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Go to the GPCR, ligand, or experimental data tables.
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GPCR

Name	5-hydroxytryptamine receptor 1A
Species	Rattus norvegicus (Rat)
Gene	Htr1a
Synonym	5-HT1A receptor 5-hydroxytryptamine (serotonin) receptor 1A, G protein-coupled 5-HT1A ADRB2RL1 ADRBRL1 5-HT-1A Gpcr18 Serotonin receptor 1A [ Show all ]
Disease	N/A for non-human GPCRs
Length	422
Amino acid sequence	MDVFSFGQGNNTTASQEPFGTGGNVTSISDVTFSYQVITSLLLGTLIFCAVLGNACVVAAIALERSLQNVANYLIGSLAVTDLMVSVLVLPMAALYQVLNKWTLGQVTCDLFIALDVLCCTSSILHLCAIALDRYWAITDPIDYVNKRTPRRAAALISLTWLIGFLISIPPMLGWRTPEDRSDPDACTISKDHGYTIYSTFGAFYIPLLLMLVLYGRIFRAARFRIRKTVRKVEKKGAGTSLGTSSAPPPKKSLNGQPGSGDWRRCAENRAVGTPCTNGAVRQGDDEATLEVIEVHRVGNSKEHLPLPSESGSNSYAPACLERKNERNAEAKRKMALARERKTVKTLGIIMGTFILCWLPFFIVALVLPFCESSCHMPALLGAIINWLGYSNSLLNPVIYAYFNKDFQNAFKKIIKCKFCRR
UniProt	P19327
Protein Data Bank	N/A
GPCR-HGmod model	N/A
3D structure model	No available structures or models
BioLiP	N/A
Therapeutic Target Database	N/A
ChEMBL	CHEMBL273
IUPHAR	1
DrugBank	N/A

