1101/2025.05.26.656101 2025-11-26
Gi/o αo Human MiniGαo with N-term scFv16 sequence 59 β1 Human γ2 Human Cryo-EM 9UMR - 3.2 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - Muscarinic acetylcholine receptor M4 N-terminal fragment C5a-pep
Peptide Agonist C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide Mishra S, Yadav MK, Dalal A, Ganguly M, Yadav R, Sawada K, Tiwari D, Roy N, Banerjee N, Fung JN, Marallag J, Cui CS, Li XX, Lee JD, Dsouza CA, Saha S, Sarma P, Rawat G, Zhu H, Khant HA, Clark RJ, Sano FK, Banerjee R, Woodruff TM, Nureki O, Gati C, Shukla AK 10.1101/2025.05.26.656101 2025-11-26
Gi/o αi1 Human - 64 β1 Rat γ2 Human Cryo-EM 9UXX - 3.6 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - salvinorin A pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem chembl_ligand pubchem drugbank
Small molecule Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-05-27
Gi/o αo Human Native human G protein subunits 63 β1 Human γ2 Human Cryo-EM 9VAV - 3.0 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Native human Gi1 heterotrimer, nucleotide-free 62 β1 Human γ2 Human Cryo-EM 9VAX - 3.5 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Native human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 9VB1 - 3.3 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Wild-type Gi1 heterotrimer 99 β1 Human γ2 Human Cryo-EM 9VB2 - 3.1 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human - 61 β1 Human γ2 Human Cryo-EM 9VI9 - 3.0 NPFF1 NPFFR1 NPFF1 Neuropeptide FF/neuropeptide AF A (Rhodopsin) Human - - - RFRP-3
Peptide Agonist QRFP43 (43RFa) (Human), neuropeptide AF (Rat), neuropeptide AF (Human), neuropeptide SF (Mouse), RFRP-3 (Human), neuropeptide SF (Human), PrRP-31 (Human), neuropeptide AF (Mouse), neuropeptide FF (Human), RFRP-1 (Human), neuropeptide SF (Rat) Peptide Na M, Yue Y, Xu K, Xu Z, Zhang L, Zhou F, De Neve J, Ballet S, Xu F 10.1093/PROCEL/PWAF090 2025-12-03
Gi/o αi1 Human Standard Gi heterotrimer for stabilization 61 β1 Human γ2 Human Cryo-EM 9VIF - 3.2 NPFF1 NPFFR1 NPFF1 Neuropeptide FF/neuropeptide AF A (Rhodopsin) Human - - - neuropeptide FF (Human) pubchem gtoplig chembl_ligand uniprot uniprot uniprot
Peptide Agonist QRFP43 (43RFa) (Human), neuropeptide AF (Rat), neuropeptide AF (Human), neuropeptide SF (Mouse), RFRP-3 (Human), neuropeptide SF (Human), PrRP-31 (Human), neuropeptide AF (Mouse), neuropeptide FF (Human), RFRP-1 (Human), neuropeptide SF (Rat) Peptide Na M, Yue Y, Xu K, Xu Z, Zhang L, Zhou F, De Neve J, Ballet S, Xu F 10.1093/PROCEL/PWAF090 2025-12-03
Gi/o αi1 Human - 64 β1 Human γ2 Human Cryo-EM 9VNZ - 2.8 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BRIL - - HY-X-1011 pubchem
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid - - 2026-01-28
Gi/o αi1 Human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 9VO0 - 2.8 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BRIL - - Ponesimod pubchem drugbank
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid - - 2026-01-28
Gi/o αi1 Human Gi heterotrimer 63 β1 Human γ2 Human Cryo-EM 9VO1 - 3.0 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BRIL - - SAR247799 pubchem gtoplig chembl_ligand
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid - - 2026-01-28
Gi/o αi1 Human Gi1 heterotrimer complex 63 β1 Human γ2 Human Cryo-EM 9W6W - 3.1 5HT5A HTR5A 5-HT5A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - 5-CT pubchem gtoplig chembl_ligand
Small molecule Agonist 5-hydroxytryptamine Small molecule Zhang X, Xie L, Chen P, Yu J, Tian X, Wang L, Wei J, Shao Z, Yan W, Xu Z 10.1186/S43556-025-00359-3 2025-11-26
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 9R42 - 3.2 DRD3 DRD3 D3 Dopamine A (Rhodopsin) Human BRIL - - quinpirole pubchem gtoplig chembl_ligand
Small molecule Agonist dopamine Small molecule - - 2026-05-20
Gi/o αo Human Mini-Gαo: N-term ScFv16 binding sequence 59 β1 Human γ2 Human Cryo-EM 9UMX - 3.2 C5AR1 C5AR1 C5a1 Complement peptide A (Rhodopsin) Human - - Muscarinic acetylcholine receptor M4 EP54
Peptide Agonist C5a des-Arg (Human), C5a (Rat), C3a (Mouse), C5a (Mouse), ribosomal protein S19 (Human), C3a (Human), C5a (Human), C3a (Rat) Peptide Mishra S, Yadav MK, Dalal A, Ganguly M, Yadav R, Sawada K, Tiwari D, Roy N, Banerjee N, Fung JN, Marallag J, Cui CS, Li XX, Lee JD, Dsouza CA, Saha S, Sarma P, Rawat G, Zhu H, Khant HA, Clark RJ, Sano FK, Banerjee R, Woodruff TM, Nureki O, Gati C, Shukla AK 10.1101/2025.05.26.656101 2025-11-26
Gi/o αi1 Human DN Gαi1; Gβ1-HiBiT C-term fusion 64 β1 Human γ2 Human Cryo-EM 9UPU - 2.8 CXCR4 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human BRIL - LgBiT
HiBiT 		SDV1a
Peptide Agonist CXCL12ε (Human), CXCL12 (Mouse), CXCL12δ (Human), CXCL12α (Human), CXCL12β (Human), CXCL12φ (Human), CXCL12γ (Human) Peptide Sang X, Jiao H, Meng Q, Fang X, Sundaram KS, Zhou J, Xu Y, Alvarado AIW, Nuryyev RL, Ourenik J, Ourednik V, Huang IS, Liu X, Mei Y, Qian T, Ciechanover A, Pizzo DP, Lane MA, Zholudeva LV, An J, Snyder EY, Hu H, Huang Z 10.1101/2025.07.08.663251 2026-04-29
Gi/o αi1 Human DN Gαi1 64 β1 Human γ2 Human Cryo-EM 9UPV - 2.7 CXCR4 CXCR4 CXCR4 Chemokine A (Rhodopsin) Human BRIL - LgBiT SDV1a
Peptide Agonist CXCL12ε (Human), CXCL12 (Mouse), CXCL12δ (Human), CXCL12α (Human), CXCL12β (Human), CXCL12φ (Human), CXCL12γ (Human) Peptide Sang X, Jiao H, Meng Q, Fang X, Sundaram KS, Zhou J, Xu Y, Alvarado AIW, Nuryyev RL, Ourenik J, Ourednik V, Huang IS, Liu X, Mei Y, Qian T, Ciechanover A, Pizzo DP, Lane MA, Zholudeva LV, An J, Snyder EY, Hu H, Huang Z 10.1101/2025.07.08.663251 2026-04-29
