Protein Information

General Information of the Protein

Protein ID	PT01462
Protein Name	Bromodomain-containing protein 4
Secondarily Protein Name	Protein HUNK1
Gene Name	BRD4
Secondarily Gene Name	HUNK1
Sequence	MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQRRESSRPVKPPKKDVPDSQQHPAPEKSSKVSEQLKCCSGILKEMFAKKHAAYAWPFYKPVDVEALGLHDYCDIIKHPMDMSTIKSKLEAREYRDAQEFGADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPEEPVVAVSSPAVPPPTKVVAPPSSSDSSSDSSSDSDSSTDDSEEERAQRLAELQEQLKAVHEQLAALSQPQQNKPKKKEKDKKEKKKEKHKRKEEVEENKKSKAKEPPPKKTKKNNSSNSNVSKKEPAPMKSKPPPTYESEEEDKCKPMSYEEKRQLSLDINKLPGEKLGRVVHIIQSREPSLKNSNPDEIEIDFETLKPSTLRELERYVTSCLRKKRKPQAEKVDVIAGSSKMKGFSSSESESSSESSSSDSEDSETEMAPKSKKKGHPGREQKKHHHHHHQQMQQAPAPVPQQPPPPPQQPPPPPPPQQQQQPPPPPPPPSMPQQAAPAMKSSPPPFIATQVPVLEPQLPGSVFDPIGHFTQPILHLPQPELPPHLPQPPEHSTPPHLNQHAVVSPPALHNALPQQPSRPSNRAAALPPKPARPPAVSPALTQTPLLPQPPMAQPPQVLLEDEEPPAPPLTSMQMQLYLQQLQKVQPPTPLLPSVKVQSQPPPPLPPPPHPSVQQQLQQQPPPPPPPQPQPPPQQQHQPPPRPVHLQPMQFSTHIQQPPPPQGQQPPHPPPGQQPPPPQPAKPQQVIQHHHSPRHHKSDPYSTGHLREAPSPLMIHSPQMSQFQSLTHQSPPQQNVQPKKQELRAASVVQPQPLVVVKEEKIHSPIIRSEPFSPSLRPEPPKHPESIKAPVHLPQRPEMKPVDVGRPVIRPPEQNAPPPGAPDKDKQKQEPKTPVAPKKDLKIKNMGSWASLVQKHPTTPSSTAKSSSDSFEQFRRAAREKEEREKALKAQAEHAEKEKERLRQERMRSREDEDALEQARRAHEEARRRQEQQQQQRQEQQQQQQQQAAAVAAAATPQAQSSQPQSMLDQQRELARKREQERRRREAMAATIDMNFQSDLLSIFEENLF Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Epigenetic regulator > Reader > Bromodomain
Function	Chromatin reader protein that recognizes and binds acetylated histones and plays a key role in transmission of epigenetic memory across cell divisions and transcription regulation. Remains associated with acetylated chromatin throughout the entire cell cycle and provides epigenetic memory for postmitotic G1 gene transcription by preserving acetylated chromatin status and maintaining high-order chromatin structure (PubMed:23589332, PubMed:23317504, PubMed:22334664). During interphase, plays a key role in regulating the transcription of signal-inducible genes by associating with the P-TEFb complex and recruiting it to promoters. Also recruits P-TEFb complex to distal enhancers, so called anti-pause enhancers in collaboration with JMJD6. BRD4 and JMJD6 are required to form the transcriptionally active P-TEFb complex by displacing negative regulators such as HEXIM1 and 7SKsnRNA complex from P-TEFb, thereby transforming it into an active form that can then phosphorylate the C-terminal domain (CTD) of RNA polymerase II (PubMed:23589332, PubMed:19596240, PubMed:16109377, PubMed:16109376, PubMed:24360279). Promotes phosphorylation of 'Ser-2' of the C-terminal domain (CTD) of RNA polymerase II (PubMed:23086925). According to a report, directly acts as an atypical protein kinase and mediates phosphorylation of 'Ser-2' of the C-terminal domain (CTD) of RNA polymerase II; these data however need additional evidences in vivo (PubMed:22509028). In addition to acetylated histones, also recognizes and binds acetylated RELA, leading to further recruitment of the P-TEFb complex and subsequent activation of NF-kappa-B (PubMed:19103749). Also acts as a regulator of p53/TP53-mediated transcription: following phosphorylation by CK2, recruited to p53/TP53 specific target promoters (PubMed:23317504). Show/Hide
Uniprot ID	Primary ID: O60885 Secondarily ID: O60433 Q4G0X8 Q86YS8 Q96PD3 Show/Hide
Ensembl ID	ENSG00000141867
HGNC ID	HGNC:13575
Subcellular Location	Nucleus Chromosome

