tretinoin [Ligand Id: 2644] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL38 (Aberel, Acticin, All-trans retinoic acid, All-trans-retinoic acid, Altreno, Atralin, Avita, Eudyna, Kerlocal, NSC-122758, Oristar rna, Renova, Retin a, Retin-a, Retin-a micro, Retin-a-micro, Retinoic acid, Tretinoin, Tretinoina, Tretinoine, Tretin-X, Vesanoid) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 5.53 | pKi | 2982 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 5.28 | pIC50 | 5275 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| synuclein alpha/Alpha-synuclein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6152] [GtoPdb: 3285] [UniProtKB: P37840] | ||||||||
| ChEMBL | Inhibition of alpha-synuclein fibril formation (unknown origin) incubated for 24 hrs to 7 days by thioflavin S based fluorescence assay | B | 5.52 | pIC50 | 3000 | nM | IC50 | Eur J Med Chem (2019) 167: 10-36 [PMID:30743095] |
| Amyloid-beta A4 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2487] [UniProtKB: P05067] | ||||||||
| ChEMBL | Inhibition of amyloid beta (1 to 40) (unknown origin) incubated for 24 hrs to 7 days by thioflavin S based fluorescence assay | B | 6.74 | pIC50 | 180 | nM | IC50 | Eur J Med Chem (2019) 167: 10-36 [PMID:30743095] |
| Cellular retinoic acid-binding protein I in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4945] [UniProtKB: P40220] | ||||||||
| ChEMBL | Inhibition of [3H]ATRA binding to chick skin Cytoplasmic retinoic acid binding protein | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (1996) 39: 3625-3635 [PMID:8809153] |
| ChEMBL | Inhibition of binding to chick skin Cytoplasmic retinoic acid binding protein | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (1995) 38: 2302-2310 [PMID:7608895] |
| ChEMBL | Tested for its ability to inhibit the binding of (all-E-)-RA to cytoplasmic retinoic acid-binding protein (CRABP) from chick skin | B | 6.43 | pIC50 | 370 | nM | IC50 | J Med Chem (1994) 37: 4499-4507 [PMID:7799400] |
| cellular retinoic acid binding protein 1/Cellular retinoic acid-binding protein I in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3208] [GtoPdb: 2529] [UniProtKB: P62965] | ||||||||
| ChEMBL | Inhibition of [3H]ATRA binding to murine Cytoplasmic retinoic acid binding protein (CRABP) type 1 | B | 9.4 | pKd | 0.4 | nM | Kd | J Med Chem (1996) 39: 3625-3635 [PMID:8809153] |
| ChEMBL | Binding affinity for mouse Cytoplasmic retinoic acid binding protein type 1 | B | 9.4 | pKd | 0.4 | nM | Kd | J Med Chem (1995) 38: 2302-2310 [PMID:7608895] |
| cellular retinoic acid binding protein 2/Cellular retinoic acid-binding protein II in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4172] [GtoPdb: 2530] [UniProtKB: P22935] | ||||||||
| ChEMBL | Inhibition of [3H]ATRA binding to murine Cytoplasmic retinoic acid binding protein (CRABP) type 2 | B | 8.7 | pKd | 2 | nM | Kd | J Med Chem (1996) 39: 3625-3635 [PMID:8809153] |
| ChEMBL | Binding affinity for mouse Cytoplasmic retinoic acid binding protein type 2 | B | 8.7 | pKd | 2 | nM | Kd | J Med Chem (1995) 38: 2302-2310 [PMID:7608895] |
| GroEL/GroES in Escherichia coli (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106139] [UniProtKB: Q548M1, Q7BGE6] | ||||||||
| ChEMBL | Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding by measuring rhodanese enzyme activity after 45 mins by Fe(SCN)3 dye based spectrometric analysis | B | 4.68 | pIC50 | 21000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084] |
| ChEMBL | Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 20 to 40 mins by malachite green dye based spectrometric analysis | B | 5.17 | pIC50 | 6700 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084] |
| HSP60/HSP10 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106131] [UniProtKB: P10809, P61604] | ||||||||
| ChEMBL | Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 40 to 60 mins by malachite green dye based spectrometric analysis | B | 5.28 | pIC50 | 5300 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084] |
| indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189159] [GtoPdb: 3019] [UniProtKB: Q8R0V5] | ||||||||
| ChEMBL | Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis | B | 4.54 | pIC50 | 28700 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7641-7646 [PMID:23122865] |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | DRUGMATRIX: Protein Serine/Threonine Kinase, ERK2 enzyme inhibition (substrate: Myelin Basic Protein) | B | 6.24 | pIC50 | 576 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| RAR-related orphan receptor-α/Nuclear receptor ROR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5868] [GtoPdb: 598] [UniProtKB: P35398] | ||||||||
| ChEMBL | Inverse agonist activity at RORalpha (unknown origin) by M1H assay | B | 6.7 | pIC50 | 199.53 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| RAR-related orphan receptor-β/Nuclear receptor ROR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091268] [GtoPdb: 599] [UniProtKB: Q92753] | ||||||||
| ChEMBL | Binding affinity to ROR beta (unknown origin) | B | 6.55 | pKd | 280 | nM | Kd | Medchemcomm (2013) 4: 764-776 |
| GtoPdb | - | - | 6.55 | pKi | - | - | - | Nat Struct Biol (2003) 10: 820-5 [PMID:12958591] |
| ChEMBL | Inverse agonist activity at recombinant N-terminally GST-tagged RORbeta ligand binding domain (unknown origin) expressed in Escherichia coli incubated for 1 hr by FRET assay | B | 4.6 | pIC50 | 25118.86 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| ChEMBL | Inverse agonist activity at RORbeta (unknown origin) by M1H assay | B | 6.9 | pIC50 | 125.89 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| GtoPdb | - | - | 9.82 | pIC50 | - | - | - | Nat Struct Biol (2003) 10: 820-5 [PMID:12958591] |
