General Information of the Protein
Protein ID
PT01430
Protein Name
3-oxo-5-alpha-steroid 4-dehydrogenase 1
Secondarily
Protein Name
SR type 1
Steroid 5-alpha-reductase 1
Gene Name
SRD5A1
Sequence
MATATGVAEERLLAALAYLQCAVGCAVFARNRQTNSVYGRHALPSHRLRVPARAAWVVQELPSLALPLYQYASESAPRLRSAPNCILLAMFLVHYGHRCLIYPFLMRGGKPMPLLACTMAIMFCTCNGYLQSRYLSHCAVYADDWVTDPRFLIGFGLWLTGMLINIHSDHILRNLRKPGDTGYKIPRGGLFEYVTAANYFGEIMEWCGYALASWSVQGAAFAFFTFCFLSGRAKEHHEWYLRKFEEYPKFRKIIIPFLF
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Oxidoreductase
Function
Converts testosterone into 5-alpha-dihydrotestosterone and progesterone or corticosterone into their corresponding 5-alpha-3-oxosteroids. It plays a central role in sexual differentiation and androgen physiology.
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Uniprot ID
Primary ID:
P18405

Secondarily ID:
B2R7Q1
Q9UHY4
Q9UP36
Q9UP37
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Ensembl ID
ENSG00000145545
HGNC ID
HGNC:11284
Subcellular Location
Microsome membrane
Endoplasmic reticulum membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0430474
4-methyl-8-chloro-1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one
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C14H14ClNO
 2
1
IC50 = 7.6 nM
   TI
   LI
   LO
   TS
2
Ki = 2.7 nM
   TI
   LI
   LO
   TS
CP0451955
4,6-dimethyl-8-chloro-1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one
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C15H16ClNO
 1
1
IC50 = 8.5 nM
   TI
   LI
   LO
   TS
CP0486419
6-methyl-8-chloro-1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one
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C14H14ClNO
 1
1
IC50 = 14.4 nM
   TI
   LI
   LO
   TS
CP0511522
4,5-dimethyl-8-chloro-1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one
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C15H16ClNO
 1
1
IC50 = 15.6 nM
   TI
   LI
   LO
   TS
CP0534577
4,6-dimethyl-8-methyl-1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one
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C16H19NO
 1
1
IC50 = 15.8 nM
   TI
   LI
   LO
   TS
CP0395403
4,8-Dimethyl-1,2,5,6-tetrahydro-pyrido[1,2-a]quinolin-3-one
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C15H17NO
 2
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
2
Ki = 5.8 nM
   TI
   LI
   LO
   TS
CP0365139
8-Chloro-1,2,5,6-tetrahydro-pyrido[1,2-a]quinolin-3-one
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C13H12ClNO
 1
1
IC50 = 49 nM
   TI
   LI
   LO
   TS
CP0524542
4-(alpha)methyl-8-methyl-3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C15H17NO
 1
1
IC50 = 137 nM
   TI
   LI
   LO
   TS
CP0497188
4-(alpha)methyl-8-chloro-3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C14H14ClNO
 1
1
IC50 = 141 nM
   TI
   LI
   LO
   TS
CP0480622
8-methyl-3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C14H15NO
 1
1
IC50 = 176 nM
   TI
   LI
   LO
   TS
CP0466748
4-Methyl-1,2,5,6-tetrahydro-pyrido[1,2-a]quinolin-3-one
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C14H15NO
 1
1
IC50 = 185 nM
   TI
   LI
   LO
   TS
CP0430600
6-(alpha)methyl-8-chloro-3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C14H14ClNO
 1
1
IC50 = 188 nM
   TI
   LI
   LO
   TS
CP0485860
1-methyl-8-chloro-1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one
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C14H14ClNO
 1
1
IC50 = 204 nM
   TI
   LI
   LO
   TS
CP0207553
1,2,5,6-Tetrahydro-pyrido[1,2-a]quinolin-3-one
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C13H13NO
 1
1
IC50 = 298 nM
   TI
   LI
   LO
   TS
CP0498894
4-(beta)methyl-8-methyl-3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C15H17NO
 1
1
IC50 = 312 nM
   TI
   LI
   LO
   TS
CP0486447
8-Methyl-1,2,5,6-tetrahydro-pyrido[1,2-a]quinolin-3-one
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C14H15NO
 1
1
IC50 = 376 nM
   TI
   LI
   LO
   TS
CP0404279
8-chloro-3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C13H12ClNO
 1
1
IC50 = 459 nM
   TI
   LI
   LO
   TS
CP0497227
4-Methyl-5,6-dihydro-pyrido[1,2-a]quinolin-3-one
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C14H13NO