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

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0500065 Compound Info	US9125915, compound 17 Show/Hide	C20H20ClN5O2S	1
1	IC50 = 12.8 nM Bioactivity Info	TI LI LO TS
CP0461553 Compound Info	US9125915, compound 13 Show/Hide	C20H20ClN5OS	1
1	IC50 = 17.3 nM Bioactivity Info	TI LI LO TS
CP0346525 Compound Info	US9125915, compound 6 Show/Hide	C20H19ClN4O2S	1
1	IC50 = 18.2 nM Bioactivity Info	TI LI LO TS
CP0513413 Compound Info	US9125915, compound 14 Show/Hide	C21H22ClN5O2S	1
1	IC50 = 21 nM Bioactivity Info	TI LI LO TS
CP0545648 Compound Info	US9125915, compound 10 Show/Hide	C29H29N5O3S	1
1	IC50 = 47.1 nM Bioactivity Info	TI LI LO TS
CP0518845 Compound Info	US9125915, compound 5 Show/Hide	C19H16Cl2N4O2S	1
1	IC50 = 54.2 nM Bioactivity Info	TI LI LO TS
CP0461577 Compound Info	US9125915, compound 3 Show/Hide	C26H26N6O2S	1
1	IC50 = 54.9 nM Bioactivity Info	TI LI LO TS
CP0538882 Compound Info	US9125915, compound 9 Show/Hide	C27H27N5O2S	1
1	IC50 = 73.6 nM Bioactivity Info	TI LI LO TS
CP0461578 Compound Info	US9125915, compound 4 Show/Hide	C26H22F3N5O3S	1
1	IC50 = 77.2 nM Bioactivity Info	TI LI LO TS
CP0538883 Compound Info	US9125915, compound 12 Show/Hide	C24H21ClN6OS	1
1	IC50 = 107.8 nM Bioactivity Info	TI LI LO TS
CP0518846 Compound Info	US9125915, compound 7 Show/Hide	C27H26N4O4S	1
1	IC50 = 113 nM Bioactivity Info	TI LI LO TS
CP0545651 Compound Info	US9125915, compound 16 Show/Hide	C25H23ClN6O2S	1
1	IC50 = 116.4 nM Bioactivity Info	TI LI LO TS
CP0518847 Compound Info	US9125915, compound 15 Show/Hide	C25H23ClN6OS	1
1	IC50 = 119.8 nM Bioactivity Info	TI LI LO TS
CP0468377 Compound Info	US9125915, compound 2 Show/Hide	C28H26N6O2S	1
1	IC50 = 121.2 nM Bioactivity Info	TI LI LO TS
CP0500064 Compound Info	US9125915, compound 8 Show/Hide	C26H25N5O2S	1
1	IC50 = 123.5 nM Bioactivity Info	TI LI LO TS
CP0518252 Compound Info	US9125915, compound 18 Show/Hide	C25H23ClN6O2S	1
1	IC50 = 146.8 nM Bioactivity Info	TI LI LO TS
CP0545650 Compound Info	US9125915, compound 11 Show/Hide	C28H28FN5O2S	1
1	IC50 = 225.3 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000067 , HCT 116