Gi/o αi1 Human Gi1 heterotrimer, heterologously expressed 64 β1 Rat γ2 Bovine Cryo-EM 9UWV - 3.3 OPRK OPRK1 κ Opioid A (Rhodopsin) Human - - - salvinorin A pubchem gtoplig chembl_ligand chembl_ligand pubchem chembl_ligand pubchem chembl_ligand pubchem drugbank
Small molecule Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-05-27
G12/13 α13 Human Human miniGα13: stabilizing muts/deletions 54 β1 Human γ2 Human Cryo-EM 9V0U - 3.5 AGRD1 ADGRD1 ADGRD1 ADGRD B2 (Adhesion) Human - - - - - - dihydrotestosterone Small molecule Pu X, Xi YT, Wang MX, Zhang D, Ping YQ, Xiao P, Sun JP 10.1016/J.BBRC.2025.152165 2025-07-30
Gi/o αi1 Human Gi1 heterotrimer complex 62 β1 Human γ2 Human Cryo-EM 9V6O - 2.8 OPRK OPRK1 κ Opioid A (Rhodopsin) Human BRIL - - nalfurafine pubchem gtoplig chembl_ligand drug_central drugbank
Small molecule Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide Suno-Ikeda C, Nishikawa R, Suzuki R, Yokoi S, Iwata S, Takai T, Ogura T, Hirose M, Tokuda A, Katamoto R, Inoue A, Asai E, Kise R, Sugita Y, Kato T, Nagase H, Mitsutake A, Saitoh T, Katayama K, Inoue A, Kandori H, Kobayashi T, Suno R 10.1038/S41467-025-64882-1 2025-11-19
Gi/o αo Human Wild-type human Go heterotrimer 62 β1 Human γ2 Human Cryo-EM 9VAT - 3.4 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αo Human Nucleotide-free G protein, non-canonical state 1 61 β1 Human γ2 Human Cryo-EM 9VAU - 3.0 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Human Gαi1 heterotrimer; Gβ1 His-tag 62 β1 Human γ2 Human Cryo-EM 9VAY - 3.7 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Native human Gi1 heterotrimer 62 β1 Human γ2 Human Cryo-EM 9VAZ - 3.4 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Native human Gi1 heterotrimer, non-canonical NC 62 β1 Human γ2 Human Cryo-EM 9VB0 - 3.2 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Human native Gαi1/Gβ1/Gγ2 99 β1 Human γ2 Human Cryo-EM 9VB3 - 3.0 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human - 99 β1 Human γ2 Human Cryo-EM 9VB4 - 2.9 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Native human Gi1 heterotrimer 99 β1 Human γ2 Human Cryo-EM 9VB5 - 3.1 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Wild-type human Gi1 heterotrimer 99 β1 Human γ2 Human Cryo-EM 9VB7 - 3.0 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αi1 Human Wild-type Gi1 heterotrimer 99 β1 Human γ2 Human Cryo-EM 9VBA - 3.4 NTR1 NTSR1 NTS1 Neurotensin A (Rhodopsin) Human - - - JMV449 pubchem gtoplig
Peptide Agonist large neuromedin N (Mouse), neurotensin (Human), neuromedin N (Human), large neuromedin N (Human), large neuromedin N (Rat), large neurotensin (Human), neuromedin N (Mouse) Peptide Kobayashi K, Kawakami K, Matsui TE, Yokoi S, Fukuda M, Narita TJ, Arai H, Tambo M, Sumikama T, Tatsumi M, Yamashita K, Koyanagi J, Kugawa M, Ikeda H, Sumino A, Mitsutake A, Kobilka BK, Inoue A, Kato HE 10.1038/S41586-026-10228-W 2026-06-03
Gi/o αo Human DN GoA: C3S/S47N/G204A/E246A/A326S 61 β1 Human γ2 Human Cryo-EM 9VJ5 - 2.7 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - GEPIRONE chembl_ligand pubchem drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule - - 2025-11-12
Gi/o αo Human DN GoA: C3S/S47N/G204A/E246A/A326S 61 β1 Human γ2 Human Cryo-EM 9VJE - 2.5 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - buspirone pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule Wang C, Zhang N, Shao Y, Li T, Zhang M, Gao M, Liang Y, Wang Y, Xue T, Shi Y, Chen H, Cao C 10.1016/J.CELL.2025.10.022 2025-11-12
Gi/o αi3 Human DN Gi3: S47N/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 9VJF - 2.7 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - buspirone pubchem gtoplig chembl_ligand drugbank drug_central pubchem
Small molecule Agonist (partial) 5-hydroxytryptamine Small molecule Wang C, Zhang N, Shao Y, Li T, Zhang M, Gao M, Liang Y, Wang Y, Xue T, Shi Y, Chen H, Cao C 10.1016/J.CELL.2025.10.022 2025-11-12
Gi/o αz Human Gz/Gi2 chimera; 6 DN mutations (S47N+more) 97 β1 Human γ2 Human Cryo-EM 9VJG - 2.7 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - CHEMBL26998 chembl_ligand pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule - - 2025-11-12
Gi/o αi1 Human - 63 β1 Human γ2 Human Cryo-EM 9VJT - 3.0 OPRM OPRM1 μ Opioid A (Rhodopsin) Human - - Oplophorus-luciferin 2-monooxygenase catalytic subunit (-)-methadone pubchem gtoplig chembl_ligand drugbank drug_central pubchem gtoplig chembl_ligand drug_central drugbank pubchem
Small molecule Agonist [Met]enkephalin (Human), dynorphin A-(1-8) (Human), dynorphin A (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), [Leu]enkephalin (Human), endomorphin-2 (Human) Peptide - - 2026-06-24
Gi/o αo Human DN GoA: C3S/S47N/G204A/E246A/A326S 60 β1 Human γ2 Human Cryo-EM 9VMY - 2.9 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - TMU4142 pubchem
Small molecule Agonist 5-hydroxytryptamine Small molecule - - 2025-11-12
Gi/o αo Human DN GαoA: C3S/S47N/G204A/E246A/A326S 61 β1 Human γ2 Human Cryo-EM 9VNF - 2.7 5HT1A HTR1A 5-HT1A 5-Hydroxytryptamine A (Rhodopsin) Human BRIL - - (-)-pindolol pubchem gtoplig chembl_ligand
Small molecule Agonist (partial) 5-hydroxytryptamine Small molecule - - 2025-11-12