Ligand

Name	8-OH-Dpat
Molecular formula	C16H25NO
IUPAC name	7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol
Molecular weight	247.382
Hydrogen bond acceptor	2
Hydrogen bond donor	1
XlogP	4.1
Synonyms	1-Naphthalenol, 7-(dipropylamino)-5,6,7,8-tetrahydro- 8-OH-DPAT,(+) ASXGJMSKWNBENU-UHFFFAOYSA-N CHEBI:73364 GTPL31 MolPort-044-830-676 PDSP2_000765 SR-01000075571-7 122341-76-8 8-HYDROXY-2-(DI-n-PROPYLAMINO)TETRALIN 8OH-DPAT Biomol-NT_000095 cid_1220 J-007140 NCGC00015493-06 S(-)-8-Hydroxy-DPAT hydrobromide (+)-8-Hydroxy-2-(dipropylamino)tetralin (+/-)-8-Hydroxy-DPAT hydrobromide AC1Q7AL7 BRD-A48015106-004-03-0 D0O3GF LS-94994 NCGC00024986-02 S8447 1-Naphthalenol,7-(dipropylamino)-5,6,7,8-tetrahydro- 7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol 8-OH-DPAT,(-) BCP25681 GTPL7 NCGC00015493-04 Ro-31-8220 in solution [3H]-8-OH-DPAT 142272-99-9 8-Hydroxy-DPAT AC1L1AZN BPBio1_001354 CS-0043224 L000086 NCGC00024635-02 S(-)-8-HYDROXY-DPAT HYDROBROMIDE PARTIAL 5-HT1A SECROT (+-)-8-OH-DPAT 5,6,7,8-tetrahydro-7-(dipropylamino)-1-naphthalenol 8-OH-DPAT (8-Hydroxy-DPAT) AKOS030627213 CCG-204665 dl-8-Hydroxy-2-(dipropylamino)tetralin MFCD00153811 PDSP1_000777 SCHEMBL496783 105558-30-3 78950-78-4 80300-08-9 BDBM21393 CHEMBL56 HY-112061 NCGC00015493-05 RT-015429 [3H]8-OH-DPAT 8-hydroxy-n,n-dipropylaminotetralin AC1Q2XPY BRD-A48015106-001-01-0 CTK5E6257 Lopac0_000576 NCGC00024635-03 S(-)-8-OH-DPAT HBr (+/-)-8-HYDROXY-2-DIPROPYL-AMINOTETRALIN [ Show all ]
Inchi Key	ASXGJMSKWNBENU-UHFFFAOYSA-N
Inchi ID	InChI=1S/C16H25NO/c1-3-10-17(11-4-2)14-9-8-13-6-5-7-16(18)15(13)12-14/h5-7,14,18H,3-4,8-12H2,1-2H3
PubChem CID	1220
ChEMBL	CHEMBL56
IUPHAR	7, 31
BindingDB	21393
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
Basal	12.98 (fM of GTP-gammaS bound) (mg of	PMID12213056	ChEMBL
Basal	13.5 (fM of GTP-gammaS bound) (mg of	PMID12213056	ChEMBL
EC50	0.084 ug kg-1	PMID11728188	ChEMBL
EC50	0.137 ug kg-1	PMID11728188	ChEMBL
ED50	0.099 umol.kg-1	PMID11101361	ChEMBL
Hill coefficient	1.01 -	PMID2521252	ChEMBL
IC50	1.1 nM	PMID7699710, PMID8289207	BindingDB,ChEMBL
IC50	2.1 nM	PMID8960552, PMID8759642	BindingDB,ChEMBL
IC50	2.4 nM	PMID8863806, PMID7912735	BindingDB,ChEMBL
IC50	3.0 nM	PMID3373482	BindingDB
IC50	3.0 nM	PMID2537429	BindingDB,ChEMBL
IC50	3.02 nM	PMID3373482	ChEMBL
IC50	4.0 nM	PMID1433207	BindingDB,ChEMBL
IC50	4.46 nM	PMID2571729	ChEMBL
IC50	4.5 nM	PMID2571729	BindingDB
IC50	8.06 nM	Bioorg. Med. Chem. Lett., (1997) 7:22:2857	ChEMBL
IC50	8.1 nM	N/A	BindingDB
IC50	14.0 nM	PMID9083484	BindingDB,ChEMBL
Increase	91.85 %	PMID12213056	ChEMBL
Kd	2.5 nM	PMID7996545	BindingDB,ChEMBL
Ki	0.27 nM	Bioorg. Med. Chem. Lett., (1993) 3:10:2035	ChEMBL
Ki	0.27 nM	N/A	BindingDB
Ki	0.47 nM	PMID10743959	BindingDB
Ki	0.47 nM	PMID10743959	ChEMBL
Ki	0.5 nM	PMID7861420, PMID7783152, PMID9083484	BindingDB,ChEMBL
Ki	0.5 nM	PMID7783152, PMID9083484	BindingDB
Ki	0.5 nM	PMID9083484	BindingDB
Ki	0.54 nM	N/A	BindingDB
Ki	0.54 nM	Bioorg. Med. Chem. Lett., (1993) 3:10:2035	ChEMBL
Ki	0.63 nM	PMID8230102	BindingDB,ChEMBL
Ki	0.64 nM	PMID17900912	BindingDB,ChEMBL
Ki	0.8 nM	PMID19954866, PMID22133459	BindingDB,ChEMBL
Ki	0.8 nM	PMID26820556	BindingDB
Ki	1.0 nM	PMID2795604, PMID2140413	BindingDB,ChEMBL
Ki	1.02 nM	PMID24050112	ChEMBL
Ki	1.09 nM	Bioorg. Med. Chem. Lett., (1993) 3:10:2035	ChEMBL
Ki	1.1 nM	N/A	BindingDB
Ki	1.18 nM	PMID7731013	BindingDB,ChEMBL
Ki	1.2 nM	PMID15588097, PMID14640559, PMID2965244, PMID12570387, PMID23466604, PMID2521252	BindingDB,ChEMBL
Ki	1.259 nM	PMID9046349	ChEMBL
Ki	1.4 nM	PMID7752194	BindingDB
Ki	1.413 nM	PMID9836623, PMID17300168, PMID17803293	ChEMBL
Ki	1.44 nM	PMID7752194, PMID1535661	BindingDB,ChEMBL
Ki	1.59 nM	PMID8289183	ChEMBL
Ki	1.6 nM	PMID8289183	BindingDB
Ki	1.862 nM	PMID8568799	ChEMBL
Ki	2.0 nM	PMID12877594, PMID12482417, PMID18760923, PMID3543362, PMID12166933	BindingDB,ChEMBL
Ki	2.1 nM	PMID11728188, PMID9836617, PMID2569041, PMID12477356	BindingDB,ChEMBL
Ki	2.26 nM	Bioorg. Med. Chem. Lett., (1993) 3:10:2035	ChEMBL
Ki	2.3 nM	N/A	BindingDB
Ki	2.33 nM	PMID9888842	BindingDB,ChEMBL
Ki	2.8 nM	PMID8410989	BindingDB,ChEMBL
Ki	3.2 nM	PMID1995871	BindingDB
Ki	4.3 nM	PMID8568804, PMID8863803	BindingDB,ChEMBL
Ki	6.17 nM	PMID8584042	BindingDB
Ki	8.13 nM	PMID8584042	BindingDB
Ki	8.7 nM	PMID8340910, PMID8230131, PMID7932553	BindingDB,ChEMBL
Ki	27.0 nM	PMID8398139	BindingDB
Ki	975.0 nM	PMID2140413	BindingDB,ChEMBL
KiAH	1.16 nM	PMID1535661	ChEMBL
Max	23.83 (fM of GTP-gammaS bound) (mg of	PMID12213056	ChEMBL
Max	25.9 (fM of GTP-gammaS bound) (mg of	PMID12213056	ChEMBL