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000018 , HL-60

Cell Line Info

Cell Line ID: CL000059 , HuT 78

Cell Line Info

Cell Line ID: CL000141 , LNCaP

Cell Line Info

Cell Line ID: CL000083 , MCF-7

Cell Line Info

Cell Line ID: CL000714 , MM1.S

Cell Line Info

Cell Line ID: CL000095 , NCI-H1299

Cell Line Info

Cell Line ID: CL000174 , Raji

Cell Line Info

Cell Line ID: CL000997 , SAE

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0036210 Compound Info	2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide Show/Hide	C22H22ClN5O2	22
1	EC50 = 440 nM
2	IC50 = 20 nM
3	IC50 = 32.5 nM
4	IC50 = 36 nM
5	IC50 = 36.1 nM
6	IC50 = 40 nM
7	IC50 = 61 nM
8	IC50 = 68 nM
9	IC50 = 120 nM
10	IC50 = 125.89 nM
11	IC50 = 590 nM
12	IC50 = 630 nM
13	IC50 = 630.96 nM
14	IC50 = 631 nM
15	Kd = 55.2 nM
16	Ki = 39.81 nM
17	Ki = 50.12 nM
18	Ki = 65.8 nM
19	Ki = 73.5 nM
20	Ki = 94 nM
21	Ki = 163 nM
22	Ki = 200 nM
CP0137899 Compound Info	US10633379, Example 35 Show/Hide	C28H30FN3O4	9
1	IC50 = 0.65 nM
2	IC50 = 1.78 nM
3	IC50 = 3.3 nM
4	IC50 = 238 nM
5	IC50 = 299.75 nM
6	IC50 = 327.5 nM
7	Kd = 1.6 nM
8	Kd = 520 nM
9	Kd = 3300 nM
CP0202074 Compound Info	12-chloro-4-ethylsulfonyl-23-methyl-8,19-dioxa-23-azatetracyclo[18.4.0.02,7.09,14]tetracosa-1(24),2(7),3,5,9(14),10,12,20-octaen-22-one Show/Hide	C24H24ClNO5S	1
1	IC50 = 0.93 nM
CP0069311 Compound Info	US10633379, Compound X Show/Hide	C22H19F2N3O4S	10
1	IC50 = 1 nM
2	IC50 = 2.5 nM
3	IC50 = 3 nM
4	IC50 = 11 nM
5	IC50 = 39 nM
6	IC50 = 47 nM
7	IC50 = 69 nM
8	IC50 = 74 nM
9	Kd < 10 nM
10	Ki = 1.5 nM
CP0044060 Compound Info	4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide Show/Hide	C28H39N7O3	7
1	IC50 = 1.2 nM
2	IC50 = 25 nM
3	IC50 = 150 nM
4	IC50 = 184 nM
5	IC50 = 205 nM
6	Kd = 37 nM
7	Kd = 87 nM
CP0335216 Compound Info	4-(5-ethylsulfonyl-2-propoxyphenyl)-2-methyl- 6-(1-methylpyrazol-4-yl)isoquinolin-1-one Show/Hide	C25H27N3O4S	1
1	IC50 = 3 nM
CP0004236 Compound Info	(+)-JQ1 Show/Hide	C23H25ClN4O2S	53
1	IC50 = 3.9 nM
2	IC50 = 5.31 nM
3	IC50 = 8 nM
4	IC50 = 12 nM
5	IC50 = 14 nM
6	IC50 = 21 nM
7	IC50 = 22 nM
8	IC50 = 24 nM
9	IC50 = 29 nM
10	IC50 = 32 nM
11	IC50 = 33 nM
12	IC50 = 39.81 nM
13	IC50 = 40 nM
14	IC50 = 42 nM
15	IC50 = 44 nM
16	IC50 = 48.12 nM
17	IC50 = 50 nM
18	IC50 = 50.12 nM
19	IC50 = 51 nM
20	IC50 = 58 nM
21	IC50 = 60 nM
22	IC50 = 62 nM
23	IC50 = 65.7 nM
24	IC50 = 69 nM
25	IC50 = 72 nM
26	IC50 = 77 nM
27	IC50 = 79 nM
28	IC50 = 80 nM
29	IC50 = 83 nM
30	IC50 = 84 nM
31	IC50 = 87 nM
32	IC50 = 88 nM
33	IC50 = 89 nM
34	IC50 = 90 nM
35	IC50 = 91 nM
36	IC50 = 92 nM
37	IC50 < 92 nM
38	IC50 = 94 nM
39	IC50 = 144 nM
40	IC50 = 170 nM
41	IC50 = 81500 nM
42	Kd = 13 nM
43	Kd = 19 nM
44	Kd = 27.2 nM
45	Kd = 49 nM
46	Kd = 50 nM
47	Kd = 60 nM
48	Kd = 62 nM
49	Kd = 90.1 nM
50	Kd = 92 nM
51	Kd = 130 nM
52	Ki = 5.3 nM
53	Ki = 77 nM
CP0103451 Compound Info	2-methyl-6-(1-methylpyrazol-4-yl)-4-(5- methylsulfonyl-2- propoxyphenyl)isoquinolin-1-one Show/Hide	C24H25N3O4S	1
1	IC50 = 5 nM
CP0335218 Compound Info	4-(2-ethoxy-5-ethylsulfonylphenyl)-2-methyl-6-(1-methylpyrazol-4-yl)isoquinolin-1-one Show/Hide	C24H25N3O4S	2
1	IC50 = 5 nM
2	IC50 < 100 nM
CP0368318 Compound Info	4-(2-ethoxy-5-methylsulfonylphenyl)-2- methyl-6-(1-methylpyrazol-4- yl)isoquinolin-1-one Show/Hide	C23H23N3O4S	1
1	IC50 = 9 nM
CP0003832 Compound Info	N'-hydroxy-N-phenyloctanediamide Show/Hide	C14H20N2O3	4
1	IC50 = 10 nM
2	IC50 = 43.13 nM
3	IC50 > 10000 nM
4	IC50 > 50000 nM
CP0096261 Compound Info	US10017501, Compound 1020-18 Show/Hide	C25H22N4O	8
1	IC50 = 14.4 nM
2	IC50 = 78 nM
3	IC50 = 83 nM
4	Kd = 1.3 nM
5	Kd = 2.8 nM
6	Ki = 3.8 nM
7	Ki = 7.5 nM
8	Ki = 16 nM
CP0335215 Compound Info	4-(5-ethylsulfonyl-2-methoxyphenyl)-2- methyl-6-(1-methylpyrazol-4-yl)isoquinolin- 1-one Show/Hide	C23H23N3O4S	1
1	IC50 = 15 nM
CP0042119 Compound Info	benzyl N-(1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl)carbamate Show/Hide	C25H21N5O2	3
1	IC50 = 15.5 nM
2	IC50 = 501 nM
3	IC50 = 501.19 nM
CP0057034 Compound Info	7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-pyridin-2-ylethyl]-3H-imidazo[4,5-c]quinolin-2-one Show/Hide	C23H21N5O3	9
1	IC50 = 18 nM
2	IC50 = 36 nM
3	IC50 = 100 nM
4	IC50 = 107 nM
5	IC50 = 274 nM
6	IC50 = 790 nM
7	IC50 = 794.33 nM
8	Ki = 61 nM
9	Ki = 385 nM
CP0575021 Compound Info	4-[5-ethylsulfonyl-2-(2- hydroxyethoxy)phenyl]-2-methyl-6-(1- methylpyrazol-4-yl)isoquinolin-1-one Show/Hide	C24H25N3O5S	1