Gi/o αi1 Human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 9VNY - 3.7 S1PR1 S1PR1 S1P1 Lysophospholipid (S1P) A (Rhodopsin) Human BRIL - - CYM5442 pubchem
Small molecule Agonist sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid - - 2026-01-28
Gi/o αi1 Human Heterotrimeric Gi protein complex 62 β1 Human γ2 Human Cryo-EM 9VPN - 4.0 APJ APLNR apelin Apelin A (Rhodopsin) Human - - - - None - apelin receptor early endogenous ligand (Mouse), apelin receptor early endogenous ligand (Human), apelin-13 (Human), apelin-17 (Human), Elabela/Toddler-11 (Human), Elabela/Toddler-21 (Human), apelin-36 (Mouse), [Pyr1]apelin-13 (Human), apelin-36 (Human), Elabela/Toddler-32 (Human) Peptide - - 2026-07-08
Gi/o αi1 Human Gi1 heterotrimer complex 61 β1 Human γ2 Human Cryo-EM 9W0M - 3.8 S1PR2 S1PR2 S1P2 Lysophospholipid (S1P) A (Rhodopsin) Human - - - - None - sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Wu Y, Chen Q, Wang H, Liu K, Wei J, Wang M, Chen K, Zhu Y, Han S, Yi C, Ma L, Schnapp G, Pautsch A, Gnamm C, Grauert M, Schmidt E, Tan Q, Wu B, Zhao Q 10.1093/PROCEL/PWAF068 2026-06-03
Gi/o αi1 Human Gi1 heterotrimer 61 β1 Human γ2 Human Cryo-EM 9W0O - 3.0 S1PR3 S1PR3 S1P3 Lysophospholipid (S1P) A (Rhodopsin) Human - - - - None - sphingosine 1-phosphate, dihydrosphingosine 1-phosphate, sphingosylphosphorylcholine Lipid Wu Y, Chen Q, Wang H, Liu K, Wei J, Wang M, Chen K, Zhu Y, Han S, Yi C, Ma L, Schnapp G, Pautsch A, Gnamm C, Grauert M, Schmidt E, Tan Q, Wu B, Zhao Q 10.1093/PROCEL/PWAF068 2026-06-03
Gi/o αi1 Human DN Gi1: S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 9W0T - 3.3 T2R46 TAS2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - - - denatonium pubchem gtoplig chembl_ligand
Small molecule Agonist - - Tan Q, Yu Y, Han X, Liu K, Han S, Wang M, Wei Y, Zhu Y, Chen Q, Ma L, Yi C, Chu X, Wu B, Zhao Q 10.1038/S41594-026-01786-8 2026-04-22
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 9W0U - 2.9 T2R46 TAS2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - - - TANGERETIN chembl_ligand pubchem
Small molecule Agonist - - - - 2026-04-22
Gi/o αi1 Human DN Gi1: 5 muts S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 9W0W - 3.2 T2R46 TAS2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - - - strychnine pubchem gtoplig chembl_ligand drug_central drugbank
Small molecule Agonist - - Tan Q, Yu Y, Han X, Liu K, Han S, Wang M, Wei Y, Zhu Y, Chen Q, Ma L, Yi C, Chu X, Wu B, Zhao Q 10.1038/S41594-026-01786-8 2026-04-22
Gi/o αi1 Human Gi1 heterotrimer complex 62 β1 Human γ2 Human Cryo-EM 9W49 - 2.9 OPRK OPRK1 κ Opioid A (Rhodopsin) Human BRIL - - U50488 pubchem gtoplig chembl_ligand
Small molecule Agonist [Met]enkephalin (Human), β-neoendorphin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), big dynorphin (Human), β-endorphin (Mouse), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2025-11-19
Gi/o αi1 Human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 9WQK - 3.7 GRM5 GRM5 mGlu5 Metabotropic glutamate C (Glutamate) Human - - - L-glutamic acid pubchem gtoplig chembl_ligand drugbank drug_central chembl_ligand pubchem pubchem drugbank
CDPPB pubchem gtoplig chembl_ligand
Small molecule
Small molecule 		Agonist
PAM 		L-glutamic acid Small molecule Lu Y, Wen T, Lu X, Zhang G, Meng T, Liu T, Wang X, Shen Y, Yang X 10.1126/SCIADV.AEE0044 2026-05-27
Gi/o αz Human Gαz/Gαi1 chimera, 7 DN mutations 63 β1 Human γ2 Human Cryo-EM 9WST - 2.8 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - LgBiT
HiBiT 		DAMGO pubchem gtoplig chembl_ligand pubchem
Peptide Agonist - - Zhang H, Wang X, Xi K, Shen Q, Xue J, Zhu Y, Zang SK, Yu T, Shen DD, Guo J, Chen LN, Ji SY, Qin J, Dong Y, Zhao M, Yang M, Wu H, Yang G, Zhang Y 10.1038/S41422-025-01191-8 2025-11-26
Gi/o αi2 Human DN Gαi2: S47N/G204A/E246A/A327S; bovine Gγ2 63 β1 Human γ2 Human Cryo-EM 9XDQ - 2.8 OPRD OPRD1 δ Opioid A (Rhodopsin) Human BRIL - LgBiT (Oplophorus-luciferin 2-monooxygenase)
HiBiT 		BMS-986187 pubchem gtoplig chembl_ligand
Small molecule Ago-PAM [Met]enkephalin (Human), dynorphin A (Human), dynorphin A-(1-8) (Human), dynorphin A-(1-13) (Human), β-endorphin (Mouse), endomorphin-1 (Human), β-endorphin (Rat), dynorphin B (Human), β-endorphin (Human), α-neoendorphin (Human), [Leu]enkephalin (Human) Peptide - - 2026-07-08
Gs αs Human - 60 β1 Human γ2 Human Cryo-EM 9XJW - 2.5 GP119 GPR119 GPR119 GPR18, GPR55 and GPR119 A (Rhodopsin) Human - Nanobody-35 - AS1269574 pubchem gtoplig chembl_ligand
Small molecule Agonist (partial) SEA, N-palmitoylethanolamine, N-oleoylethanolamide, anandamide Small molecule - - 2026-05-27
Gs αs Human Gs heterotrimer 58 β1 Human γ2 Human Cryo-EM 9XXT - 2.0 GP174 GPR174 GPR174 Orphan A (Rhodopsin) Human - Nanobody-35 - lysophosphatidylserine pubchem gtoplig chembl_ligand
Lipid Agonist lysophosphatidylserine Lipid - - 2026-04-15
Gi/o αi1 Human DN Gs: 5 muts S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 9W0P - 3.6 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human b562RIL - - CHLORHEXIDINE chembl_ligand pubchem pubchem pubchem pubchem pubchem drugbank
Small molecule Agonist - - Tan Q, Yu Y, Han X, Liu K, Han S, Wang M, Wei Y, Zhu Y, Chen Q, Ma L, Yi C, Chu X, Wu B, Zhao Q 10.1038/S41594-026-01786-8 2026-04-22
Gi/o αi1 Human DN human Gαi1: S47C/G202T +3 more mutations 61 β1 Human γ2 Human Cryo-EM 9W0Q - 3.2 T2R14 TAS2R14 TAS2R14 Taste 2 T2 (Taste 2) Human BRIL - - TANGERETIN chembl_ligand pubchem
Small molecule Agonist - - - - 2026-04-22