| ChEMBL | Inhibition of ROR beta (unknown origin)-mediated transactivation | B | 9.82 | pIC50 | 0.15 | nM | IC50 | Medchemcomm (2013) 4: 764-776 |
| RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449] | ||||||||
| ChEMBL | Inverse agonist activity at RORgammaT (unknown origin) by M1H assay | B | 6.7 | pIC50 | 199.53 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| ChEMBL | Inverse agonist activity at human RoRc-LBD fusion protein with GST expressed in BL-21 (BL3) cells assessed as SRC1 coactivator peptide recruitment | B | 4.74 | pEC50 | 18000 | nM | EC50 | J Med Chem (2014) 57: 5871-5892 [PMID:24502334] |
| peptidylprolyl cis/trans isomerase, NIMA-interacting 1/Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2288] [GtoPdb: 3171] [UniProtKB: Q13526] | ||||||||
| ChEMBL | Binding affinity to Pin1 (unknown origin) preincubated for 2 hrs followed by UV irradiation for 15 mins by SDS-PAGE gel based photoaffinity labelling method | B | 6.1 | pKd | 800 | nM | Kd | J Med Chem (2020) 63: 13355-13388 [PMID:32786507] |
| ChEMBL | Binding affinity to Pin1 (unknown origin) | B | 6.1 | pKd | 800 | nM | Kd | J Med Chem (2016) 59: 9622-9644 [PMID:27409354] |
| ChEMBL | Inhibition of GST-tagged Pin1 (unknown origin) using Suc-Ala-pSer-Pro-Phe-pNA, Suc-Ala-Glu-Pro-Phe-pNA or Suc-Ala-Ala-Pro-Phe-pNA as substrate preincubated with enzyme for 0.5 to 2 hrs followed by substrate addition by chymotrypsin coupled assay | B | 6.09 | pKi | 820 | nM | Ki | Bioorg Med Chem (2021) 29: 115878-115878 [PMID:33246256] |
| ChEMBL | Inhibition of human N-terminal His6-tagged Pin1 PPIase activity expressed in Escherichia coli BL21 using Suc-Ala-Glu-cis-Pro-Phe-4-nitroanilide as substrate preincubated for 10 mins followed by substrate addition monitored for 90 secs by protease enzyme coupled based spectrophotometric analysis | B | 6.09 | pIC50 | 820 | nM | IC50 | Bioorg Med Chem (2018) 26: 2186-2197 [PMID:29576270] |
| ChEMBL | Inhibition of Gst-tagged human Pin1by FP assay | B | 6.24 | pIC50 | 580 | nM | IC50 | J Med Chem (2023) 66: 9251-9277 [PMID:37438908] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276] | ||||||||
| ChEMBL | In vitro binding affinity for Retinoic acid receptor RAR alpha | B | 7.8 | pKd | 16 | nM | Kd | J Med Chem (1999) 42: 4961-4969 [PMID:10585206] |
| ChEMBL | Inhibition of [3H]RA binding to retinoic acid receptor RAR alpha | B | 7.82 | pKd | 15 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 589-594 [PMID:10098670] |
| ChEMBL | Binding affinity for Retinoic acid receptor alpha | B | 7.82 | pKd | 15 | nM | Kd | Bioorg Med Chem Lett (1997) 7: 2373-2378 |
| ChEMBL | Binding affinity for baculovirus-expressed Retinoic acid receptor RAR alpha | B | 7.82 | pKd | 15 | nM | Kd | J Med Chem (1996) 39: 3035-3038 [PMID:8759622] |
| ChEMBL | Inhibition of [3H]ATRA binding to human Retinoic acid receptor RAR alpha | B | 7.82 | pKd | 15 | nM | Kd | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Inhibition of [3H]ATRA binding to baculovirus expressed Retinoic acid receptor RAR alpha | B | 7.82 | pKd | 15 | nM | Kd | J Med Chem (1996) 39: 5027-5030 [PMID:8978832] |
| ChEMBL | Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor | B | 7.82 | pKd | 15 | nM | Kd | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Ability to displace 3[H](all-E)-retinoic acid (5 nM) from alpha retinoic acid receptor (alpha RAR) using transactivation assay | B | 7.82 | pKd | 15 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 573-576 [PMID:10098666] |
| ChEMBL | Binding affinity towards retinoic acid receptor alpha was determined using [3H]ATRA (5 nM) as radioligand | B | 7.85 | pKd | 14 | nM | Kd | Bioorg Med Chem Lett (2001) 11: 765-768 [PMID:11277515] |
| ChEMBL | Binding affinity fo retinoic acid receptor RAR alpha | B | 7.85 | pKd | 14 | nM | Kd | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
| ChEMBL | Apparent binding constant against Retinoic acid receptor alpha in HeLa cell GAl-4 transactivation assay | B | 8.64 | pKd | 2.3 | nM | Kd | J Med Chem (1996) 39: 2411-2421 [PMID:8691435] |
| GtoPdb | - | - | 9.4 | pKd | - | - | - |
Proc Natl Acad Sci USA (1993) 90: 30-4 [PMID:8380496]; Mol Cell Biol (1994) 14: 287-98 [PMID:8264595]; J Mol Biol (2000) 302: 155-70 [PMID:10964567]; Mol Cell Biol (1995) 15: 3540-51 [PMID:7791761]; Curr Pharm Des (2000) 6: 25-58 [PMID:10637371] |
| ChEMBL | Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR alpha | B | 6.73 | pKi | 187 | nM | Ki | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Binding affinity to retinoic acid receptor alpha using [3H]CD 367 as radioligand | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (1995) 38: 4993-5006 [PMID:8544175] |
| ChEMBL | Agonistic activity towards retinoic acid receptor-alpha | F | 8.48 | pKi | 3.3 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| ChEMBL | Binding affinity towards human Retinoic acid receptor alpha | B | 10 | pKi | 0.1 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2313-2318 |
| ChEMBL | Displacement of [11,12-3H]ARTA from RARalpha | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2004) 47: 6716-6729 [PMID:15615521] |
| ChEMBL | Binding affinity against retinoic Acid alpha receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Binding affinity for Retinoic acid receptor alpha | B | 9.05 | pIC50 | 0.89 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 623-625 [PMID:10762039] |