1	IC50 = 18 nM
CP0109050 Compound Info	2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]acetamide Show/Hide	C20H18ClN3O2S	1
1	IC50 = 26 nM
CP0202113 Compound Info	6-[(2-amino-4-hydroxy-5-methylphenyl)diazenyl]-3,4-dihydro-1H-quinolin-2-one Show/Hide	C16H16N4O2	2
1	IC50 = 27 nM
2	IC50 = 32 nM
CP0248859 Compound Info	2-[(9S)-4,5,13-trimethyl-7-phenyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]acetamide Show/Hide	C20H19N3O2S	1
1	IC50 = 29 nM
CP0033805 Compound Info	4-[(2-amino-4-hydroxy-5-methylphenyl)diazenyl]-N-cyclopentylbenzenesulfonamide Show/Hide	C18H22N4O3S	2
1	IC50 = 32 nM
2	IC50 = 49 nM
CP0071180 Compound Info	2-[(9S)-7-(4-cyanophenyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]acetamide Show/Hide	C21H18N4O2S	1
1	IC50 = 33 nM
CP0102231 Compound Info	1-[2-(2,4-difluorophenoxy)-5-methylsulfonylphenyl]-3-methyl-2,5,6,7-tetrahydropyrrolo[3,4-c]pyridin-4-one Show/Hide	C21H18F2N2O4S	3
1	IC50 = 35 nM
2	Ki = 34 nM
3	Ki = 300 nM
CP0210886 Compound Info	2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]-N-ethylacetamide Show/Hide	C22H22ClN3O2S	1
1	IC50 = 36 nM
CP0058410 Compound Info	2-[4-(2-hydroxyethoxy)-3,5-dimethylphenyl]-5,7-dimethoxy-3H-quinazolin-4-one Show/Hide	C20H22N2O5	26
1	IC50 = 40 nM
2	IC50 = 43.8 nM
3	IC50 = 67 nM
4	IC50 = 100 nM
5	IC50 = 132 nM
6	IC50 = 135 nM
7	IC50 = 510 nM
8	IC50 = 610 nM
9	IC50 = 645 nM
10	IC50 = 1142 nM
11	IC50 = 1584.89 nM
12	IC50 = 1800 nM
13	IC50 = 1985 nM
14	IC50 = 2450 nM
15	IC50 = 3100 nM
16	IC50 = 6309.57 nM
17	IC50 = 12700 nM
18	IC50 > 10000 nM
19	Kd = 135 nM
20	Kd = 140 nM
21	Kd = 200 nM
22	Kd = 303 nM
23	Kd = 1100 nM
24	Kd = 1142 nM
25	Kd = 4100 nM
26	Kd = 8930 nM
CP0133576 Compound Info	GSK778 Show/Hide	C30H33N5O3	15
1	IC50 = 41 nM
2	IC50 = 5843 nM
3	IC50 ~ 39.81 nM
4	IC50 ~ 41 nM
5	IC50 ~ 50.12 nM
6	IC50 ~ 5843 nM
7	IC50 ~ 6309.57 nM
8	Kd = 6.3 nM
9	Kd = 1258.93 nM
10	Kd ~ 5.9 nM
11	Kd ~ 10 nM
12	Kd ~ 11 nM
13	Kd ~ 100 nM
14	Kd ~ 670 nM
15	Kd ~ 1258.93 nM
CP0153327 Compound Info	2-[(9S)-7-(4-chloro-2-methylphenyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]acetamide Show/Hide	C21H20ClN3O2S	1
1	IC50 = 42 nM
CP0340722 Compound Info	4-[2-(2-aminoethoxy)-5-ethylsulfonylphenyl]- 2-methyl-6-(1-methylpyrazol-4-yl) isoquinolin-1-one Show/Hide	C24H26N4O4S	1
1	IC50 = 49 nM
CP0410254 Compound Info	N-[3-[2-methyl-6-(1-methylpyrazol-4-yl)-1- oxoisoquinolin-4-yl] phenyl]methanesulfonamide Show/Hide	C21H20N4O3S	1
1	IC50 = 50 nM
CP0462117 Compound Info	2-[(9S)-7-(5-chloropyridin-2-yl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]acetamide Show/Hide	C19H17ClN4O2S	1
1	IC50 = 72 nM
CP0084888 Compound Info	2-[(9S)-7-(6-aminopyridin-3-yl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]acetamide Show/Hide	C19H19N5O2S	1
1	IC50 = 73 nM
CP0574202 Compound Info	2-[(9S)-7-(3-chlorophenyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]acetamide Show/Hide	C20H18ClN3O2S	1
1	IC50 = 74 nM
CP0414322 Compound Info	methyl N-[[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]methyl]carbamate Show/Hide	C21H20ClN3O3S	1
1	IC50 = 86 nM
CP0048535 Compound Info	2-methoxy-N-(3-methyl-2-oxo-1,4-dihydroquinazolin-6-yl)benzenesulfonamide Show/Hide	C16H17N3O4S	5
1	IC50 = 88 nM
2	IC50 = 220 nM
3	IC50 = 980 nM
4	IC50 = 3540 nM
5	Kd = 136 nM
CP0407958 Compound Info	1-[(2S)-4-(cyclopropanecarbonyl)-6-[4-(1,1-dioxo-1,4-thiazinan-4-yl)phenyl]-2-methyl-2,3-dihydroquinoxalin-1-yl]ethanone Show/Hide	C25H29N3O4S	1
1	IC50 = 100 nM
CP0240428 Compound Info	4-(3-ethylsulfonylphenyl)-2-methyl-6-(1- methylpyrazol-4-yl)isoquinolin-1-one Show/Hide	C22H21N3O3S	1
1	IC50 = 130 nM
CP0087167 Compound Info	(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-9-(1,3-thiazol-2-ylmethyl)-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaene Show/Hide	C22H18ClN3OS2	1
1	IC50 = 190 nM
CP0248951 Compound Info	N-[[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]methyl]acetamide Show/Hide	C21H20ClN3O2S	1
1	IC50 = 190 nM
CP0121406 Compound Info	(9S)-7-(4-chlorophenyl)-9-(1H-imidazol-2-ylmethyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaene Show/Hide	C22H19ClN4OS	1
1	IC50 = 200 nM
CP0073926 Compound Info	2-[(9S)-7-(2-chlorophenyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]acetamide Show/Hide	C20H18ClN3O2S	1
1	IC50 = 250 nM
CP0073928 Compound Info	(2R)-2-[(9S)-7-(4-cyanophenyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]propanamide Show/Hide	C22H20N4O2S	1
