                         SEQUENCE LISTING

<110>  Janssen Pharmaceutica NV
 
<120>  ALKYL LINKED QUINOLINYL MODULATORS OF RORyt

<130>  PRD-3315USNP

<140>  Application Number 

<141>  2014-10-15

<160>  9     

<170>  PatentIn version 3.5

<210>  1
<211>  3054
<212>  DNA
<213>  Homo sapiens

<400>  1
agagagctag gtgcagagct tcaggctgag gcgctgctga gagggcctcg ccccgcctct       60

gccgccagct gcaccccact cctggaccac cccctgctga gaaggacagg gagccaaggc      120

cggcagagcc aaggctcagt catgagaaca caaattgaag tgatcccttg caaaatctgt      180

ggggacaagt cgtctgggat ccactacggg gttatcacct gtgaggggtg caagggcttc      240

ttccgccgga gccagcgctg taacgcggcc tactcctgca cccgtcagca gaactgcccc      300

atcgaccgca ccagccgaaa ccgatgccag cactgccgcc tgcagaaatg cctggcgctg      360

ggcatgtccc gagatgctgt caagttcggc cgcatgtcca agaagcagag ggacagcctg      420

catgcagaag tgcagaaaca gctgcagcag cggcaacagc agcaacagga accagtggtc      480

aagacccctc cagcaggggc ccaaggagca gataccctca cctacacctt ggggctccca      540

gacgggcagc tgcccctggg ctcctcgcct gacctgcctg aggcttctgc ctgtccccct      600

ggcctcctga aagcctcagg ctctgggccc tcatattcca acaacttggc caaggcaggg      660

ctcaatgggg cctcatgcca ccttgaatac agccctgagc ggggcaaggc tgagggcaga      720

gagagcttct atagcacagg cagccagctg acccctgacc gatgtggact tcgttttgag      780

gaacacaggc atcctgggct tggggaactg ggacagggcc cagacagcta cggcagcccc      840

agtttccgca gcacaccgga ggcaccctat gcctccctga cagagataga gcacctggtg      900

cagagcgtct gcaagtccta cagggagaca tgccagctgc ggctggagga cctgctgcgg      960

cagcgctcca acatcttctc ccgggaggaa gtgactggct accagaggaa gtccatgtgg     1020

gagatgtggg aacggtgtgc ccaccacctc accgaggcca ttcagtacgt ggtggagttc     1080

gccaagaggc tctcaggctt tatggagctc tgccagaatg accagattgt gcttctcaaa     1140

gcaggagcaa tggaagtggt gctggttagg atgtgccggg cctacaatgc tgacaaccgc     1200

acggtctttt ttgaaggcaa atacggtggc atggagctgt tccgagcctt gggctgcagc     1260

gagctcatca gctccatctt tgacttctcc cactccctaa gtgccttgca cttttccgag     1320

gatgagattg ccctctacac agcccttgtt ctcatcaatg cccatcggcc agggctccaa     1380

gagaaaagga aagtagaaca gctgcagtac aatctggagc tggcctttca tcatcatctc     1440

tgcaagactc atcgccaaag catcctggca aagctgccac ccaaggggaa gcttcggagc     1500

ctgtgtagcc agcatgtgga aaggctgcag atcttccagc acctccaccc catcgtggtc     1560

caagccgctt tccctccact ctacaaggag ctcttcagca ctgaaaccga gtcacctgtg     1620

gggctgtcca agtgacctgg aagagggact ccttgcctct ccctatggcc tgctggccca     1680

cctccctgga ccccgttcca ccctcaccct tttcctttcc catgaaccct ggagggtggt     1740

ccccaccagc tctttggaag tgagcagatg ctgcggctgg ctttctgtca gcaggccggc     1800

ctggcagtgg gacaatcgcc agagggtggg gctggcagaa caccatctcc agcctcagct     1860

ttgacctgtc tcatttccca tattccttca cacccagctt ctggaaggca tggggtggct     1920

gggatttaag gacttctggg ggaccaagac atcctcaaga aaacaggggc atccagggct     1980

ccctggatga atagaatgca attcattcag aagctcagaa gctaagaata agcctttgaa     2040

atacctcatt gcatttccct ttgggcttcg gcttggggag atggatcaag ctcagagact     2100

ggcagtgaga gcccagaagg acctgtataa aatgaatctg gagctttaca ttttctgcct     2160

ctgccttcct cccagctcag caaggaagta tttgggcacc ctacccttta cctggggtct     2220

aaccaaaaat ggatgggatg aggatgagag gctggagata attgttttat gggatttggg     2280