Gi/o αi1 Human DN Gi1: S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 9W0R - 2.7 T2R46 TAS2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - - - - None - - - Tan Q, Yu Y, Han X, Liu K, Han S, Wang M, Wei Y, Zhu Y, Chen Q, Ma L, Yi C, Chu X, Wu B, Zhao Q 10.1038/S41594-026-01786-8 2026-04-22
Gi/o αi1 Human DN Gαi1: S47C/G202T/G203A/E245A/A326S 61 β1 Human γ2 Human Cryo-EM 9W0S - 3.3 T2R46 TAS2R46 TAS2R46 Taste 2 T2 (Taste 2) Human - - - Artemisinin pubchem drugbank
Small molecule Agonist - - - - 2026-04-22
Gi/o αi1 Human - 60 β1 Human γ2 Human Cryo-EM 9WIK - 3.3 GPR84 GPR84 GPR84 Orphan A (Rhodopsin) Human BRIL - LgBiT tag DL-175 pubchem gtoplig chembl_ligand
Small molecule Agonist - - - - 2026-07-01
Gi/o αz Human Gαz/Gαi1 chimera, 7 DN muts, scFv16 63 β1 Human γ2 Human Cryo-EM 9WSW - 2.8 OPRM Oprm1 μ Opioid A (Rhodopsin) Mouse - - - endomorphin-1 (Human) pubchem gtoplig chembl_ligand
Peptide Agonist - - Zhang H, Wang X, Xi K, Shen Q, Xue J, Zhu Y, Zang SK, Yu T, Shen DD, Guo J, Chen LN, Ji SY, Qin J, Dong Y, Zhao M, Yang M, Wu H, Yang G, Zhang Y 10.1038/S41422-025-01191-8 2025-11-26
Gi/o αi3 Human DN human Gαi3: S47C/G202T/G203A/E245A/A326S 62 β1 Human γ2 Human Cryo-EM 9WXM - 3.3 GPR15 GPR15 GPR15 Orphan A (Rhodopsin) Human - - - GPR15LG
Protein Agonist - - Chen S, Han X, Zhang Y, Ma L, Yi C, Chu X, Tan Q, Han S, Zhao Q, Wu B 10.1016/J.ISCI.2025.113935 2025-11-19
Gi/o αi1 Human Human Gi1 heterotrimer 64 β1 Human γ2 Human Cryo-EM 9X20 - 3.2 GLP1R GLP1R GLP-1 Glucagon B1 (Secretin) Human - - - Glucagon-like peptide 1(7-36) pubchem
Peptide Agonist glucagon-like peptide 1-(7-37) (Human), glucagon (Human), glucagon-like peptide 1-(7-36) amide (Human) Protein Zhou Q, Li J, Zhang Y, Cai X, Han W, Yang D, Wang MW 10.1016/J.APSB.2026.01.023 2026-05-06
Gi/o αi1 Human dnGi: S47N/G203A/A326S/E245A 60 β1 Human γ2 Human Cryo-EM 9YDU - 3.2 P2Y14 P2RY14 P2Y14 P2Y A (Rhodopsin) Human - - - UDP-glucose pubchem gtoplig chembl_ligand drugbank
Small molecule Agonist UDP, UDP-galactose, UDP-glucose, UDP N-acetyl-glucosamine, UDP-glucuronic acid Small molecule Fay JF, Kousouros J, Gao ZG, Pavan M, Oliva P, Pramanik A, Meyer C, Kurma SH, Xu W, Krumm B, Jacobson KA 10.1038/S42003-025-09174-6 2025-11-19
Gi/o αi1 Human dnGi: S47N/G203A/A326S/E245A 60 β1 Human γ2 Human Cryo-EM 9YDV - 3.1 P2Y14 P2RY14 P2Y14 P2Y A (Rhodopsin) Human - - - CHEMBL1198696 chembl_ligand pubchem
Small molecule Agonist UDP, UDP-galactose, UDP-glucose, UDP N-acetyl-glucosamine, UDP-glucuronic acid Small molecule - - 2025-11-19
Gi/o αi1 Rat - 100 - - - - X-ray 1SVK - 2.0 - - - - - - - - - - - - - - Thomas CJ, Du X, Li P, Wang Y, Ross EM, Sprang SR 15128951 2004-06-01
Gi/o αi1 Rat - 100 - - - - X-ray 1AS3 - 2.4 - - - - - - - - - - - - - - Raw AS, Coleman DE, Gilman AG, Sprang SR 9398294 1997-11-12
Gi/o αi1 Rat - 100 - - - - X-ray 1GIL - 2.3 - - - - - - - - - - - - - - Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR 8073283 1995-02-14
Gi/o αi1 Rat - 100 - - - - X-ray 1BOF - 2.2 - - - - - - - - - - - - - - Coleman DE, Sprang SR 9772163 1999-01-06
Gi/o αi1 Rat - 100 - - - - X-ray 1AS2 - 2.8 - - - - - - - - - - - - - - Raw AS, Coleman DE, Gilman AG, Sprang SR 9398294 1997-11-12
Gi/o αi1 Rat - 100 - - - - X-ray 1GIA - 2.0 - - - - - - - - - - - - - - Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR 8073283 1994-09-30
Gi/o αi1 Rat - 100 - - - - X-ray 1SVS - 1.5 - - - - - - - - - - - - - - Thomas CJ, Du X, Li P, Wang Y, Ross EM, Sprang SR 15128951 2004-06-01
Gi/o αi1 Rat - 100 - - - - X-ray 3FFA - 2.3 - - - - - - - - - - - - - - Kapoor N, Menon ST, Chauhan R, Sachdev P, Sakmar TP 19703466 2009-10-06
Gi/o αi1 Rat - 100 - - - - X-ray 1AS0 - 2.0 - - - - - - - - - - - - - - Raw AS, Coleman DE, Gilman AG, Sprang SR 9398294 1997-11-12
Gi/o αi1 Rat - 100 - - - - X-ray 1GDD - 2.2 - - - - - - - - - - - - - - Mixon MB, Lee E, Coleman DE, Berghuis AM, Gilman AG, Sprang SR 7481799 1995-11-27
Gi/o αi1 Rat - 89 - - - - X-ray 1BH2 - 2.1 - - - - - - - - - - - - - - Posner BA, Mixon MB, Wall MA, Sprang SR, Gilman AG 9705312 1998-11-04
Gi/o αi1 Rat - 100 - - - - X-ray 1GFI - 2.2 - - - - - - - - - - - - - - Coleman DE, Berghuis AM, Lee E, Linder ME, Gilman AG, Sprang SR 8073283 1995-03-31
Gi/o αi1 Rat - 100 - - - - X-ray 1GIT - 2.6 - - - - - - - - - - - - - - Berghuis AM, Lee E, Raw AS, Gilman AG, Sprang SR 8939752 1997-02-12
Gi/o αi1 Rat - 100 - - - - X-ray 3FFB - 2.6 - - - - - - - - - - - - - - Kapoor N, Menon ST, Chauhan R, Sachdev P, Sakmar TP 19703466 2009-10-06
Gi/o αi1 Rat - 100 - - - - X-ray 1CIP - 1.5 - - - - - - - - - - - - - - Coleman DE, Sprang SR 10358003 1999-04-09
Gi/o αi1 Rat - 100 - - - - X-ray 2ZJZ - 2.6 - - - - - - - - - - - - - - - - 2009-03-24
Gi/o αi1 Rat - 100 - - - - X-ray 4N0D - 1.6 - - - - - - - - - - - - - - Thaker TM, Sarwar M, Preininger AM, Hamm HE, Iverson TM 24596087 2014-03-12
Gi/o αi1 Rat - 100 - - - - X-ray 3V00 - 2.9 - - - - - - - - - - - - - - Singh G, Ramachandran S, Cerione RA 22448927 2012-04-18
Gi/o αi1 Rat - 100 - - - - X-ray 3D7M - 2.9 - - - - - - - - - - - - - - Preininger AM, Funk MA, Oldham WM, Meier SM, Johnston CA, Adhikary S, Kimple AJ, Siderovski DP, Hamm HE, Iverson TM 19222191 2009-03-03
Gs αl Mouse - 100 - - - - X-ray 8HTG - 2.9 - - - - - - - - - - - - - - Choi C, Bae J, Kim S, Lee S, Kang H, Kim J, Bang I, Kim K, Huh WK, Seok C, Park H, Im W, Choi HJ 38062020 2023-12-20