| ChEMBL | Inhibition of [3H]ATRA-Hl60 binding to Retinoic acid receptor alpha | B | 9.11 | pIC50 | 0.78 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 619-622 [PMID:10762038] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha | F | 6.25 | pEC50 | 563 | nM | EC50 | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha | B | 6.34 | pEC50 | 459 | nM | EC50 | J Med Chem (1996) 39: 5027-5030 [PMID:8978832] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing human Retinoic acid receptor RAR alpha | B | 6.36 | pEC50 | 436 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Transactivation potency for Retinoic acid receptor alpha | B | 6.46 | pEC50 | 350 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 2373-2378 |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR alpha | B | 6.46 | pEC50 | 350 | nM | EC50 | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Binding affinity against retinoic Acid alpha receptors co-transfected into CV-1 cells | B | 6.46 | pEC50 | 350 | nM | EC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Agonist activity for retinoic acid receptor RAR alpha in transcriptional activation assay | F | 6.46 | pEC50 | 350 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 2729-2734 |
| ChEMBL | Agonist activity RARalpha (unknown origin) assessed as induction of receptor transactivation | B | 6.62 | pEC50 | 240 | nM | EC50 | J Med Chem (2019) 62: 2112-2126 [PMID:30702885] |
| ChEMBL | Ability to inhibit TTNPB-induced transactivation at retinoic acid receptor alpha | B | 6.62 | pEC50 | 240 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 765-768 [PMID:11277515] |
| ChEMBL | Effective concentration for retinoic acid receptor RAR alpha transcriptional activation | F | 6.62 | pEC50 | 240 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
| ChEMBL | Activation of RXRalpha (unknown origin) by CAT reporter gene assay | B | 7.3 | pEC50 | 50 | nM | EC50 | Bioorg Med Chem (2013) 21: 4342-4350 [PMID:23685180] |
| ChEMBL | Effective concentration against RAR-alpha receptor | B | 7.57 | pEC50 | 27 | nM | EC50 | J Med Chem (1993) 36: 2605-2613 [PMID:8410972] |
| ChEMBL | Activity at human RARalpha ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay | B | 7.77 | pEC50 | 17 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-492 [PMID:19058965] |
| GtoPdb | - | - | 7.77 | pEC50 | 17 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-92 [PMID:19058965] |
| ChEMBL | Transactivation of GST-tagged RARalpha LBD (unknown origin) assessed as fluorescein-labelled coactivator peptide recruitment measured after 4 hrs by TR-FRET analysis | B | 7.79 | pEC50 | 16.1 | nM | EC50 | Bioorg Med Chem (2018) 26: 1560-1572 [PMID:29439915] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha | F | 8.15 | pEC50 | 7 | nM | EC50 | J Med Chem (1995) 38: 4764-4767 [PMID:7490725] |
| ChEMBL | Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor alpha using transactivation assay | B | 8.15 | pEC50 | 7 | nM | EC50 | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Activity at RARalpha expressed in mouse NIH3T3 cells by R-SAT assay | B | 8.2 | pEC50 | 6.31 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
| ChEMBL | Transcriptional activation of retinoic acid receptor RAR alpha | B | 8.3 | pEC50 | 5 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 523-527 |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR alpha | B | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (1995) 38: 2820-2829 [PMID:7636843] |
| ChEMBL | Transcriptional activation for RAR alpha receptor | B | 8.3 | pEC50 | 5 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 1447-1452 |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR alpha | F | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (1999) 42: 4961-4969 [PMID:10585206] |
| ChEMBL | Transactivation of human Gal4-DBD-fused RARalpha-LBD expressed in HEK293T cells after 16 to 24 hrs by FRET based beta-lactamase reporter gene assay | B | 9 | pEC50 | 1.01 | nM | EC50 | Bioorg Med Chem (2018) 26: 798-814 [PMID:29288071] |
| Retinoic acid receptor-α/Retinoic acid receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2792] [GtoPdb: 590] [UniProtKB: P11416] | ||||||||
| ChEMBL | Dissociation constant for binding to Retinoic acid receptor alpha | B | 7.82 | pKd | 15 | nM | Kd | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Inhibition of [3H]ATRA binding to mouse Retinoic acid receptor RAR alpha | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1996) 39: 3625-3635 [PMID:8809153] |
| ChEMBL | Inhibition of binding to retinoid A receptor RAR alpha | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1998) 41: 1679-1687 [PMID:9572893] |
| ChEMBL | Inhibition of murine Retinoic acid receptor RAR alpha | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1995) 38: 2302-2310 [PMID:7608895] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing retinoid A receptor RAR alpha | B | 7.66 | pEC50 | 22 | nM | EC50 | J Med Chem (1998) 41: 1679-1687 [PMID:9572893] |
| ChEMBL | Transactivation of mouse Gal4-fused RARalpha-LBD expressed in COS-7 cells after 1 day by bright-Glo reagent based assay | B | 8.82 | pEC50 | 1.51 | nM | EC50 | Bioorg Med Chem (2018) 26: 798-814 [PMID:29288071] |
| ChEMBL | Transactivation of GAL4-fused mouse RARalpha-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay | B | 8.92 | pEC50 | 1.2 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 995-1000 [PMID:30792038] |
| Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826] | ||||||||
| ChEMBL | Inhibition of [3H]-ATRA binding to human Retinoic acid receptor RAR beta | B | 7.77 | pKd | 17 | nM | Kd | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Inhibition of [3H]RA binding to retinoic acid receptor RAR beta | B | 7.89 | pKd | 13 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 589-594 [PMID:10098670] |
| ChEMBL | Binding affinity for Retinoic acid receptor beta | B | 7.89 | pKd | 13 | nM | Kd | Bioorg Med Chem Lett (1997) 7: 2373-2378 |
| ChEMBL | Ability to displace 3[H](all-E)-retinoic acid (5 nM) from beta retinoic acid receptor (beta RAR) using transactivation assay | B | 7.89 | pKd | 13 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 573-576 [PMID:10098666] |
| ChEMBL | Inhibition of [3H]ATRA binding to baculovirus expressed Retinoic acid receptor RAR beta | B | 7.89 | pKd | 13 | nM | Kd | J Med Chem (1996) 39: 5027-5030 [PMID:8978832] |
| ChEMBL | Binding affinity for baculovirus-expressed Retinoic acid receptor RAR beta | B | 7.89 | pKd | 13 | nM | Kd | J Med Chem (1996) 39: 3035-3038 [PMID:8759622] |
| ChEMBL | Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor | B | 7.89 | pKd | 13 | nM | Kd | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Binding constant for baculovirus-expressed Retinoic acid receptor RAR beta | B | 7.92 | pKd | 12 | nM | Kd | J Med Chem (1995) 38: 4764-4767 [PMID:7490725] |
| ChEMBL | Binding affinity towards retinoic acid receptor beta was determined using [3H]ATRA (5 nM) as radioligand | B | 7.96 | pKd | 11 | nM | Kd | Bioorg Med Chem Lett (2001) 11: 765-768 [PMID:11277515] |
| ChEMBL | Binding affinity for retinoic acid receptor RAR beta | B | 7.96 | pKd | 11 | nM | Kd | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
| ChEMBL | In vitro binding affinity for Retinoic acid receptor RAR beta | B | 8.15 | pKd | 7 | nM | Kd | J Med Chem (1999) 42: 4961-4969 [PMID:10585206] |
| ChEMBL | Apparent binding constant for Retinoic acid receptor beta in HeLa cellGAL-4 transactivation assay | B | 9.4 | pKd | 0.4 | nM | Kd | J Med Chem (1996) 39: 2411-2421 [PMID:8691435] |
| ChEMBL | Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR beta | B | 7.76 | pKi | 17.4 | nM | Ki | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Binding affinity to retinoic acid receptor beta using [3H]CD 367 as radioligand | B | 8.15 | pKi | 7 | nM | Ki | J Med Chem (1995) 38: 4993-5006 [PMID:8544175] |
| ChEMBL | Agonistic activity towards retinoic acid receptor-beta | F | 8.39 | pKi | 4.1 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| ChEMBL | Binding affinity towards cRARbeta2 receptor by displacing 0.82 nM 3[H]all-trans-RA | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2313-2318 |
| ChEMBL | Binding affinity towards cRAR-beta-2 receptor by displacing 1.1 nM 3[H]-9-cis-RA | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2313-2318 |
| GtoPdb | - | - | 9.4 | pKi | - | - | - |
Mol Cell Biol (1994) 14: 287-98 [PMID:8264595]; J Mol Biol (2000) 302: 155-70 [PMID:10964567]; Mol Cell Biol (1995) 15: 3540-51 [PMID:7791761]; Curr Pharm Des (2000) 6: 25-58 [PMID:10637371] |
| ChEMBL | Displacement of [11,12-3H]ARTA from RARbeta | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2004) 47: 6716-6729 [PMID:15615521] |
| ChEMBL | Binding affinity against retinoic Acid beta receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Binding affinity for Retinoic acid receptor beta | B | 9.03 | pIC50 | 0.94 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 623-625 [PMID:10762039] |
| ChEMBL | Inhibition of [3H]-ATRA-Hl60 binding to Retinoic acid receptor beta | B | 9.05 | pIC50 | 0.9 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 619-622 [PMID:10762038] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta | F | 6.98 | pEC50 | 105 | nM | EC50 | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta | B | 7.06 | pEC50 | 87 | nM | EC50 | J Med Chem (1996) 39: 5027-5030 [PMID:8978832] |
| ChEMBL | Agonist activity for retinoic acid receptor RAR beta in transcriptional activation assay | F | 7.1 | pEC50 | 80 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 2729-2734 |
| ChEMBL | Transactivation potency for Retinoic acid receptor beta | B | 7.1 | pEC50 | 80 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 2373-2378 |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR beta | B | 7.1 | pEC50 | 80 | nM | EC50 | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Binding affinity against retinoic Acid beta receptors co-transfected into CV-1 cells | B | 7.1 | pEC50 | 80 | nM | EC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing human Retinoic acid receptor RAR beta | B | 7.11 | pEC50 | 78 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Agonist activity RARbeta (unknown origin) assessed as induction of receptor transactivation | B | 7.42 | pEC50 | 38 | nM | EC50 | J Med Chem (2019) 62: 2112-2126 [PMID:30702885] |
| ChEMBL | Ability to inhibit TTNPB-induced transactivation at retinoic acid receptor beta | B | 7.42 | pEC50 | 38 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 765-768 [PMID:11277515] |
| ChEMBL | Effective concentration for retinoic acid receptor RAR beta transcriptional activation | F | 7.42 | pEC50 | 38 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
| ChEMBL | Activity at RARbeta1 expressed in mouse NIH3T3 cells by R-SAT assay | B | 7.6 | pEC50 | 25.12 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