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0430492
8-Chloro-5-methyl-5,6-dihydro-pyrido[1,2-a]quinolin-3-one
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C14H12ClNO
 1
1
IC50 = 1880 nM
   TI
   LI
   LO
   TS
CP0510861
4-(alpha)methyl-3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C14H15NO
 1
1
IC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0395416
4-(beta)methyl-3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C14H15NO
 1
1
IC50 = 4300 nM
   TI
   LI
   LO
   TS
CP0096672
3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C13H13NO
 1
1
IC50 = 5130 nM
   TI
   LI
   LO
   TS
CP0461072
5-methyl-8-chloro-1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one
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C14H14ClNO
 1
1
IC50 = 5310 nM
   TI
   LI
   LO
   TS
CP0392648
6-methyl-8-methyl-1,2,5,6-tetrahydro pyrido[1,2-a]quinolin-3-one
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C15H17NO
 1
1
IC50 = 5310 nM
   TI
   LI
   LO
   TS
CP0405900
5-(alpha)methyl-8-chloro-3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C14H14ClNO
 1
1
IC50 = 9100 nM
   TI
   LI
   LO
   TS
CP0043937
(17beta-(N-tert-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one
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C23H36N2O2
 1
1
Ki = 366 nM
   TI
   LI
   LO
   TS
CP0366718
5-methoxy-6-phenylmethoxy-1H-indole-2-carboxylic acid
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C17H15NO4
 1
1
Ki = 460 nM
   TI
   LI
   LO
   TS
CP0408546
5-methoxy-1-methyl-6-phenylmethoxyindole-2-carboxylic acid
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C18H17NO4
 1
1
Ki = 500 nM
   TI
   LI
   LO
   TS
CP0223232
5-Benzyloxy-1H-indole-2-carboxylic acid
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C16H13NO3
 1
1
Ki > 2500 nM
   TI
   LI
   LO
   TS
CP0375173
4-Benzyloxy-1H-indole-2-carboxylic acid
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C16H13NO3
 1
1
Ki > 2500 nM
   TI
   LI
   LO
   TS
CP0447964
1-methyl-5-phenylmethoxyindole-2-carboxylic acid
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C17H15NO3
 1
1
Ki > 2500 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0150571
(1S,3aS,3bS,5aR,9aR,9bS,11aS)-N,N-diethyl-6,9a,11a-trimethyl-7-oxo-2,3,3a,3b,4,5,5a,8,9,9b,10,11-dodecahydro-1H-indeno[5,4-f]quinoline-1-carboxamide
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C24H40N2O2
 3
1 IC50 = 1.7 nM
2 Ki = 3 nM
3 Ki = 5 nM
CP0345390
4-(3-{3-[(4-Isobutyl-benzyl)-(4-isobutyl-phenyl)-amino]-benzoyl}-indol-1-yl)-butyric acid
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C40H44N2O3
 1
1 IC50 = 38 nM
CP0365139
8-Chloro-1,2,5,6-tetrahydro-pyrido[1,2-a]quinolin-3-one
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C13H12ClNO
 1
1 IC50 = 49 nM
CP0043937
(17beta-(N-tert-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one
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C23H36N2O2
 5
1 IC50 = 52 nM
2 IC50 = 150 nM
3 IC50 = 500 nM
4 Ki = 100 nM
5 Ki = 150 nM
CP0207553
1,2,5,6-Tetrahydro-pyrido[1,2-a]quinolin-3-one
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C13H13NO
 1
1 IC50 = 298 nM
CP0112369
(8S,9S,10R,13S,14S,17S)-17-(tert-butylcarbamoyl)-10,13-dimethyl-2,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene-3-carboxylic acid
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C25H37NO3
 5
1 IC50 = 1600 nM
2 IC50 > 1000 nM
3 Ki = 410 nM
4 Ki = 1600 nM
5 Ki > 5000 nM
CP0096672
3,4,5,6-Tetrahydrobenzo[c]quinolizin-3-(4aH)-one
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C13H13NO
 1
1 IC50 = 5130 nM
CP0223232
5-Benzyloxy-1H-indole-2-carboxylic acid
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C16H13NO3
 1
1 Ki > 2500 nM
CP0177563
4-(3-(4-(N-methylacetamido)phenyl)pentan-3-yl)phenyl dibenzylcarbamate
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C35H38N2O3
 1
1 Km = 9100 nM
Clinical Information about the Protein
Target 1 ( Steroid 5-alpha-reductase 1 (SRD5A1) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Acne vulgaris [ICD-11: ED80]
Discontinued Drug(s) 1 Discontinued Drug  1
1 AS-601811 Discontinued in Phase 1
Acne vulgaris