Gi/o αi1 Rat - 100 β1 Bovine γ2 Bovine X-ray 1GG2 - 2.4 - - - - - - - - - - - - - - Wall MA, Coleman DE, Lee E, Iniguez-Lluhi JA, Posner BA, Gilman AG, Sprang SR 8521505 1997-02-12
Gi/o αi1 Rat - 92 - - - - X-ray 1FQK - 2.3 - - - - - - - - Regulator of G-protein signaling 9 - - - - - Slep KC, Kercher MA, He W, Cowan CW, Wensel TG, Sigler PB 11234020 2001-02-28
Gi/o αi1 Rat - 96 - - - - X-ray 1SHZ - 2.9 - - - - - - - - Guanine Nucleotide-Binding Protein Galpha(13):Galpha(i1) Chimera
Rho guanine nucleotide exchange factor 1 		- - - - - Chen Z, Singer WD, Sternweis PC, Sprang SR 15665872 2005-01-18
Gi/o αi1 Rat - 100 β1 Bovine γ2 Bovine X-ray 1GP2 - 2.3 - - - - - - - - - - - - - - Wall MA, Coleman DE, Lee E, Iniguez-Lluhi JA, Posner BA, Gilman AG, Sprang SR 8521505 1997-02-12
Gi/o αi1 Rat - 100 - - - - X-ray 1AGR - 2.8 - - - - - - - - RGS4 - - - - - Tesmer JJ, Berman DM, Gilman AG, Sprang SR 9108480 1997-06-16
Gi/o αi1 Rat - 100 - - - - X-ray 2RGN - 3.5 - - - - - - - - Rho guanine nucleotide exchange factor 25
Transforming protein RhoA 		- - - - - Lutz S, Shankaranarayanan A, Coco C, Ridilla M, Nance MR, Vettel C, Baltus D, Evelyn CR, Neubig RR, Wieland T, Tesmer JJ 18096806 2008-01-15
Gs αl Human - 100 - - - - Cryo-EM 8EL8 - 3.2 - - - - - - - - Isoform 1 of Synembryn-B - - - - - Papasergi-Scott MM, Kwarcinski FE, Yu M, Panova O, Ovrutsky AM, Skiniotis G, Tall GG 36931277 2023-03-01
Gi/o αi1 Rat - 100 - - - - X-ray 4N0E - 2.1 - - - - - - - - - - - - - - Thaker TM, Sarwar M, Preininger AM, Hamm HE, Iverson TM 24596087 2014-03-12
Gi/o αi1 Rat - 100 - - - - X-ray 2ZJY - 2.8 - - - - - - - - - - - - - - - - 2009-03-24
Gi/o αi1 Rat - 100 β1 Bovine γ2 Bovine X-ray 3AH8 - 2.9 - - - - - - - - YM-254890 - - - - - Nishimura A, Kitano K, Takasaki J, Taniguchi M, Mizuno N, Tago K, Hakoshima T, Itoh H 20639466 2010-07-21
Gi/o αi1 Rat - 92 - - - - X-ray 1FQJ - 2.0 - - - - - - - - Regulator of G-protein signaling 9 - - - - - Slep KC, Kercher MA, He W, Cowan CW, Wensel TG, Sigler PB 11234020 2001-02-28
Gi/o αi1 Rat - 100 β1 Bovine γ2 Bovine X-ray 2BCJ - 3.1 - - - - - - - - G-protein-coupled receptor kinase 2 - - - - - Tesmer VM, Kawano T, Shankaranarayanan A, Kozasa T, Tesmer JJ 16339447 2005-12-20
Gi/o αi1 Rat - 100 - - - - X-ray 4PAO - 2.0 - - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 25037222 2014-07-30
Gi/o αi1 Rat - 100 - - - - X-ray 6M8H - 2.1 - - - - - - - - - - - - - - - - 2019-08-21
Gi/o αi1 Rat - 100 - - - - X-ray 4PAM - 2.1 - - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 25037222 2014-07-30
Gi/o αi1 Rat - 100 - - - - X-ray 4PAQ - 2.0 - - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 25037222 2014-07-30
Gi/o αi1 Rat - 100 - - - - X-ray 4PAN - 2.4 - - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 25037222 2014-07-30
Gi/o αi1 Rat - 100 - - - - X-ray 5KDL - 2.7 - - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 27462082 2016-08-03
Gs αs2 Bovine - 100 - - - - X-ray 1AZT - 2.3 - - - - - - - - - - - - - - Sunahara RK, Tesmer JJ, Gilman AG, Sprang SR 9395396 1998-02-25
Gi/o αi1 Rat - 100 β1 Bovine γT1 Bovine X-ray 5KDO - 1.9 - - - - - - - - - - - - - - Kaya AI, Lokits AD, Gilbert JA, Iverson TM, Meiler J, Hamm HE 27462082 2016-08-03
Gs αs2 Bovine - 100 - - - - X-ray 1AZS - 2.3 - - - - - - - - VC1
IIC2 		- - - - - Tesmer JJ, Sunahara RK, Gilman AG, Sprang SR 9417641 1998-02-25
Gs αs2 Bovine - 100 - - - - X-ray 1CJK - 3.0 - - - - - - - - Adenylate cyclase
type V
ADENYLATE CYCLASE
TYPE II 		- - - - - Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR 10427002 1999-08-31
Gs αs2 Bovine - 100 - - - - Cryo-EM 6R4O - 4.2 - - - - - - - - Adenylate cyclase 9 - - - - - Qi C, Sorrentino S, Medalia O, Korkhov VM 31023924 2019-05-08
Gs αs2 Bovine - 100 - - - - X-ray 1CJU - 2.8 - - - - - - - - Adenylate cyclase
type V
ADENYLATE CYCLASE
TYPE II 		- - - - - Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR 10427002 1999-08-31
Gs αs2 Bovine - 100 - - - - Cryo-EM 6R3Q - 3.4 - - - - - - - - Adenylate cyclase 9 - - - - - Qi C, Sorrentino S, Medalia O, Korkhov VM 31023924 2019-05-08
Gs αs2 Human - 96 - - - - X-ray 6AU6 - 1.7 - - - - - - - - - - - - - - Hu Q, Shokat KM 29628140 2018-05-09
Gs αs2 Bovine - 100 - - - - X-ray 1CJT - 2.8 - - - - - - - - Adenylate cyclase
type V
ADENYLATE CYCLASE
TYPE II 		- - - - - Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR 10427002 1999-08-31
Gs αs2 Bovine - 100 - - - - X-ray 1TL7 - 2.8 - - - - - - - - Adenylate cyclase
type V
Adenylate cyclase
type II 		- - - - - Mou TC, Gille A, Fancy DA, Seifert R, Sprang SR 15591060 2004-12-14
Gs αs2 Bovine - 100 - - - - X-ray 1CJV - 3.0 - - - - - - - - Adenylate cyclase
type V
ADENYLATE CYCLASE
TYPE II 		- - - - - Tesmer JJ, Sunahara RK, Johnson RA, Gosselin G, Gilman AG, Sprang SR 10427002 1999-08-31
Gs αs2 Bovine - 96 - - - - X-ray 1CUL - 2.4 - - - - - - - - TYPE V ADENYLYL CYCLASE
TYPE II ADENYLYL CYCLASE 		- - - - - Tesmer JJ, Dessauer CW, Sunahara RK, Murray LD, Johnson RA, Gilman AG, Sprang SR 11087399 2001-01-10
Gs αs2 Bovine - 100 - - - - X-ray 1CS4 - 2.5 - - - - - - - - TYPE V ADENYLATE CYCLASE
TYPE II ADENYLATE CYCLASE 		- - - - - Tesmer JJ, Dessauer CW, Sunahara RK, Murray LD, Johnson RA, Gilman AG, Sprang SR 11087399 2001-01-10
Gs αs2 Bovine - 100 - - - - Cryo-EM 7PDE - 4.5 - - - - - - - - Adenylate cyclase 9 - - - - - Qi C, Lavriha P, Mehta V, Khanppnavar B, Mohammed I, Li Y, Lazaratos M, Schaefer JV, Dreier B, Pluckthun A, Bondar AN, Dessauer CW, Korkhov VM 35210418 2022-01-19