| ChEMBL | Transcriptional activity against RARbeta1 | F | 7.6 | pEC50 | 25.12 | nM | EC50 | J Med Chem (2005) 48: 7517-7519 [PMID:16302793] |
| ChEMBL | Transactivation of GST-tagged RARbeta LBD (unknown origin) assessed as fluorescein-labelled coactivator peptide recruitment measured after 4 hrs by TR-FRET analysis | B | 7.75 | pEC50 | 17.6 | nM | EC50 | Bioorg Med Chem (2018) 26: 1560-1572 [PMID:29439915] |
| GtoPdb | - | - | 7.92 | pEC50 | 12 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-92 [PMID:19058965] |
| ChEMBL | Effective concentration against Retinoic acid receptor beta | B | 7.92 | pEC50 | 12 | nM | EC50 | J Med Chem (1993) 36: 2605-2613 [PMID:8410972] |
| ChEMBL | Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay | B | 7.92 | pEC50 | 12 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-492 [PMID:19058965] |
| ChEMBL | Agonist activity at RARbeta2 expressed in mouse NIH3T3 cells by R-SAT assay | F | 8.2 | pEC50 | 6.31 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
| ChEMBL | Transcriptional activity against RARbeta2 | F | 8.2 | pEC50 | 6.31 | nM | EC50 | J Med Chem (2005) 48: 7517-7519 [PMID:16302793] |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR beta | F | 8.82 | pEC50 | 1.5 | nM | EC50 | J Med Chem (1999) 42: 4961-4969 [PMID:10585206] |
| ChEMBL | Transcriptional activation for RAR beta receptor | B | 8.82 | pEC50 | 1.5 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 1447-1452 |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR beta | B | 8.82 | pEC50 | 1.5 | nM | EC50 | J Med Chem (1995) 38: 2820-2829 [PMID:7636843] |
| ChEMBL | Transcriptional activation of retinoic acid receptor RAR beta | B | 8.82 | pEC50 | 1.5 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 523-527 |
| ChEMBL | Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor beta using transactivation assay | B | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (1995) 38: 4764-4767 [PMID:7490725] |
| Retinoic acid receptor-β/Retinoic acid receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3266] [GtoPdb: 591] [UniProtKB: P22605] | ||||||||
| ChEMBL | Dissociation constant for binding to Retinoic acid receptor beta | B | 7.89 | pKd | 13 | nM | Kd | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Inhibition of binding to retinoid A receptor RAR beta | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1998) 41: 1679-1687 [PMID:9572893] |
| ChEMBL | Inhibition of murine Retinoic acid receptor RAR beta | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (1995) 38: 2302-2310 [PMID:7608895] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing retinoid A receptor RAR beta | B | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (1998) 41: 1679-1687 [PMID:9572893] |
| ChEMBL | Transactivation of GAL4-fused mouse RARbeta-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay | B | 8.92 | pEC50 | 1.2 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 995-1000 [PMID:30792038] |
| ChEMBL | Transactivation of mouse Gal4-fused RARbeta-LBD expressed in COS-7 cells after 1 day by bright-Glo reagent based assay | B | 9.28 | pEC50 | 0.52 | nM | EC50 | Bioorg Med Chem (2018) 26: 798-814 [PMID:29288071] |
| Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631] | ||||||||
| ChEMBL | Binding constant for baculovirus-expressed Retinoic acid receptor RAR gamma | B | 7.72 | pKd | 19 | nM | Kd | J Med Chem (1995) 38: 4764-4767 [PMID:7490725] |
| ChEMBL | Inhibition of [3H]RA binding to retinoic acid receptor RAR gamma | B | 7.74 | pKd | 18 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 589-594 [PMID:10098670] |
| ChEMBL | Binding affinity for Retinoic acid receptor gamma | B | 7.74 | pKd | 18 | nM | Kd | Bioorg Med Chem Lett (1997) 7: 2373-2378 |
| ChEMBL | Inhibition of [3H]ATRA binding to baculovirus expressed Retinoic acid receptor RAR gamma | B | 7.74 | pKd | 18 | nM | Kd | J Med Chem (1996) 39: 5027-5030 [PMID:8978832] |
| ChEMBL | Binding affinity for baculovirus-expressed Retinoic acid receptor RAR gamma | B | 7.74 | pKd | 18 | nM | Kd | J Med Chem (1996) 39: 3035-3038 [PMID:8759622] |
| ChEMBL | Ability to displace 3[H](all-E)-retinoic acid (5 nM) from Retinoic acid receptor gamma using transactivation assay | B | 7.74 | pKd | 18 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 573-576 [PMID:10098666] |
| ChEMBL | Compound was tested for binding affinity against retinoic acid receptor using 5 nM of [3H]RA as a radioligand in baculovirus expressed receptor | B | 7.74 | pKd | 18 | nM | Kd | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Inhibition of [3H]ATRA binding to human Retinoic acid receptor RAR gamma | B | 7.77 | pKd | 17 | nM | Kd | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Binding affinity towards retinoic acid receptor gamma was determined using [3H]ATRA (5 nM) as radioligand | B | 7.8 | pKd | 16 | nM | Kd | Bioorg Med Chem Lett (2001) 11: 765-768 [PMID:11277515] |
| ChEMBL | Binding affinity for retinoic acid receptor RAR gamma | B | 7.8 | pKd | 16 | nM | Kd | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
| ChEMBL | In vitro binding affinity for Retinoic acid receptor RAR gamma | B | 8.52 | pKd | 3 | nM | Kd | J Med Chem (1999) 42: 4961-4969 [PMID:10585206] |
| ChEMBL | Apparent binding constant against Retinoic acid receptor gamma in HeLa cell GAl-4 transactivation assay | B | 9.52 | pKd | 0.3 | nM | Kd | J Med Chem (1996) 39: 2411-2421 [PMID:8691435] |
| GtoPdb | - | - | 9.6 | pKd | - | - | - |