tgtgggacta gggtacaatg aaggccaaga gcatctcaga catagagtta aaactcaaac     2340

ctcttatgtg cactttaaag atagacttta ggggctggca caaatctgat cagagacaca     2400

tatccataca caggtgaaac acatacagac tcaacagcaa tcatgcagtt ccagagacac     2460

atgaacctga cacaatctct cttatccttg aggccacagc ttggaggagc ctagaggcct     2520

caggggaaag tcccaatcct gagggaccct cccaaacatt tccatggtgc tccagtccac     2580

tgatcttggg tctggggtga tccaaatacc accccagctc cagctgtctt ctaccactag     2640

aagacccaag agaagcagaa gtcgctcgca ctggtcagtc ggaaggcaag atcagatcct     2700

ggaggacttt cctggcctgc ccgccagccc tgctcttgtt gtggagaagg aagcagatgt     2760

gatcacatca ccccgtcatt gggcaccgct gactccagca tggaggacac cagggagcag     2820

ggcctgggcc tgtttcccca gctgtgatct tgcccagaac ctctcttggc ttcataaaca     2880

gctgtgaacc ctcccctgag ggattaacag caatgatggg cagtcgtgga gttggggggg     2940

ttgggggtgg gattgtgtcc tctaagggga cgggttcatc tgagtaaaca taaaccccaa     3000

cttgtgccat tctttataaa atgattttaa aggcaaaaaa aaaaaaaaaa aaaa           3054


<210>  2
<211>  786
<212>  DNA
<213>  Homo sapiens

<400>  2
agcacaccgg aggcacccta tgcctccctg acagagatag agcacctggt gcagagcgtc       60

tgcaagtcct acagggagac atgccagctg cggctggagg acctgctgcg gcagcgctcc      120

aacatcttct cccgggagga agtgactggc taccagagga agtccatgtg ggagatgtgg      180

gaacggtgtg cccaccacct caccgaggcc attcagtacg tggtggagtt cgccaagagg      240

ctctcaggct ttatggagct ctgccagaat gaccagattg tgcttctcaa agcaggagca      300

atggaagtgg tgctggttag gatgtgccgg gcctacaatg ctgacaaccg cacggtcttt      360

tttgaaggca aatacggtgg catggagctg ttccgagcct tgggctgcag cgagctcatc      420

agctccatct ttgacttctc ccactcccta agtgccttgc acttttccga ggatgagatt      480

gccctctaca cagcccttgt tctcatcaat gcccatcggc cagggctcca agagaaaagg      540

aaagtagaac agctgcagta caatctggag ctggcctttc atcatcatct ctgcaagact      600

catcgccaaa gcatcctggc aaagctgcca cccaagggga agcttcggag cctgtgtagc      660

cagcatgtgg aaaggctgca gatcttccag cacctccacc ccatcgtggt ccaagccgct      720

ttccctccac tctacaagga gctcttcagc actgaaaccg agtcacctgt ggggctgtcc      780

aagtga                                                                 786


<210>  3
<211>  7
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  TurboTEV protease cleavage site

<400>  3

Glu Asn Leu Tyr Phe Gln Gly 
1               5           


<210>  4
<211>  283
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  Construct used in the Thermofluor assay

<400>  4

Met Ala His His His His His His Ala Gly Gly Ala Glu Asn Leu Tyr 
1               5                   10                  15      


Phe Gln Gly Ala Met Asp Ser Thr Pro Glu Ala Pro Tyr Ala Ser Leu 
            20                  25                  30          


Thr Glu Ile Glu His Leu Val Gln Ser Val Cys Lys Ser Tyr Arg Glu 
        35                  40                  45              


Thr Cys Gln Leu Arg Leu Glu Asp Leu Leu Arg Gln Arg Ser Asn Ile 
    50                  55                  60                  


Phe Ser Arg Glu Glu Val Thr Gly Tyr Gln Arg Lys Ser Met Trp Glu 
65                  70                  75                  80  


Met Trp Glu Arg Cys Ala His His Leu Thr Glu Ala Ile Gln Tyr Val 
                85                  90                  95      