Gs αs2 Bovine - 100 - - - - X-ray 1U0H - 2.9 - - - - - - - - Adenylate cyclase
type V
Adenylate cyclase
type II 		- - - - - Mou TC, Gille A, Fancy DA, Seifert R, Sprang SR 15591060 2004-12-14
Gs αs2 Bovine - 100 - - - - X-ray 3C16 - 2.9 - - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Masada N, Cooper DM, Sprang SR 19243146 2009-02-03
Gs αs2 Bovine - 100 - - - - Cryo-EM 6R4P - 3.1 - - - - - - - - Adenylate cyclase 9 - - - - - Qi C, Sorrentino S, Medalia O, Korkhov VM 31023924 2019-05-08
Gs αs2 Bovine - 100 - - - - X-ray 3C14 - 2.7 - - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Masada N, Cooper DM, Sprang SR 19243146 2009-02-03
Gs αs2 Bovine - 100 - - - - X-ray 2GVZ - 3.3 - - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Gille A, Suryanarayana S, Richter M, Seifert R, Sprang SR 16766715 2006-07-04
Gs αs2 Bovine - 100 - - - - X-ray 3G82 - 3.1 - - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - - - 2010-02-16
Gs αs2 Bovine - 100 - - - - X-ray 2GVD - 2.9 - - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Gille A, Suryanarayana S, Richter M, Seifert R, Sprang SR 16766715 2006-07-04
Gs αs2 Bovine - 100 - - - - Cryo-EM 8BUZ - 3.5 - - - - - - - - Adenylate cyclase type 8 - - - - - Khanppnavar B, Schuster D, Lavriha P, Uliana F, Ozel M, Mehta V, Leitner A, Picotti P, Korkhov VM 38351373 2023-12-13
Gi/o αi1 Rat - 91 - - - - Cryo-EM 6UKT - 3.9 - - - - - - - NB8109
NB8117
NB8119
NB9156 		Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) - - - - - McClelland LJ, Zhang K, Mou TC, Johnston J, Yates-Hansen C, Li S, Thomas CJ, Doukov TI, Triest S, Wohlkonig A, Tall GG, Steyaert J, Chiu W, Sprang SR 32103024 2020-03-11
Gs αs2 Bovine - 100 - - - - Cryo-EM 7PDF - 3.8 - - - - - - - - Adenylate cyclase 9 - - - - - Qi C, Lavriha P, Mehta V, Khanppnavar B, Mohammed I, Li Y, Lazaratos M, Schaefer JV, Dreier B, Pluckthun A, Bondar AN, Dessauer CW, Korkhov VM 35210418 2022-01-26
Gs αs2 Bovine - 100 - - - - X-ray 3MAA - 3.0 - - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Masada N, Cooper DM, Sprang SR 19243146 2010-04-07
Gi/o αi1 Rat - 100 - - - - X-ray 6TYL - 3.3 - - - - - - - Nanobody A
Nanobody B
Nanobody C 		Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) - - - - - McClelland LJ, Zhang K, Mou TC, Johnston J, Yates-Hansen C, Li S, Thomas CJ, Doukov TI, Triest S, Wohlkonig A, Tall GG, Steyaert J, Chiu W, Sprang SR 32103024 2020-03-11
Gs αs2 Human - 88 - - - - X-ray 7E5E - 2.0 - - - - - - - - GD20 - - - - - Dai SA, Hu Q, Gao R, Blythe EE, Touhara KK, Peacock H, Zhang Z, von Zastrow M, Suga H, Shokat KM 36170854 2022-03-02
Gs αs2 Bovine - 100 - - - - Cryo-EM 8BV5 - 3.5 - - - - - - - - Adenylate cyclase type 8 - - - - - Khanppnavar B, Schuster D, Lavriha P, Uliana F, Ozel M, Mehta V, Leitner A, Picotti P, Korkhov VM 38351373 2024-01-17
Gs αs2 Bovine - 100 - - - - X-ray 3C15 - 2.8 - - - - - - - - Adenylate cyclase type 5
Adenylate cyclase type 2 		- - - - - Mou TC, Masada N, Cooper DM, Sprang SR 19243146 2009-02-03
Gs αs2 Human - 96 - - - - X-ray 7BPH - 1.6 - - - - - - - - GN13 - - - - - Dai SA, Hu Q, Gao R, Blythe EE, Touhara KK, Peacock H, Zhang Z, von Zastrow M, Suga H, Shokat KM 36170854 2021-03-31
Gs αs2 Human - 96 - - - - Cryo-EM 8EL7 - 2.8 - - - - - - - - Isoform 1 of Synembryn-B - - - - - Papasergi-Scott MM, Kwarcinski FE, Yu M, Panova O, Ovrutsky AM, Skiniotis G, Tall GG 36931277 2023-03-01
Gs αs2 Human - 97 β1 Human γ2 Human X-ray 6EG8 - 2.8 - - - - - - - - - - - - - - Liu X, Xu X, Hilger D, Aschauer P, Tiemann JKS, Du Y, Liu H, Hirata K, Sun X, Guixa-Gonzalez R, Mathiesen JM, Hildebrand PW, Kobilka BK 31080070 2019-06-05
Gs αs2 Human - 100 - - - - Cryo-EM 9U3P - 2.7 - - - - - - - - Adenylate cyclase type 9
Protein M2-1 		- - - - - Nomura R, Suzuki S, Nishikawa K, Suzuki H, Fujiyoshi Y 40466787 2025-06-11
Gi/o αi1 Human - 100 - - - - X-ray 3UMS - 2.3 - - - - - - - - - - - - - - - - 2012-02-08
Gi/o αi1 Human - 88 - - - - X-ray 2G83 - 2.8 - - - - - - - - KB-1753 phage display peptide - - - - - Johnston CA, Lobanova ES, Shavkunov AS, Low J, Ramer JK, Blaesius R, Fredericks Z, Willard FS, Kuhlman B, Arshavsky VY, Siderovski DP 16981699 2006-10-10
Gi/o αi1 Human - 100 - - - - X-ray 3UMR - 2.0 - - - - - - - - - - - - - - - - 2012-10-24
Gi/o αi1 Human - 92 - - - - X-ray 1KJY - 2.7 - - - - - - - - Regulator of G-protein signaling 14 - - - - - Kimple RJ, Kimple ME, Betts L, Sondek J, Siderovski DP 11976690 2002-05-08
Gi/o αi1 Human - 93 - - - - X-ray 1Y3A - 2.5 - - - - - - - - KB752 peptide - - - - - Johnston CA, Willard FS, Jezyk MR, Fredericks Z, Bodor ET, Jones MB, Blaesius R, Watts VJ, Harden TK, Sondek J, Ramer JK, Siderovski DP 16004878 2005-07-12
Gi/o αi1 Human - 91 - - - - X-ray 2GTP - 2.6 - - - - - - - - Regulator of G-protein signaling 1 - - - - - Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP 18434541 2006-05-23
Gi/o αi1 Human - 93 - - - - X-ray 3QI2 - 2.8 - - - - - - - - Regulator of G-protein signaling 14 - - - - - Bosch DE, Willard FS, Ramanujam R, Kimple AJ, Willard MD, Naqvi NI, Siderovski DP 22383884 2012-02-01
Gi/o αi1 Human - 92 - - - - X-ray 2OM2 - 2.2 - - - - - - - - Regulator of G-protein signalling 14 GoLoco motif peptide - - - - - Sammond DW, Eletr ZM, Purbeck C, Kimple RJ, Siderovski DP, Kuhlman B 17603074 2007-07-10
Gi/o αi1 Human - 100 - - - - Cryo-EM 6VU8 - 4.1 - - - - - - - - Resistance to inhibitors of cholinesterase 8 homolog A (C. elegans) - - - - - Seven AB, Hilger D, Papasergi-Scott MM, Zhang L, Qu Q, Kobilka BK, Tall GG, Skiniotis G 32126208 2020-03-18
