Target Poor or Non Binder(s) Information

Target General Information

Target ID

T53381

Target Info

Target Name

Adrenergic receptor alpha-1D (ADRA1D)

Synonyms

Alpha-adrenergic receptor 1a; Alpha-1D adrenoreceptor; Alpha-1D adrenoceptor; Alpha-1D adrenergic receptor; Alpha adrenergic receptor 1a; Alpha 1D-adrenoreceptor; Alpha 1D-adrenoceptor; ADRA1A

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Target Type

Successful Target

Gene Name

ADRA1D

Biochemical Class

GPCR rhodopsin

UniProt ID

P25100

Poor Binders of This Target (in total, 2 binders)

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Compound Name

2-[[4-[2-[4-(2-Methylphenyl)piperazin-1-yl]ethyl]phenyl]methyl]isoindole-1,3-dione

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Investigative

Compound Info

Synonyms

CHEMBL3740042; BDBM50500009

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Activity

IC50 = 80550 nM

[1]

Compound Name

N-(5-Bromoquinoxalin-6-yl)-4,5-dihydro-1,3-oxazol-2-amine

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Investigative

Compound Info

Synonyms

CHEMBL73164; BDBM50213346

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Activity

Ki = 102329.3 nM

[2]

Non Binders of This Target (in total, 23 non binders)

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Compound Name

(4R,5S)-4-(3,4-Difluorophenyl)-N-[3-[4-(4-fluorophenyl)piperidin-1-yl]propyl]-5-methyl-2-oxo-1,3-oxazolidine-3-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL2112365; BDBM50218551

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Activity

Ki = 253122 nM

[3]

Compound Name

3-[2-[4-(4-Cyclohexylphenyl)piperazin-1-yl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione

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Investigative

Compound Info

Synonyms

CHEMBL99397

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Activity

Ki = 1.00E+12 nM

[4]

Compound Name

2-Methyl-3-[2-[4-(4-propan-2-ylphenyl)piperazin-1-yl]ethyl]-5H-pyrimido[5,4-b]indol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL100481

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Activity

Ki = 5.89E+14 nM

[4]

Compound Name

3-[2-[4-(4-Butylphenyl)piperazin-1-yl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione

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Investigative

Compound Info

Synonyms

CHEMBL330198; BDBM50418772

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Activity

Ki = 4.07E+15 nM

[4]

Compound Name

3-[2-(2,4,4a,5-Tetrahydro-1H-pyrazino[2,1-c][1,4]benzoxazin-3-yl)ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione

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Investigative

Compound Info

Synonyms

CHEMBL95605

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Activity

Ki = 7.94E+15 nM

[4]

Compound Name

3-[2-[4-(4-Propan-2-ylphenyl)piperazin-1-yl]ethyl]-1H-[1]benzothiolo[3,2-d]pyrimidine-2,4-dione

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Investigative

Compound Info

Synonyms

CHEMBL95986

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Activity

Ki = 7.94E+15 nM

[4]

Compound Name

3-[2-[4-(4-Tert-butylphenyl)piperazin-1-yl]ethyl]-2-methyl-5H-pyrimido[5,4-b]indol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL317556

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Activity

Ki = 1.02E+16 nM

[4]

Compound Name

3-[2-[4-(4-Butan-2-ylphenyl)piperazin-1-yl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione

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Investigative

Compound Info

Synonyms

CHEMBL95191; BDBM50418746

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Activity

Ki = 1.66E+16 nM

[4]

Compound Name

3-[2-[4-(4-Propan-2-ylphenyl)piperazin-1-yl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione

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Investigative

Compound Info

Synonyms

CHEMBL100434; BDBM50418771

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Activity

Ki = 2.82E+16 nM

[4]

Compound Name

3-[2-[4-(4-Tert-butylphenyl)piperazin-1-yl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione

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Investigative

Compound Info

Synonyms

CHEMBL319972; BDBM50418745

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Activity

Ki = 5.01E+16 nM

[4]

Compound Name

3-{3-[4-(2-Methoxyphenyl)piperazin-1-yl]propyl}-3,5-dihydro-4h-pyrimido[5,4-b]indol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL98807; CTK7B1317

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Activity

Ki = 6.17E+16 nM

[4]

Compound Name

2-Ethyl-3-[3-[4-(2-methoxyphenyl)piperazin-1-yl]propyl]-5H-pyrimido[5,4-b]indol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL99979

