tretinoin [Ligand Id: 2644] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL38 (Atralin, Retin-a, Altreno, Tretinoin, Retin-a micro, Vesanoid, Avita, Renova, Retin-a-micro, Retinoic acid, NSC-122758, Acticin, Tretin-X)
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • This target only has 1 pki data point
  • 5.53
1 CHEMBL38_lig_chart_1 Adenosine A3 receptor Human
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  • Cellular retinoic acid-binding protein I in Chicken [ChEMBL: CHEMBL4945] [UniProtKB: P40220]
  • cellular retinoic acid binding protein 1/Cellular retinoic acid-binding protein I in Mouse [ChEMBL: CHEMBL3208] [GtoPdb: 2529] [UniProtKB: P62965]
  • This target only has 0 pki data point
  • 0
2 CHEMBL38_lig_chart_2 Cellular retinoic acid-binding protein I ChickenMouse
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  • cellular retinoic acid binding protein 2/Cellular retinoic acid-binding protein II in Mouse [ChEMBL: CHEMBL4172] [GtoPdb: 2530] [UniProtKB: P22935]
  • This target only has 0 pki data point
  • 0
3 CHEMBL38_lig_chart_3 Cellular retinoic acid-binding protein II Mouse
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  • GroEL/GroES in Escherichia coli [ChEMBL: CHEMBL4106139] [UniProtKB: Q548M1Q7BGE6]
  • This target only has 0 pki data point
  • 0
4 CHEMBL38_lig_chart_4 GroEL/GroES Escherichia coli
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5 CHEMBL38_lig_chart_5 HSP60/HSP10 Human
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  • indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Mouse [ChEMBL: CHEMBL2189159] [GtoPdb: 3019] [UniProtKB: Q8R0V5]
  • This target only has 0 pki data point
  • 0
6 CHEMBL38_lig_chart_6 Indoleamine 2,3-dioxygenase 2 Mouse
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  • mitogen-activated protein kinase 1/MAP kinase ERK2 in Human [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482]
  • This target only has 0 pki data point
  • 0
7 CHEMBL38_lig_chart_7 MAP kinase ERK2 Human
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  • RAR-related orphan receptor-α/Nuclear receptor ROR-alpha in Human [ChEMBL: CHEMBL5868] [GtoPdb: 598] [UniProtKB: P35398]
  • This target only has 0 pki data point
  • 0
8 CHEMBL38_lig_chart_8 Nuclear receptor ROR-alpha Human
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  • RAR-related orphan receptor-β/Nuclear receptor ROR-beta in Human [ChEMBL: CHEMBL3091268] [GtoPdb: 599] [UniProtKB: Q92753]
  • This target only has 1 pki data point
  • 6.55
9 CHEMBL38_lig_chart_9 Nuclear receptor ROR-beta Human
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  • RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
  • This target only has 0 pki data point
  • 0
10 CHEMBL38_lig_chart_10 Nuclear receptor ROR-gamma Human
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  • peptidylprolyl cis/trans isomerase, NIMA-interacting 1/Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 in Human [ChEMBL: CHEMBL2288] [GtoPdb: 3171] [UniProtKB: Q13526]
  • This target only has 0 pki data point
  • 0
11 CHEMBL38_lig_chart_11 Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 Human
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
12 CHEMBL38_lig_chart_12 Plasmodium falciparum Plasmodium falciparum
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  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Human [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Mouse [ChEMBL: CHEMBL2792] [GtoPdb: 590] [UniProtKB: P11416]
  • 0
13 CHEMBL38_lig_chart_13 Retinoic acid receptor alpha HumanMouse
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  • Retinoic acid receptor-β/Retinoic acid receptor beta in Human [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
  • Retinoic acid receptor-β/Retinoic acid receptor beta in Mouse [ChEMBL: CHEMBL3266] [GtoPdb: 591] [UniProtKB: P22605]
  • 0
14 CHEMBL38_lig_chart_14 Retinoic acid receptor beta HumanMouse
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  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Mouse [ChEMBL: CHEMBL4177] [GtoPdb: 592] [UniProtKB: P18911]
  • 0
15 CHEMBL38_lig_chart_15 Retinoic acid receptor gamma HumanMouse
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  • Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
  • Retinoid X receptor-α/Retinoid X receptor alpha in Mouse [ChEMBL: CHEMBL3084] [GtoPdb: 610] [UniProtKB: P28700]
  • 0
16 CHEMBL38_lig_chart_16 Retinoid X receptor alpha HumanMouse
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  • Retinoid X receptor-β/Retinoid X receptor beta in Human [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
  • Retinoid X receptor-β/Retinoid X receptor beta in Mouse [ChEMBL: CHEMBL4047] [GtoPdb: 611] [UniProtKB: P28704]
  • 0
17 CHEMBL38_lig_chart_17 Retinoid X receptor beta HumanMouse
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  • Retinoid X receptor-γ/Retinoid X receptor gamma in Human [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
  • Retinoid X receptor-γ/Retinoid X receptor gamma in Mouse [ChEMBL: CHEMBL4402] [GtoPdb: 612] [UniProtKB: P28705]
  • 0
18 CHEMBL38_lig_chart_18 Retinoid X receptor gamma HumanMouse
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • This target only has 1 pki data point
  • 6.64
19 CHEMBL38_lig_chart_19 Serotonin 2b (5-HT2b) receptor Human
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  • Peroxisome proliferator-activated receptor-β/δ in Human [GtoPdb: 594] [UniProtKB: Q03181]
  • This target only has 0 pki data point
  • 0
20 CHEMBL38_lig_chart_20 Peroxisome proliferator-activated receptor-β/δ Human
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  • Testicular receptor 4 in Human [GtoPdb: 614] [UniProtKB: P49116]
  • This target only has 0 pki data point
  • 0
21 CHEMBL38_lig_chart_21 Testicular receptor 4 Human
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  • TLX in Human [GtoPdb: 615] [UniProtKB: Q9Y466]
  • This target only has 0 pki data point
  • 0
22 CHEMBL38_lig_chart_22 TLX Human
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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
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: Q548M1Q7BGE6]
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: P10809P61604]
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 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]
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 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 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 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 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 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 F 8.3 pEC50 5 nM EC50 J. Med. Chem. (1999) 42: 4961-4969 [PMID:10585206]
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 of retinoic acid receptor RAR alpha B 8.3 pEC50 5 nM EC50 Bioorg. Med. Chem. Lett. (1995) 5: 523-527
ChEMBL Transcriptional activation for RAR alpha receptor B 8.3 pEC50 5 nM EC50 Bioorg. Med. Chem. Lett. (1994) 4: 1447-1452
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