Gi/o αi1 Human - 92 - - - - X-ray 2IK8 - 2.7 - - - - - - - - Regulator of G-protein signaling 16 - - - - - Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP 18434541 2006-11-21
Gi/o αi1 Human - 92 - - - - X-ray 2XNS - 3.4 - - - - - - - - Regulator of G-protein signaling 14 - - - - - Sammond DW, Bosch DE, Butterfoss GL, Purbeck C, Machius M, Siderovski DP, Kuhlman B 21388199 2011-06-08
Gi/o αi1 Human - 93 - - - - X-ray 3ONW - 2.4 - - - - - - - - Regulator of G-protein signaling 14 - - - - - Bosch DE, Kimple AJ, Sammond DW, Muller RE, Miley MJ, Machius M, Kuhlman B, Willard FS, Siderovski DP 21115486 2010-11-24
Gi/o αi1 Human - 92 - - - - X-ray 3QE0 - 3.0 - - - - - - - - KB752 peptide - - - - - Bosch DE, Willard FS, Ramanujam R, Kimple AJ, Willard MD, Naqvi NI, Siderovski DP 22383884 2012-01-25
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 9ODO - 3.8 - - - - - - - - - - - - - - - - 2026-03-04
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 9ODI - 3.7 - - - - - - - - - - - - - - Robertson MJ, Modak A, Papasergi-Scott MM, Hu M, Peroto MC, Varga BR, Majumdar S, Kalathur R, Blanchard SC, Skiniotis G 41430437 2026-03-04
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 9ODH - 3.8 - - - - - - - - - - - - - - Robertson MJ, Modak A, Papasergi-Scott MM, Hu M, Peroto MC, Varga BR, Majumdar S, Kalathur R, Blanchard SC, Skiniotis G 41430437 2026-03-04
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 9ODP - 4.3 - - - - - - - - - - - - - - - - 2026-03-04
Gi/o αi1 Human - 93 - - - - X-ray 4G5Q - 2.9 - - - - - - - - G-protein-signaling modulator 2 - - - - - Jia M, Li J, Zhu J, Wen W, Zhang M, Wang W 22952234 2012-09-05
Gi/o αi1 Human - 100 β1 Rat γ2 Bovine X-ray 5TDH - 3.0 - - - - - - - - - - - - - - Liu P, Jia MZ, Zhou XE, De Waal PW, Dickson BM, Liu B, Hou L, Yin YT, Kang YY, Shi Y, Melcher K, Xu HE, Jiang Y 27498775 2016-11-09
Gi/o αi1 Human - 100 β1 Human γ2 Human X-ray 6CRK - 2.0 - - - - - - - single-chain Fv - - - - - - Maeda S, Koehl A, Matile H, Hu H, Hilger D, Schertler GFX, Manglik A, Skiniotis G, Dawson RJP, Kobilka BK 30213947 2018-10-24
Gi/o αt1 Bovine - 93 - - - - X-ray 1TAG - 1.8 - - - - - - - - - - - - - - Lambright DG, Noel JP, Hamm HE, Sigler PB 8208289 1995-02-07
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 7RKX - 3.1 - - - - - - - Antibody fragment scFv16 G-protein coupled receptor homolog US27 - - - - - - - 2022-01-26
Gi/o αi3 Mouse - 100 - - - - X-ray 3AB3 - 2.4 - - - - - - - - Rho guanine nucleotide exchange factor 1 - - - - - Hajicek N, Kukimoto-Niino M, Mishima-Tsumagari C, Chow CR, Shirouzu M, Terada T, Patel M, Yokoyama S, Kozasa T 21507947 2010-12-29
Gi/o αt1 Bovine - 93 - - - - X-ray 1TAD - 1.7 - - - - - - - - - - - - - - Sondek J, Lambright DG, Noel JP, Hamm HE, Sigler PB 7969474 1995-05-08
Gi/o αi1 Human - 100 β1 Human γ2 Human Cryo-EM 7RKY - 3.8 - - - - - - - Antibody fragment scFv16 G-protein coupled receptor homolog US27 - - - - - - - 2022-01-26
Gi/o αt1 Bovine - 93 - - - - X-ray 1TND - 2.2 - - - - - - - - - - - - - - Noel JP, Hamm HE, Sigler PB 8259210 1994-07-31
Gi/o αi3 Rat - 99 - - - - X-ray 6MHF - 2.0 - - - - - - - - Girdin - - - - - Kalogriopoulos NA, Rees SD, Ngo T, Kopcho NJ, Ilatovskiy AV, Sun N, Komives EA, Chang G, Ghosh P, Kufareva I 31363053 2019-07-31
Gi/o αi3 Rat - 99 - - - - X-ray 6MHE - 2.2 - - - - - - - - KB752 peptide - - - - - Kalogriopoulos NA, Rees SD, Ngo T, Kopcho NJ, Ilatovskiy AV, Sun N, Komives EA, Chang G, Ghosh P, Kufareva I 31363053 2019-07-31
Gi/o αi3 Human - 91 - - - - X-ray 2IHB - 2.7 - - - - - - - - Regulator of G-protein signalling 10 - - - - - Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP 18434541 2006-11-21
Gi/o αi3 Human - 91 - - - - X-ray 8OY1 - 3.3 - - - - - - - - - - - - - - Ferreras-Gutierrez M, Minguez-Toral M, Ibanez de Opakua A, Martin-Santamaria S, Garcia-Marcos M, Medrano FJ, Blanco FJ 39706421 2024-05-15
Gq/11 α11 Human - 98 β1 Human γ2 Human X-ray 8QEG - 1.7 - - - - - - - - - - - - - - Muhle J, Alenfelder J, Rodrigues MJ, Jurgenliemke L, Guixa-Gonzalez R, Gratz L, Andres F, Bacchin A, Hennig M, Schihada H, Crusemann M, Konig GM, Schertler G, Kostenis E, Deupi X 40333756 2025-03-19
Gi/o αt1 Human - 3 - - - - X-ray 3RBQ - 2.0 - - - - - - - - Protein unc-119 homolog A - - - - - Zhang H, Constantine R, Vorobiev S, Chen Y, Seetharaman J, Huang YJ, Xiao R, Montelione GT, Gerstner CD, Davis MW, Inana G, Whitby FG, Jorgensen EM, Hill CP, Tong L, Baehr W 21642972 2011-06-08
Gq/11 αq Human - 100 - - - - Cryo-EM 6VU5 - 3.5 - - - - - - - - Resistance to inhibitors of cholinesterase-8A (Ric-8A) - - - - - Seven AB, Hilger D, Papasergi-Scott MM, Zhang L, Qu Q, Kobilka BK, Tall GG, Skiniotis G 32126208 2020-03-18
Gi/o αt1 Bovine - 100 β1 Bovine γT1 Bovine X-ray 1GOT - 2.0 - - - - - - - - - - - - - - Lambright DG, Sondek J, Bohm A, Skiba NP, Hamm HE, Sigler PB 8552184 1997-03-12
Gq/11 αq Human - 98 - - - - Cryo-EM 8JPE - 2.9 - - - - - - - - - - - - - - Duan J, Liu H, Zhao F, Yuan Q, Ji Y, Cai X, He X, Li X, Li J, Wu K, Gao T, Zhu S, Lin S, Wang MW, Cheng X, Yin W, Jiang Y, Yang D, Xu HE 37532940 2023-08-09
Gi/o αi3 Human - 99 - - - - X-ray 2ODE - 1.9 - - - - - - - - Regulator of G-protein signaling 8 - - - - - Soundararajan M, Willard FS, Kimple AJ, Turnbull AP, Ball LJ, Schoch GA, Gileadi C, Fedorov OY, Dowler EF, Higman VA, Hutsell SQ, Sundstrom M, Doyle DA, Siderovski DP 18434541 2007-02-06