Proc Natl Acad Sci USA (1993) 90: 30-4 [PMID:8380496]; Mol Cell Biol (1994) 14: 287-98 [PMID:8264595]; J Mol Biol (2000) 302: 155-70 [PMID:10964567]; Mol Cell Biol (1995) 15: 3540-51 [PMID:7791761]; Curr Pharm Des (2000) 6: 25-58 [PMID:10637371] |
| ChEMBL | Dissociation constant for Retinoic acid receptor gamma | B | 9.7 | pKd | 0.2 | nM | Kd | J Med Chem (2005) 48: 6212-6219 [PMID:16190748] |
| ChEMBL | Inhibition of [3H]ATRA binding to Retinoic acid receptor RAR gamma | B | 7.73 | pKi | 18.5 | nM | Ki | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Binding affinity to retinoic acid receptor (RAR) gamma using [3H]CD 367 as radioligand | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (1995) 38: 4993-5006 [PMID:8544175] |
| ChEMBL | Binding affinity against Retinoic acid receptor gamma | B | 9.15 | pKi | 0.7 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1583-1586 [PMID:11412986] |
| ChEMBL | Binding affinity towards human Retinoic acid receptor gamma | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2313-2318 |
| ChEMBL | Inhibition of [3H]RA to binding Retinoic acid receptor RAR gamma | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 2117-2122 |
| ChEMBL | Agonistic activity towards retinoic acid receptor-gamma | F | 10.4 | pKi | 0.04 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| ChEMBL | Binding affinity against retinoic Acid gamma receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Binding affinity against Retinoic acid receptor gamma | B | 9.21 | pIC50 | 0.62 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 623-625 [PMID:10762039] |
| ChEMBL | Inhibition of [3H]ATRA-Hl60 binding to Retinoic acid receptor gamma | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 619-622 [PMID:10762038] |
| ChEMBL | Activity at RARgamma expressed in mouse NIH3T3 cells by R-SAT assay | B | 7.3 | pEC50 | 50.12 | nM | EC50 | J Med Chem (2009) 52: 1540-1545 [PMID:19239230] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma | F | 7.48 | pEC50 | 33 | nM | EC50 | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma | B | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (1996) 39: 5027-5030 [PMID:8978832] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing human Retinoic acid receptor RAR gamma | B | 7.72 | pEC50 | 19 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Transactivation of GST-tagged RARgamma LBD (unknown origin) assessed as fluorescein-labelled coactivator peptide recruitment measured after 4 hrs by TR-FRET analysis | B | 7.83 | pEC50 | 14.7 | nM | EC50 | Bioorg Med Chem (2018) 26: 1560-1572 [PMID:29439915] |
| ChEMBL | Binding affinity against retinoic Acid gamma receptors co-transfected into CV-1 cells | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR gamma | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Transactivation potency for Retinoic acid receptor gamma | B | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 2373-2378 |
| ChEMBL | Agonist activity for retinoic acid receptor RAR gamma in transcriptional activation assay | F | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 2729-2734 |
| ChEMBL | Effective concentration against RAR-gamma receptor | B | 8.1 | pEC50 | 8 | nM | EC50 | J Med Chem (1993) 36: 2605-2613 [PMID:8410972] |
| ChEMBL | Effective concentration for retinoic acid receptor RAR gamma transcriptional activation | F | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 3145-3148 [PMID:12372520] |
| ChEMBL | Ability to inhibit TTNPB-induced transactivation at retinoic acid receptor gamma | B | 8.22 | pEC50 | 6 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 765-768 [PMID:11277515] |
| ChEMBL | Agonist activity RARgamma (unknown origin) assessed as induction of receptor transactivation | B | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (2019) 62: 2112-2126 [PMID:30702885] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma | F | 9.15 | pEC50 | 0.7 | nM | EC50 | J Med Chem (1995) 38: 4764-4767 [PMID:7490725] |
| ChEMBL | Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoic acid receptor gamma using transactivation assay | B | 9.15 | pEC50 | 0.7 | nM | EC50 | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR gamma | B | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (1995) 38: 2820-2829 [PMID:7636843] |
| ChEMBL | Transcriptional activation of retinoic acid receptor RAR gamma | B | 9.3 | pEC50 | 0.5 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 523-527 |
| ChEMBL | Transcriptional activation for RAR gamma receptor | B | 9.3 | pEC50 | 0.5 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 1447-1452 |
| ChEMBL | Transcriptional activation of Retinoic acid receptor RAR gamma | F | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (1999) 42: 4961-4969 [PMID:10585206] |
| ChEMBL | Activity at human RARgamma ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay | B | 9.7 | pEC50 | 0.2 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-492 [PMID:19058965] |
| GtoPdb | - | - | 9.7 | pEC50 | 0.2 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 489-92 [PMID:19058965] |
| Retinoic acid receptor-γ/Retinoic acid receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4177] [GtoPdb: 592] [UniProtKB: P18911] | ||||||||
| ChEMBL | Dissociation constant for binding to Retinoic acid receptor gamma | B | 7.74 | pKd | 18 | nM | Kd | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Inhibition of binding to retinoid A receptor RAR gamma | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1998) 41: 1679-1687 [PMID:9572893] |