1	IC50 = 250 nM
CP0210887 Compound Info	tert-butyl 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]acetate Show/Hide	C24H25ClN2O3S	1
1	IC50 = 290 nM
CP0336245 Compound Info	2-[(9S)-4,5,13-trimethyl-7-propyl-11-oxa-3-thia-8,12-diazatricyclo[8.3.0.02,6]trideca-1(10),2(6),4,7,12-pentaen-9-yl]acetamide Show/Hide	C17H21N3O2S	1
1	IC50 = 300 nM
CP0750822 Compound Info	Tert-butyl (S)-(2-(2-(2-(2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)ethoxy)ethoxy)ethyl)carbamate Show/Hide	C30H39ClN6O5S	1
1	IC50 = 526 nM
CP0058397 Compound Info	5-nitro-8-quinolinol Show/Hide	C9H6N2O3	1
1	IC50 = 980 nM
CP0199056 Compound Info	8-[[(3R,4R)-3-(cyclohexylmethoxy)piperidin-4-yl]amino]-3-methyl-5-(5-methylpyridin-3-yl)-1H-1,7-naphthyridin-2-one Show/Hide	C27H35N5O2	1
1	IC50 = 1584.89 nM
CP0700230 Compound Info	(S)-N-(2-(2-(2-aminoethoxy)ethoxy)ethyl)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide Show/Hide	C25H31ClN6O3S	1
1	IC50 = 2480 nM
CP0136306 Compound Info	2-[7-(hydroxyamino)-7-oxoheptoxy]-N-(7H-purin-6-yl)benzamide Show/Hide	C19H22N6O4	1
1	IC50 = 2700 nM
CP0717935 Compound Info	rac-8-(((3R,4R)-3-((1,1-Dioxidotetrahydro-2H-thiopyran-4-yl)-methoxy)piperidin-4-yl)amino)-3-methyl-5-(5-methylpyridin-3-yl)quinolin-2(1H)-one Show/Hide	C27H34N4O4S	1
1	IC50 = 3981.07 nM
CP0771696 Compound Info	3-(3-(1-((S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-2,13-dioxo-6,9-dioxa-3,12-diazaoctadecan-18-yl)-2-((1E,3E)-5-((E)-3,3-dimethyl-5-sulfo-1-(3-sulfopropyl)indolin-2-ylidene)penta-1,3-dien-1-yl)-3-methyl-5-sulfo-3H-indol-1-ium-1-yl)propane-1-sulfonate Show/Hide	C61H75ClN8O16S5	1
1	IC50 = 9110 nM
CP0071989 Compound Info	1-[7-(3,4-dimethoxyphenyl)-9-[[(3S)-1-methylpiperidin-3-yl]methoxy]-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]propan-1-one Show/Hide	C27H36N2O5	3
1	IC50 = 15000 nM
2	Kd = 5590 nM
3	Kd = 5600 nM
CP0261967 Compound Info	(1R,9S,12R)-13-[8-[[1-(2-fluoro-2-methylpropyl)piperidin-4-yl]amino]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-12-propan-2-yl-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one Show/Hide	C30H39FN8O2	1
1	IC50 = 19952.62 nM
CP0571907 Compound Info	(1R,9S,12R)-13-[3-methyl-8-(3-pyrrolidin-1-ylpropylamino)-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-12-propan-2-yl-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one Show/Hide	C28H36N8O2	1
1	IC50 = 25118.86 nM
CP0651910 Compound Info	8-(((3R,4R)-3-((1,1-Dioxidotetrahydro-2H-thiopyran-4-yl)-methoxy)-1-methylpiperidin-4-yl)amino)-3-methyl-5-(5-methylpyridin-3-yl)-1,7-naphthyridin-2(1H)-one Show/Hide	C27H35N5O4S	2
1	IC50 = 79432.82 nM
2	Ki = 7943.28 nM
CP0707841 Compound Info	(S)-14-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-2,13-dioxo-6,9-dioxa-3,12-diazatetradecane-1-sulfonic acid Show/Hide	C27H33ClN6O7S2	1
1	IC50 > 10000 nM
CP0742521 Compound Info	4-((2-(2-(2-(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)ethoxy)ethoxy)ethyl)carbamoyl)cyclobutane-1,2,3-tricarboxylic acid Show/Hide	C33H37ClN6O10S	1
1	IC50 > 10000 nM
CP0086064 Compound Info	6-(3-hydroxypropyl)-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione Show/Hide	C25H23N3O4	1
1	IC50 > 15650 nM
CP0127907 Compound Info	6-(3-hydroxypropyl)-2-(1-methyl-2-oxo-3H-benzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione Show/Hide	C23H19N3O4	1
1	IC50 > 20000 nM
CP0489411 Compound Info	(1R,9S)-13-[3-methyl-8-[(1-methylpiperidin-4-yl)amino]-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one Show/Hide	C24H28N8O2	1
1	IC50 > 31622.78 nM
CP0537714 Compound Info	(1R,9S,12R)-13-[8-[[1-(2,2-difluoropropyl)piperidin-4-yl]amino]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-12-propan-2-yl-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one Show/Hide	C29H36F2N8O2	1
1	IC50 > 31622.78 nM
CP0575351 Compound Info	(1R,9S,12R)-13-[8-[3-(4,4-difluoropiperidin-1-yl)propylamino]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-12-propan-2-yl-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one Show/Hide	C29H36F2N8O2	1
1	IC50 > 31622.78 nM
CP0941506 Compound Info	2-Methyl-4((1R,2R,5S)-2-methyl-4-oxo-1,2,3,4,5,6-hexahydro-1,5-epiminobenzo[d]azocine-11-carbonyl)-6-(trifluoromethoxy)-2,9-dihydro-1H-pyrido[3,4-b]indol-1-one Show/Hide	C26H21F3N4O4	1
1	IC50 > 31622.78 nM
CP0134636 Compound Info	(7R)-2-[2-ethoxy-4-(1-methylpiperidin-4-yl)anilino]-7-ethyl-5-methyl-8-[(4-methylthiophen-2-yl)methyl]-7H-pteridin-6-one Show/Hide	C29H38N6O2S	1