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Activity

Ki = 7.94E+16 nM

[4]

Compound Name

2-[4-[4-[2-(2,4-Dioxo-1,5-dihydropyrimido[5,4-b]indol-3-yl)ethyl]piperazin-1-yl]phenyl]acetonitrile

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Investigative

Compound Info

Synonyms

CHEMBL319345

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Activity

Ki = 1.00E+17 nM

[4]

Compound Name

2-Ethyl-3-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-5H-pyrimido[5,4-b]indol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL329971

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Activity

Ki = 1.45E+17 nM

[4]

Compound Name

3-[2-[4-(2-Ethoxyphenyl)piperazin-1-yl]ethyl]-5H-pyrimido[5,4-b]indol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL433014

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Activity

Ki = 1.66E+17 nM

[4]

Compound Name

3-[2-[4-(2-Chlorophenyl)-1-piperazinyl]ethyl]-1H-pyrimido[5,4-b]indole-2,4(3H,5H)-dione

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Investigative

Compound Info

Synonyms

CHEMBL57163; SCHEMBL12648691; BDBM50006954; 2-{2-[4-(2-Chloro-phenyl)-piperazin-1-yl]-ethyl}-4,9-dihydro-2,4,9-triaza-fluorene-1,3-dione; 3-{2-[4-(2-Chloro-phenyl)-piperazin-1-yl]-ethyl}-1,5-dihydro-pyrimido[5,4-b]indole-2,4-dione

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Activity

Ki = 2.75E+17 nM

[4]

Compound Name

3-[3-[4-(2-Methoxyphenyl)piperazin-1-yl]propyl]-2-methyl-5H-pyrimido[5,4-b]indol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL316677

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Activity

Ki = 3.89E+17 nM

[4]

Compound Name

3-[2-[4-(2-Ethoxyphenyl)piperazin-1-yl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione

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Investigative

Compound Info

Synonyms

CHEMBL317555

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Activity

Ki = 6.31E+17 nM

[4]

Compound Name

3-[2-[4-(2-Methoxyphenyl)piperidin-1-yl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione

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Investigative

Compound Info

Synonyms

CHEMBL99761

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Activity

Ki = 1.07E+18 nM

[4]

Compound Name

3-[2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl]-5H-pyrimido[5,4-b]indol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL433203

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Activity

Ki = 1.38E+18 nM

[4]

Compound Name

3-[2-[4-(2-Hydroxyphenyl)piperazin-1-yl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione

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Investigative

Compound Info

Synonyms

CHEMBL99879

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Activity

Ki = 1.58E+18 nM

[4]

Compound Name

3-[2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl]-2-methyl-5H-pyrimido[5,4-b]indol-4-one

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Investigative

Compound Info

Synonyms

CHEMBL99142; BDBM50476084

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Activity

Ki = 2.45E+18 nM

[4]

Compound Name

3-[2-[4-(2-Methoxyphenyl)-1-piperazinyl]ethyl]-1,5-dihydropyrimido[5,4-b]indole-2,4-dione

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Investigative

Compound Info

Synonyms

3-MPPI; CHEMBL301707; NCGC00024664-01; Tocris-0581; Biomol-NT_000127; BPBio1_000310; HMS3266M22; HMS3411G12; HMS3675G12; BDBM50006952; ZINC29486259; AKOS024458570; NCGC00024664-02; NCGC00024664-03; B6361; SR-01000597636; J-006367; SR-01000597636-1; BRD-K62581435-001-01-2; BRD-K62581435-001-02-0; Q27195293

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Activity

Ki = 2.75E+18 nM

[4]

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References

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REF 1

Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as alpha1A/1D-AR subselective antagonists for BPH. Bioorg Med Chem. 2015 Dec 15;23(24):7735-42.

REF 2

Pharmacological evaluation of UK-14,304 analogs at cloned human alpha adrenergic receptors. Bioorg Med Chem Lett. 1995 Oct 5;5(19):2255-8.

REF 3

Determination of the relative and absolute stereochemistry of a potent and alpha1A-selective adrenoceptor antagonist. Bioorg Med Chem Lett. 2000 Dec 18;10(24):2705-7.

REF 4

New pyrimido[5,4-b]indoles as ligands for alpha(1)-adrenoceptor subtypes. J Med Chem. 2003 Jul 3;46(14):2877-94.

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