| ChEMBL | Inhibition of binding to murine Retinoic acid receptor RAR gamma | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1995) 38: 2302-2310 [PMID:7608895] |
| ChEMBL | Transactivation of GAL4-fused mouse RARgamma-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay | B | 9.22 | pEC50 | 0.6 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 995-1000 [PMID:30792038] |
| ChEMBL | Transactivation of mouse Gal4-fused RARgamma-LBD expressed in COS-7 cells after 1 day by bright-Glo reagent based assay | B | 9.66 | pEC50 | 0.22 | nM | EC50 | Bioorg Med Chem (2018) 26: 798-814 [PMID:29288071] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793] | ||||||||
| ChEMBL | Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]-9-cis-RA as a radioligand in baculovirus expressed receptor | B | 6 | pKd | >1000 | nM | Kd | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Inhibition of binding to human Retinoic acid receptor RXR DEF domain | B | 6.7 | pKd | >200 | nM | Kd | J Med Chem (1996) 39: 3625-3635 [PMID:8809153] |
| ChEMBL | Inhibition of binding to human Retinoid X receptor RXR alpha | B | 6.7 | pKd | >200 | nM | Kd | J Med Chem (1995) 38: 2302-2310 [PMID:7608895] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to human Retinoid X receptor RXR alpha | B | 7.28 | pKd | 53 | nM | Kd | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Relative activity against Retinoid X receptor RXR-alpha compared to 9-cis-RA | B | 8.05 | pKd | 9 | nM | Kd | J Med Chem (1995) 38: 4764-4767 [PMID:7490725] |
| ChEMBL | Inhibition of [3H]-9-cis RA binding to Retinoid X receptor RXR gamma | B | 12 | pKd | >0 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 589-594 [PMID:10098670] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR alpha | B | 6.46 | pKi | 350 | nM | Ki | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Agonistic activity towards retinoid X receptor-alpha | F | 6.48 | pKi | 330 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| ChEMBL | Binding affinity for retinoic acid receptor RAR alpha | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2447-2450 [PMID:12161154] |
| ChEMBL | Binding affinity against retinoic Acid X alpha receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Transcriptional activation of retinoid X receptor RXR alpha; not active | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 523-527 |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR alpha | F | 5.96 | pEC50 | 1084 | nM | EC50 | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing human Retinoid X receptor RXR-alpha | B | 5.99 | pEC50 | 1015 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Agonist activity for retinoic acid receptor RXR alpha in transcriptional activation assay | F | 6.05 | pEC50 | 900 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 2729-2734 |
| ChEMBL | Binding affinity against retinoic Acid X alpha receptors co-transfected into CV-1 cells | B | 6.05 | pEC50 | 900 | nM | EC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor alpha using transactivation assay | B | 6.05 | pEC50 | 900 | nM | EC50 | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Transcriptional activation of Retinoid X receptor RXR alpha | B | 6.05 | pEC50 | 900 | nM | EC50 | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Effective concentration against Retinoic acid receptor RXR-alpha | B | 6.28 | pEC50 | 530 | nM | EC50 | J Med Chem (1995) 38: 3368-3383 [PMID:7650690] |
| ChEMBL | Effective concentration against RXR-alpha receptor | B | 6.37 | pEC50 | 430 | nM | EC50 | J Med Chem (1993) 36: 2605-2613 [PMID:8410972] |
| ChEMBL | Effective concentration against Retinoic acid receptor RXR-alpha | B | 7.27 | pEC50 | 54 | nM | EC50 | J Med Chem (1995) 38: 3368-3383 [PMID:7650690] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3084] [GtoPdb: 610] [UniProtKB: P28700] | ||||||||
| ChEMBL | Dissociation constant for binding to Retinoid X receptor alpha | B | 6 | pKd | 1000 | nM | Kd | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Inhibition of binding to murine Retinoid X receptor RXR alpha | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (1995) 38: 2302-2310 [PMID:7608895] |
| ChEMBL | Inhibition of [3H]-ATRA binding to mouse Retinoic acid receptor RXR alpha | B | 5.7 | pIC50 | >2000 | nM | IC50 | J Med Chem (1996) 39: 3625-3635 [PMID:8809153] |
| ChEMBL | Inhibition of binding to retinoid X receptor RXR alpha | B | 5.7 | pIC50 | >2000 | nM | IC50 | J Med Chem (1998) 41: 1679-1687 [PMID:9572893] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha | B | 5.7 | pEC50 | >2000 | nM | EC50 | J Med Chem (1998) 41: 1679-1687 [PMID:9572893] |
| Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702] | ||||||||
| ChEMBL | Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]9-cis-RA as a radioligand in baculovirus expressed receptor | B | 6 | pKd | >1000 | nM | Kd | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Inhibition of [3H]-9-cis RA binding to Retinoid X receptor RXR beta | B | 12 | pKd | >0 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 589-594 [PMID:10098670] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR beta | B | 6.06 | pKi | 881 | nM | Ki | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Agonistic activity towards retinoid X receptor-beta | F | 7.27 | pKi | 54 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| ChEMBL | Binding affinity for retinoic acid receptor RAR beta | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2447-2450 [PMID:12161154] |