1	Kd = 44 nM
CP0350379 Compound Info	(7R)-8-benzyl-2-[2-ethoxy-4-(1-methylpiperidin-4-yl)anilino]-7-ethyl-5-methyl-7H-pteridin-6-one Show/Hide	C30H38N6O2	1
1	Kd = 54 nM
CP0142866 Compound Info	(7R)-2-[2-ethoxy-4-(1-methylpiperidin-4-yl)anilino]-7-ethyl-5-methyl-8-[(3-methylthiophen-2-yl)methyl]-7H-pteridin-6-one Show/Hide	C29H38N6O2S	1
1	Kd = 63 nM
CP0356954 Compound Info	2-[4-[6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-(3-phenylmorpholin-4-yl)quinazolin-2-yl]pyrazol-1-yl]ethanol Show/Hide	C28H28N6O3	1
1	Kd = 66 nM
CP0069317 Compound Info	15-methyl-4-(methylsulfonylmethyl)-8-pyridin-2-yl-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C22H20N4O3S	3
1	Ki = 0.62 nM
2	Ki = 1.2 nM
3	Ki = 1.5 nM
CP0069312 Compound Info	8-(2,4-difluorophenyl)-15-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C23H19F2N3O3S	3
1	Ki = 0.73 nM
2	Ki = 0.87 nM
3	Ki = 2.6 nM
CP0387151 Compound Info	8-(4-fluorophenyl)-15-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C23H20FN3O3S	1
1	Ki = 0.87 nM
CP0069319 Compound Info	8-(4-fluorophenyl)-12-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C23H20FN3O3S	3
1	Ki = 1.2 nM
2	Ki = 2.5 nM
3	Ki = 3.3 nM
CP0106552 Compound Info	US9296741, 21 Show/Hide	C22H21N3O4S	1
1	Ki = 1.5 nM
CP0362338 Compound Info	1-[(3S,5R)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]-3,5-dimethylpiperazin-1-yl]ethanone Show/Hide	C27H37N7O3	3
1	Ki = 1.585 nM
2	Ki = 15.85 nM
3	Ki = 50.12 nM
CP0120224 Compound Info	US9296741, 4 Show/Hide	C21H19N3O4S	1
1	Ki = 2.4 nM
CP0148525 Compound Info	8-(2,4-difluorophenyl)-12-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C23H19F2N3O3S	1
1	Ki = 2.7 nM
CP0514936 Compound Info	N-(12-methyl-14-oxo-8-pyridin-2-yl-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-4-yl)ethanesulfonamide Show/Hide	C22H21N5O3S	1
1	Ki = 2.7 nM
CP0131103 Compound Info	US9296741, 22 Show/Hide	C22H22N4O4S	1
1	Ki = 2.9 nM
CP0219122 Compound Info	12-methyl-4-(methylsulfonylmethyl)-8-pyridin-2-yl-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C22H20N4O3S	1
1	Ki = 2.9 nM
CP0347240 Compound Info	US9296741, 34 Show/Hide	C21H17ClFN3O4S	1
1	Ki = 3.1 nM
CP0249898 Compound Info	(3R)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenyl]ethyl]-1,3-dimethylpiperazin-2-one Show/Hide	C25H33N7O2	3
1	Ki = 3.162 nM
2	Ki = 100 nM
3	Ki = 125.89 nM
CP0369516 Compound Info	N-[4-(4-chlorophenoxy)-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide Show/Hide	C22H20ClN3O4S	1
1	Ki = 3.4 nM
CP0198214 Compound Info	US9296741, 95 Show/Hide	C20H17N3O4S	1
1	Ki = 3.6 nM
CP0227160 Compound Info	US9296741, 57 Show/Hide	C21H25N3O4S	1
1	Ki = 3.7 nM
CP0368533 Compound Info	(3R)-4-[3-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]propyl]-1,3-dimethylpiperazin-2-one Show/Hide	C26H35N7O3	3
1	Ki = 3.981 nM
2	Ki = 63.1 nM
3	Ki = 79.43 nM
CP0131105 Compound Info	US9296741, 23 Show/Hide	C20H18N4O4S	1
1	Ki = 4.1 nM
CP0429554 Compound Info	N-[8-(2,4-difluorophenyl)-15-methyl-14-oxo-6,8,12,15-tetrazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-4-yl]ethanesulfonamide Show/Hide	C22H19F2N5O3S	1
1	Ki = 4.1 nM
CP0326185 Compound Info	US9296741, 5 Show/Hide	C22H18F3N3O4S	1
1	Ki = 4.4 nM
CP0317868 Compound Info	N-[8-(2,4-difluorophenyl)-12-methyl-14-oxo-6,8,12,15-tetrazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-4-yl]ethanesulfonamide Show/Hide	C22H19F2N5O3S	1
1	Ki = 4.4 nM
CP0217104 Compound Info	US9296741, 27 Show/Hide	C21H17F2N3O4S	1
1	Ki = 4.5 nM
CP0542881 Compound Info	8-(4,4-difluorocyclohexyl)-15-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C23H25F2N3O3S	1
1	Ki = 4.7 nM
CP0542880 Compound Info	N-[8-(4-fluorophenyl)-12-methyl-14-oxo-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-4-yl]ethanesulfonamide Show/Hide	C23H21FN4O3S	1
1	Ki = 4.8 nM
CP0143638 Compound Info	(3R)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]-1,3-dimethylpiperazin-2-one Show/Hide	C25H33N7O3	4
1	Ki = 5 nM
2	Ki = 5.012 nM
3	Ki = 125.89 nM
4	Ki = 158.49 nM
CP0362339 Compound Info	1-[(2S,6R)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]-2,6-dimethylpiperazin-1-yl]ethanone Show/Hide	C27H37N7O3	3
1	Ki = 5.012 nM
2	Ki = 50.12 nM
3	Ki = 158.49 nM
CP0311314 Compound Info	N-[4-(4-fluorophenoxy)-3-(1-methyl-7-oxo-6H-pyrrolo[2,3-c]pyridin-3-yl)phenyl]ethanesulfonamide Show/Hide	C22H20FN3O4S	1
1	Ki = 5.5 nM
CP0355322 Compound Info	US9296741, 85 Show/Hide	C21H18N2O4S	1
1	Ki = 5.8 nM