Val Glu Phe Ala Lys Arg Leu Ser Gly Phe Met Glu Leu Cys Gln Asn 
            100                 105                 110         


Asp Gln Ile Val Leu Leu Lys Ala Gly Ala Met Glu Val Val Leu Val 
        115                 120                 125             


Arg Met Cys Arg Ala Tyr Asn Ala Asp Asn Arg Thr Val Phe Phe Glu 
    130                 135                 140                 


Gly Lys Tyr Gly Gly Met Glu Leu Phe Arg Ala Leu Gly Cys Ser Glu 
145                 150                 155                 160 


Leu Ile Ser Ser Ile Phe Asp Phe Ser His Ser Leu Ser Ala Leu His 
                165                 170                 175     


Phe Ser Glu Asp Glu Ile Ala Leu Tyr Thr Ala Leu Val Leu Ile Asn 
            180                 185                 190         


Ala His Arg Pro Gly Leu Gln Glu Lys Arg Lys Val Glu Gln Leu Gln 
        195                 200                 205             


Tyr Asn Leu Glu Leu Ala Phe His His His Leu Cys Lys Thr His Arg 
    210                 215                 220                 


Gln Ser Ile Leu Ala Lys Leu Pro Pro Lys Gly Lys Leu Arg Ser Leu 
225                 230                 235                 240 


Cys Ser Gln His Val Glu Arg Leu Gln Ile Phe Gln His Leu His Pro 
                245                 250                 255     


Ile Val Val Gln Ala Ala Phe Pro Pro Leu Tyr Lys Glu Leu Phe Ser 
            260                 265                 270         


Thr Glu Thr Glu Ser Pro Val Gly Leu Ser Lys 
        275                 280             


<210>  5
<211>  6
<212>  PRT
<213>  Homo sapiens

<400>  5

Leu Tyr Lys Glu Leu Phe 
1               5       


<210>  6
<211>  6
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  mutated AF2 domain

<400>  6

Leu Phe Lys Glu Leu Phe 
1               5       


<210>  7
<211>  786
<212>  DNA
<213>  Artificial Sequence

<220>
<223>  LBD with mutated AF2 domain

<400>  7
agcacaccgg aggcacccta tgcctccctg acagagatag agcacctggt gcagagcgtc       60

tgcaagtcct acagggagac atgccagctg cggctggagg acctgctgcg gcagcgctcc      120

aacatcttct cccgggagga agtgactggc taccagagga agtccatgtg ggagatgtgg      180

gaacggtgtg cccaccacct caccgaggcc attcagtacg tggtggagtt cgccaagagg      240

ctctcaggct ttatggagct ctgccagaat gaccagattg tgcttctcaa agcaggagca      300

atggaagtgg tgctggttag gatgtgccgg gcctacaatg ctgacaaccg cacggtcttt      360

tttgaaggca aatacggtgg catggagctg ttccgagcct tgggctgcag cgagctcatc      420

agctccatct ttgacttctc ccactcccta agtgccttgc acttttccga ggatgagatt      480

gccctctaca cagcccttgt tctcatcaat gcccatcggc cagggctcca agagaaaagg      540

aaagtagaac agctgcagta caatctggag ctggcctttc atcatcatct ctgcaagact      600

catcgccaaa gcatcctggc aaagctgcca cccaagggga agcttcggag cctgtgtagc      660

cagcatgtgg aaaggctgca gatcttccag cacctccacc ccatcgtggt ccaagccgct      720

ttccctccac tcttcaagga gctcttcagc actgaaaccg agtcacctgt ggggctgtcc      780

aagtga                                                                 786


<210>  8
<211>  261
<212>  PRT
<213>  Homo sapiens

<400>  8

Ser Thr Pro Glu Ala Pro Tyr Ala Ser Leu Thr Glu Ile Glu His Leu 
1               5                   10                  15      


Val Gln Ser Val Cys Lys Ser Tyr Arg Glu Thr Cys Gln Leu Arg Leu 
            20                  25                  30          


Glu Asp Leu Leu Arg Gln Arg Ser Asn Ile Phe Ser Arg Glu Glu Val 
        35                  40                  45              


Thr Gly Tyr Gln Arg Lys Ser Met Trp Glu Met Trp Glu Arg Cys Ala 
    50                  55                  60                  