| ChEMBL | Binding affinity against retinoic Acid X beta receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Binding affinity against retinoic Acid X beta receptors co-transfected into CV-1 cells | B | 5.85 | pEC50 | 1400 | nM | EC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Agonist activity for retinoic acid receptor RXR beta in transcriptional activation assay | F | 5.85 | pEC50 | 1400 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 2729-2734 |
| ChEMBL | Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor beta using transactivation assay | B | 5.85 | pEC50 | 1400 | nM | EC50 | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Transcriptional activation of Retinoid X receptor RXR beta | B | 5.85 | pEC50 | 1400 | nM | EC50 | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR beta | F | 5.86 | pEC50 | 1394 | nM | EC50 | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Effective concentrations against Retinoic acid receptor RXR-beta | B | 8.35 | pEC50 | 4.5 | nM | EC50 | J Med Chem (1995) 38: 3368-3383 [PMID:7650690] |
| Retinoid X receptor-β/Retinoid X receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4047] [GtoPdb: 611] [UniProtKB: P28704] | ||||||||
| ChEMBL | Dissociation constant for binding to Retinoid X receptor beta | B | 6 | pKd | 1000 | nM | Kd | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to mouse Retinoid X receptor RXR beta | B | 6.51 | pKd | 306 | nM | Kd | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Inhibition of binding to murine Retinoid X receptor RXR beta | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (1995) 38: 2302-2310 [PMID:7608895] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing mouse Retinoid X receptor RXR beta | B | 5.92 | pEC50 | 1211 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443] | ||||||||
| ChEMBL | Compound was tested for binding affinity against retinoid X receptor using 5 nM of [3H]9-cis-RA as a radioligand in baculovirus expressed receptor | B | 6.46 | pKd | 350 | nM | Kd | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Inhibition of [3H]-9-cis-RA binding to human Retinoid X receptor RXR gamma | B | 6.51 | pKd | 306 | nM | Kd | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR gamma | B | 6.54 | pKi | 288 | nM | Ki | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Agonistic activity towards retinoid X receptor-gamma | F | 6.92 | pKi | 120 | nM | Ki | J Med Chem (1997) 40: 4222-4234 [PMID:9435893] |
| ChEMBL | Binding affinity for retinoic acid receptor RAR gamma | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2447-2450 [PMID:12161154] |
| ChEMBL | Binding affinity against retinoic Acid X gamma receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assay | B | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing Retinoid X receptor RXR gamma | F | 5.91 | pEC50 | 1225 | nM | EC50 | J Med Chem (1996) 39: 2659-2663 [PMID:8709094] |
| ChEMBL | Binding affinity against retinoic Acid X gamma receptors co-transfected into CV-1 cells | B | 5.96 | pEC50 | 1100 | nM | EC50 | J Med Chem (1994) 37: 408-414 [PMID:8308867] |
| ChEMBL | Agonist activity for retinoic acid receptor RXR gamma in transcriptional activation assay | F | 5.96 | pEC50 | 1100 | nM | EC50 | Bioorg Med Chem Lett (1995) 5: 2729-2734 |
| ChEMBL | Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor gamma using transactivation assay | B | 5.96 | pEC50 | 1100 | nM | EC50 | Bioorg Med Chem Lett (1996) 6: 213-218 |
| ChEMBL | Transcriptional activation of Retinoid X receptor RXR gamma | B | 5.96 | pEC50 | 1100 | nM | EC50 | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Effective concentrations against Retinoic acid receptor RXR-gamma | B | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (1995) 38: 3368-3383 [PMID:7650690] |
| Retinoid X receptor-γ/Retinoid X receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4402] [GtoPdb: 612] [UniProtKB: P28705] | ||||||||
| ChEMBL | Dissociation constant for binding to Retinoid X receptor gamma | B | 6.46 | pKd | 350 | nM | Kd | J Med Chem (1996) 39: 3556-3563 [PMID:8784454] |
| ChEMBL | Inhibition of binding to murine Retinoid X receptor RXR gamma | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (1995) 38: 2302-2310 [PMID:7608895] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing mouse Retinoid X receptor RXR gamma | B | 6.02 | pEC50 | 961 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 261-264 [PMID:12482435] |
| ChEMBL | Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma | B | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (1998) 41: 1679-1687 [PMID:9572893] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.64 | pKi | 228 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 6.45 | pIC50 | 358 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Peroxisome proliferator-activated receptor-β/δ in Human [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| GtoPdb | - | - | 7.8 | pKd | - | - | - | J Biol Chem (2003) 278: 41589-92 [PMID:12963727] |
| Testicular receptor 4 in Human [GtoPdb: 614] [UniProtKB: P49116] | ||||||||
| GtoPdb | - | - | 4.62 | pEC50 | 23800 | nM | EC50 | J Biol Chem (2011) 286: 2877-85 [PMID:21068381] |
| TLX in Human [GtoPdb: 615] [UniProtKB: Q9Y466] | ||||||||
| GtoPdb | Gal4-DBD TLX LBD screening to determine changes in TLX activity in HEK293 cells. | - | 5.74 | pEC50 | 1830 | nM | EC50 | Cell Chem Biol (2020) 27: 1272-1284.e4 [PMID:32763139] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