CP0263573 Compound Info	US9296741, 11 Show/Hide	C20H18N4O4S	1
1	Ki = 6.3 nM
CP0213780 Compound Info	(3R)-4-[4-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]butyl]-1,3-dimethylpiperazin-2-one Show/Hide	C27H37N7O3	3
1	Ki = 6.31 nM
2	Ki = 63.1 nM
3	Ki = 100 nM
CP0566085 Compound Info	N-[3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-[2-(trifluoromethyl)phenoxy]phenyl]methanesulfonamide Show/Hide	C22H18F3N3O4S	1
1	Ki = 6.4 nM
CP0320209 Compound Info	8-(cyclopropanecarbonyl)-15-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C21H21N3O4S	1
1	Ki = 7.1 nM
CP0320208 Compound Info	15-methyl-4-(methylsulfonylmethyl)-8-propanoyl-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C20H21N3O4S	1
1	Ki = 7.3 nM
CP0578000 Compound Info	8-(cyclopropanecarbonyl)-12-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C21H21N3O4S	1
1	Ki = 7.7 nM
CP0362373 Compound Info	(3R,5R)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]-1,3,5-trimethylpiperazin-2-one Show/Hide	C26H35N7O3	3
1	Ki = 7.943 nM
2	Ki = 125.89 nM
3	Ki = 251.19 nM
CP0480263 Compound Info	(3R)-1,3-dimethyl-4-[2-[4-[1-[3-(trifluoromethyl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazin-2-one Show/Hide	C25H30F3N7O2	3
1	Ki = 7.943 nM
2	Ki = 63.1 nM
3	Ki = 398.11 nM
CP0368355 Compound Info	8-(cyclopropylmethyl)-15-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C21H23N3O3S	1
1	Ki = 8.4 nM
CP0199478 Compound Info	N-[3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-[4-(trifluoromethyl)phenoxy]phenyl]ethanesulfonamide Show/Hide	C23H20F3N3O4S	1
1	Ki = 9 nM
CP0199479 Compound Info	US9296741, 90 Show/Hide	C23H20N4O4S	1
1	Ki = 9.4 nM
CP0244064 Compound Info	US9296741, 6 Show/Hide	C22H19N3O3	1
1	Ki = 9.8 nM
CP0326283 Compound Info	N-[3-(7-methyl-1-oxo-2,6-dihydropyrrolo[3,4-d]pyridazin-5-yl)-4-phenoxyphenyl]ethanesulfonamide Show/Hide	C21H20N4O4S	1
1	Ki = 10 nM
CP0213781 Compound Info	(3R)-4-[[1-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenyl]azetidin-3-yl]methyl]-1,3-dimethylpiperazin-2-one Show/Hide	C27H36N8O2	3
1	Ki = 10 nM
2	Ki = 100 nM
3	Ki = 158.49 nM
CP0236547 Compound Info	3-[2-(2,4-difluorophenoxy)-5-(methylsulfonylmethyl)phenyl]-1-methyl-6H-pyrrolo[2,3-c]pyridin-7-one Show/Hide	C22H18F2N2O4S	1
1	Ki = 11 nM
CP0326282 Compound Info	N-[4-(2,4-difluorophenoxy)-3-(1-methyl-7-oxo-6H-pyrrolo[2,3-c]pyridin-3-yl)phenyl]ethanesulfonamide Show/Hide	C22H19F2N3O4S	1
1	Ki = 11 nM
CP0153834 Compound Info	US9296741, 62 Show/Hide	C22H18F3N3O4S	1
1	Ki = 12 nM
CP0515982 Compound Info	8-(cyclopropylmethyl)-15-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.014,17]heptadeca-1(16),2(7),3,5,10,14(17)-hexaen-13-one Show/Hide	C21H23N3O3S	1
1	Ki = 12 nM
CP0213782 Compound Info	(3R)-1,3-dimethyl-4-[2-[4-[1-(3-methylsulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]piperazin-2-one Show/Hide	C25H33N7O2S	3
1	Ki = 12.59 nM
2	Ki = 125.89 nM
3	Ki = 158.49 nM
CP0236893 Compound Info	(3R)-4-[2-[4-[1-(3-chloro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]-1,3-dimethylpiperazin-2-one Show/Hide	C24H30ClN7O2	3
1	Ki = 12.59 nM
2	Ki = 199.53 nM
3	Ki = 316.23 nM
CP0236899 Compound Info	(3R)-4-[2-[4-[1-[3-(dimethylamino)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]-1,3-dimethylpiperazin-2-one Show/Hide	C26H36N8O2	2
1	Ki = 12.59 nM
2	Ki = 316.23 nM
CP0219124 Compound Info	US9296741, 329 Show/Hide	C19H21N3O3S	1
1	Ki = 13 nM
CP0265296 Compound Info	US9296741, 19 Show/Hide	C21H17N3O3	1
1	Ki = 14 nM
CP0082466 Compound Info	N-[3-(3-methyl-4-oxo-4,5,6,7-tetrahydro-2H-isoindol-1-yl)-4-phenoxyphenyl]methanesulfonamide Show/Hide	C22H22N2O4S	4
1	Ki = 15 nM
2	Ki = 18 nM
3	Ki = 33 nM
4	Ki = 43 nM
CP0259597 Compound Info	(3R)-1,3-dimethyl-4-[2-[4-[1-(3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]piperazin-2-one Show/Hide	C25H33N7O2	3
1	Ki = 15.85 nM
2	Ki = 199.53 nM
3	Ki = 251.19 nM
CP0078524 Compound Info	N-[4-(2,4-difluorophenoxy)-3-(7-methyl-1-oxo-2,6-dihydropyrrolo[3,4-d]pyridazin-5-yl)phenyl]methanesulfonamide Show/Hide	C20H16F2N4O4S	1
1	Ki = 16 nM
CP0148529 Compound Info	8-(cyclopropylmethyl)-15-methyl-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2,4,6,10,13(17)-hexaen-14-one Show/Hide	C19H19N3O	1
1	Ki = 16 nM
CP0072563 Compound Info	N-[4-(2,4-difluorophenoxy)-3-(1-methyl-7-oxo-6H-pyrrolo[2,3-c]pyridin-3-yl)phenyl]methanesulfonamide Show/Hide	C21H17F2N3O4S	1
1	Ki = 17 nM
CP0346525 Compound Info	US9125915, compound 6 Show/Hide	C20H19ClN4O2S	1