His His Leu Thr Glu Ala Ile Gln Tyr Val Val Glu Phe Ala Lys Arg 
65                  70                  75                  80  


Leu Ser Gly Phe Met Glu Leu Cys Gln Asn Asp Gln Ile Val Leu Leu 
                85                  90                  95      


Lys Ala Gly Ala Met Glu Val Val Leu Val Arg Met Cys Arg Ala Tyr 
            100                 105                 110         


Asn Ala Asp Asn Arg Thr Val Phe Phe Glu Gly Lys Tyr Gly Gly Met 
        115                 120                 125             


Glu Leu Phe Arg Ala Leu Gly Cys Ser Glu Leu Ile Ser Ser Ile Phe 
    130                 135                 140                 


Asp Phe Ser His Ser Leu Ser Ala Leu His Phe Ser Glu Asp Glu Ile 
145                 150                 155                 160 


Ala Leu Tyr Thr Ala Leu Val Leu Ile Asn Ala His Arg Pro Gly Leu 
                165                 170                 175     


Gln Glu Lys Arg Lys Val Glu Gln Leu Gln Tyr Asn Leu Glu Leu Ala 
            180                 185                 190         


Phe His His His Leu Cys Lys Thr His Arg Gln Ser Ile Leu Ala Lys 
        195                 200                 205             


Leu Pro Pro Lys Gly Lys Leu Arg Ser Leu Cys Ser Gln His Val Glu 
    210                 215                 220                 


Arg Leu Gln Ile Phe Gln His Leu His Pro Ile Val Val Gln Ala Ala 
225                 230                 235                 240 


Phe Pro Pro Leu Tyr Lys Glu Leu Phe Ser Thr Glu Thr Glu Ser Pro 
                245                 250                 255     


Val Gly Leu Ser Lys 
            260     


<210>  9
<211>  261
<212>  PRT
<213>  Artificial Sequence

<220>
<223>  LBD with mutated AF2 domain

<400>  9

Ser Thr Pro Glu Ala Pro Tyr Ala Ser Leu Thr Glu Ile Glu His Leu 
1               5                   10                  15      


Val Gln Ser Val Cys Lys Ser Tyr Arg Glu Thr Cys Gln Leu Arg Leu 
            20                  25                  30          


Glu Asp Leu Leu Arg Gln Arg Ser Asn Ile Phe Ser Arg Glu Glu Val 
        35                  40                  45              


Thr Gly Tyr Gln Arg Lys Ser Met Trp Glu Met Trp Glu Arg Cys Ala 
    50                  55                  60                  


His His Leu Thr Glu Ala Ile Gln Tyr Val Val Glu Phe Ala Lys Arg 
65                  70                  75                  80  


Leu Ser Gly Phe Met Glu Leu Cys Gln Asn Asp Gln Ile Val Leu Leu 
                85                  90                  95      


Lys Ala Gly Ala Met Glu Val Val Leu Val Arg Met Cys Arg Ala Tyr 
            100                 105                 110         


Asn Ala Asp Asn Arg Thr Val Phe Phe Glu Gly Lys Tyr Gly Gly Met 
        115                 120                 125             


Glu Leu Phe Arg Ala Leu Gly Cys Ser Glu Leu Ile Ser Ser Ile Phe 
    130                 135                 140                 


Asp Phe Ser His Ser Leu Ser Ala Leu His Phe Ser Glu Asp Glu Ile 
145                 150                 155                 160 


Ala Leu Tyr Thr Ala Leu Val Leu Ile Asn Ala His Arg Pro Gly Leu 
                165                 170                 175     


Gln Glu Lys Arg Lys Val Glu Gln Leu Gln Tyr Asn Leu Glu Leu Ala 
            180                 185                 190         


Phe His His His Leu Cys Lys Thr His Arg Gln Ser Ile Leu Ala Lys 
        195                 200                 205             


Leu Pro Pro Lys Gly Lys Leu Arg Ser Leu Cys Ser Gln His Val Glu 
    210                 215                 220                 


Arg Leu Gln Ile Phe Gln His Leu His Pro Ile Val Val Gln Ala Ala 
225                 230                 235                 240 


Phe Pro Pro Leu Phe Lys Glu Leu Phe Ser Thr Glu Thr Glu Ser Pro 
                245                 250                 255     


Val Gly Leu Ser Lys 
            260     