Gq/11 αq Human - 99 - - - - Cryo-EM 8UQN - 3.4 - - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Falzone ME, MacKinnon R 37991948 2023-12-06
Gi/o αi3 Human - 99 - - - - X-ray 2V4Z - 2.8 - - - - - - - - REGULATOR OF G-PROTEIN SIGNALING 2 - - - - - Kimple AJ, Soundararajan M, Hutsell SQ, Roos AK, Urban DJ, Setola V, Temple BR, Roth BL, Knapp S, Willard FS, Siderovski DP 19478087 2008-11-04
Gq/11 αq Human - 99 β1 Human γ2 Human Cryo-EM 8UQO - 3.4 - - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Falzone ME, MacKinnon R 37991948 2023-12-06
Gi/o αt2 Human - 100 - - - - X-ray 6N84 - 1.8 - - - - - - - - - - - - - - Srivastava D, Gakhar L, Artemyev NO 31300652 2019-07-10
G12/13 α12 Mouse - 95 - - - - X-ray 1ZCA - 2.9 - - - - - - - - - - - - - - Kreutz B, Yau DM, Nance MR, Tanabe S, Tesmer JJ, Kozasa T 16388592 2005-11-15
Gi/o αi3 Human - 93 - - - - X-ray 4G5S - 3.6 - - - - - - - - G-protein-signaling modulator 2 - - - - - Jia M, Li J, Zhu J, Wen W, Zhang M, Wang W 22952234 2012-09-05
Gi/o αi3 Human - 93 - - - - X-ray 4G5O - 2.9 - - - - - - - - G-protein-signaling modulator 2 - - - - - Jia M, Li J, Zhu J, Wen W, Zhang M, Wang W 22952234 2012-09-05
G12/13 α13 Mouse - 96 - - - - X-ray 1ZCB - 2.0 - - - - - - - - - - - - - - Kreutz B, Yau DM, Nance MR, Tanabe S, Tesmer JJ, Kozasa T 16388592 2005-11-15
Gi/o αi3 Human - 93 - - - - X-ray 4G5R - 3.5 - - - - - - - - G-protein-signaling modulator 2 - - - - - Jia M, Li J, Zhu J, Wen W, Zhang M, Wang W 22952234 2012-09-05
G12/13 α13 Mouse - 90 - - - - X-ray 3CX6 - 2.5 - - - - - - - - Rho guanine nucleotide exchange factor 11 - - - - - Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR 18940608 2008-10-28
Gi/o αi3 Human - 100 - - - - Cryo-EM 8GVX - 3.9 - - - - - - - - Short transient receptor potential channel 5 - - - - - Won J, Kim J, Jeong H, Kim J, Feng S, Jeong B, Kwak M, Ko J, Im W, So I, Lee HH 37137991 2023-05-24
G12/13 α13 Mouse - 90 - - - - X-ray 3CX7 - 2.3 - - - - - - - - Glutamate Transporter Associated Protein 48 - - - - - Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR 18940608 2008-10-28
Gi/o αo Mouse - 94 - - - - X-ray 3C7K - 2.9 - - - - - - - - Regulator of G-protein signaling 16 - - - - - Slep KC, Kercher MA, Wieland T, Chen CK, Simon MI, Sigler PB 18434540 2008-05-06
G12/13 α13 Mouse - 90 - - - - X-ray 3CX8 - 2.0 - - - - - - - - Rho guanine nucleotide exchange factor 11 - - - - - Chen Z, Singer WD, Danesh SM, Sternweis PC, Sprang SR 18940608 2008-10-28
Gi/o αi3 Human - 100 - - - - Cryo-EM 7X6I - 3.9 - - - - - - - - Short transient receptor potential channel 5 - - - - - Won J, Kim J, Jeong H, Kim J, Feng S, Jeong B, Kwak M, Ko J, Im W, So I, Lee HH 37137991 2023-04-26
Gi/o αt1 Bovine - 100 - - - - Cryo-EM 7JSN - 3.2 - - - - - - - - Rod cGMP-specific 3'
5'-cyclic phosphodiesterase subunit alpha
Rod cGMP-specific 3'
5'-cyclic phosphodiesterase subunit beta 		- - - - - Gao Y, Eskici G, Ramachandran S, Poitevin F, Seven AB, Panova O, Skiniotis G, Cerione RA 33007200 2020-10-21
Gi/o αt2 Human - 100 - - - - X-ray 6N85 - 2.5 - - - - - - - - Synembryn-A - - - - - Srivastava D, Gakhar L, Artemyev NO 31300652 2019-07-10
Gi/o αo Human - 64 β1 Human γ2 Human Cryo-EM 8IEC - 3.2 - - - - - - - Single-chain variable fragment scFv16 - - - - - - Shin J, Park J, Jeong J, Lam JH, Qiu X, Wu D, Kim K, Lee JY, Robinson CV, Hyun J, Katritch V, Kim KP, Cho Y 38332368 2024-02-14
Gq/11 α11 Human - 100 β1 Human γ2 Human Cryo-EM 9P8A - 3.7 - - - - - - - - - - - - - - Vo AA, Modak A, Lu S, Blanchard SC, Lambert NA, Robertson MJ 41813894 2026-03-25
Gq/11 αq Mouse - 97 - - - - X-ray 4EKC - 7.4 - - - - - - - - Regulator of G-protein signaling 2 - - - - - Nance MR, Kreutz B, Tesmer VM, Sterne-Marr R, Kozasa T, Tesmer JJ 23434405 2013-01-30
Gq/11 αq Mouse - 97 - - - - X-ray 4EKD - 2.7 - - - - - - - - Regulator of G-protein signaling 2 - - - - - Nance MR, Kreutz B, Tesmer VM, Sterne-Marr R, Kozasa T, Tesmer JJ 23434405 2013-01-30
Gq/11 αq Mouse - 100 - - - - X-ray 4QJ4 - 3.3 - - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Lyon AM, Begley JA, Manett TD, Tesmer JJG 25435326 2014-10-22
Gq/11 αq Mouse - 91 - - - - X-ray 7SQ2 - 2.6 - - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Waldo GL, Ricks TK, Hicks SN, Cheever ML, Kawano T, Tsuboi K, Wang X, Montell C, Kozasa T, Sondek J, Harden TK 20966218 2021-11-17
Gq/11 αq Mouse - 100 - - - - X-ray 4QJ5 - 3.4 - - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Lyon AM, Begley JA, Manett TD, Tesmer JJG 25435326 2014-10-22
Gq/11 αq Mouse - 87 - - - - X-ray 5DO9 - 2.6 - - - - - - - - Regulator of G-protein signaling 8 - - - - - Taylor VG, Bommarito PA, Tesmer JJ 26755720 2016-01-20
Gq/11 α11 Human - 98 β1 Human γ2 Human X-ray 8QEH - 1.4 - - - - - - - - - - - - - - Muhle J, Alenfelder J, Rodrigues MJ, Jurgenliemke L, Guixa-Gonzalez R, Gratz L, Andres F, Bacchin A, Hennig M, Schihada H, Crusemann M, Konig GM, Schertler G, Kostenis E, Deupi X 40333756 2025-03-19
Gq/11 αq Mouse - 100 - - - - X-ray 4QJ3 - 3.0 - - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Lyon AM, Begley JA, Manett TD, Tesmer JJG 25435326 2014-10-22
Gq/11 αq Mouse - 98 - - - - X-ray 4GNK - 4.0 - - - - - - - - 1-phosphatidylinositol 4
5-bisphosphate phosphodiesterase beta-3 		- - - - - Lyon AM, Dutta S, Boguth CA, Skiniotis G, Tesmer JJ 23377541 2013-02-06