1	Ki = 17 nM
CP0536109 Compound Info	1-methyl-3-(5-methylsulfonyl-2-phenoxyphenyl)-6H-pyrrolo[2,3-c]pyridin-7-one Show/Hide	C21H18N2O4S	1
1	Ki = 17 nM
CP0148526 Compound Info	methyl 12-methyl-4-(methylsulfonylmethyl)-14-oxo-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaene-8-carboxylate Show/Hide	C19H19N3O5S	1
1	Ki = 17 nM
CP0244069 Compound Info	US9296741, 59 Show/Hide	C21H23F2N3O4S	1
1	Ki = 19 nM
CP0237899 Compound Info	N-[4-[4-(dimethylamino)cyclohexyl]oxy-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamide Show/Hide	C24H32N4O4S	1
1	Ki = 26 nM
CP0219123 Compound Info	8-(cyclopropylmethyl)-15-methyl-4-methylsulfonyl-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-one Show/Hide	C20H21N3O3S	1
1	Ki = 26 nM
CP0326285 Compound Info	N-[3-(7-methyl-1-oxo-2,6-dihydropyrrolo[3,4-d]pyridazin-5-yl)-4-phenoxyphenyl]methanesulfonamide Show/Hide	C20H18N4O4S	1
1	Ki = 30 nM
CP0217103 Compound Info	US9296741, 141 Show/Hide	C20H19N5O4S	1
1	Ki = 32 nM
CP0286070 Compound Info	US9296741, 13 Show/Hide	C23H21N3O3	1
1	Ki = 32 nM
CP0078526 Compound Info	7-methyl-5-(2-phenoxyphenyl)-2,6-dihydropyrrolo[3,4-d]pyridazin-1-one Show/Hide	C19H15N3O2	1
1	Ki = 37 nM
CP0325482 Compound Info	US9296741, 144 Show/Hide	C21H27N3O4S	1
1	Ki = 38 nM
CP0078527 Compound Info	N-[3-(3-methyl-4-oxo-2,5,6,7-tetrahydropyrrolo[3,4-c]pyridin-1-yl)-4-phenoxyphenyl]methanesulfonamide Show/Hide	C21H21N3O4S	1
1	Ki = 41 nM
CP0148528 Compound Info	8-(cyclopropylmethyl)-15-methyl-8,12,15-triazatetracyclo[8.6.1.02,7.014,17]heptadeca-1(16),2,4,6,10,14(17)-hexaen-13-one Show/Hide	C19H19N3O	1
1	Ki = 43 nM
CP0093431 Compound Info	US9296741, 1 Show/Hide	C20H16N2O2	1
1	Ki = 48 nM
CP0245134 Compound Info	(3R)-4-[1-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenyl]piperidin-4-yl]-1,3-dimethylpiperazin-2-one Show/Hide	C28H38N8O2	3
1	Ki = 50.12 nM
2	Ki = 158.49 nM
3	Ki = 316.23 nM
CP0480262 Compound Info	(3R)-4-[1-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenyl]azetidin-3-yl]-1,3-dimethylpiperazin-2-one Show/Hide	C26H34N8O2	3
1	Ki = 63.1 nM
2	Ki = 199.53 nM
3	Ki = 398.11 nM
CP0198210 Compound Info	US9296741, 29 Show/Hide	C20H23N3O5S	1
1	Ki = 68 nM
CP0244071 Compound Info	US9296741, 63 Show/Hide	C22H21N3O4S	1
1	Ki = 68 nM
CP0069313 Compound Info	US9296741, 328 Show/Hide	C20H23N3O3S	1
1	Ki = 69 nM
CP0227914 Compound Info	3-[2-(2,4-difluorophenoxy)-5-methylsulfonylphenyl]-1-methyl-6H-pyrrolo[2,3-c]pyridin-7-one Show/Hide	C21H16F2N2O4S	2
1	Ki = 77 nM
2	Ki = 98 nM
CP0308316 Compound Info	5-[2-(2,4-difluorophenoxy)-5-methylsulfonylphenyl]-7-methyl-2,6-dihydropyrrolo[3,4-d]pyridazin-1-one Show/Hide	C20H15F2N3O4S	1
1	Ki = 77 nM
CP0515981 Compound Info	3-[2-(cyclopropylmethylamino)-5-methylsulfonylphenyl]-1-methyl-6H-pyrrolo[2,3-c]pyridin-7-one Show/Hide	C19H21N3O3S	1
1	Ki = 80 nM
CP0468714 Compound Info	N-[4-(2,4-difluorophenoxy)-3-(3-methyl-4-oxo-2,5,6,7-tetrahydropyrrolo[3,4-c]pyridin-1-yl)phenyl]methanesulfonamide Show/Hide	C21H19F2N3O4S	1
1	Ki = 84 nM
CP0536107 Compound Info	US9776990, Example 53 Show/Hide	C23H21NO4	1
1	Ki = 91 nM
CP0102233 Compound Info	N-[4-(2,4-difluorophenoxy)-3-(3-methyl-4-oxo-4,5,6,7-tetrahydro-2H-isoindol-1-yl)phenyl]methanesulfonamide Show/Hide	C22H20F2N2O4S	1
1	Ki = 97 nM
CP0308310 Compound Info	1-methyl-3-(2-phenoxyphenyl)-6H-pyrrolo[2,3-c]pyridin-7-one Show/Hide	C20H16N2O2	1
1	Ki = 120 nM
CP0191020 Compound Info	(3S)-4-[2-[4-[1-(3-methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]-1,3-dimethylpiperazin-2-one Show/Hide	C25H33N7O3	3
1	Ki = 125.89 nM
2	Ki = 251.19 nM
3	Ki = 1000 nM
CP0571581 Compound Info	N-[3-(5-methyl-4-oxo-3,6-dihydropyrrolo[3,4-d]pyrimidin-7-yl)-4-phenoxyphenyl]methanesulfonamide Show/Hide	C20H18N4O4S	1
1	Ki = 150 nM
CP0148527 Compound Info	8-(cyclopropylmethyl)-15-methyl-4-methylsulfonyl-8,12,15-triazatetracyclo[8.6.1.02,7.014,17]heptadeca-1(16),2(7),3,5,10,14(17)-hexaen-13-one Show/Hide	C20H21N3O3S	1
1	Ki = 180 nM
CP0213778 Compound Info	1-methyl-4-[2-[4-[1-[3-(trifluoromethyl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazin-2-one Show/Hide	C24H28F3N7O2	3
1	Ki = 199.53 nM
2	Ki = 316.23 nM
3	Ki = 1000 nM
CP0102234 Compound Info	1-(5-amino-2-phenoxyphenyl)-3-methyl-2,5,6,7-tetrahydro-4H-isoindol-4-one Show/Hide	C21H20N2O2	1
1	Ki = 210 nM
CP0368354 Compound Info	3-[2-(cyclopropylmethylamino)-5-(methylsulfonylmethyl)phenyl]-1-methyl-6H-pyrrolo[2,3-c]pyridin-7-one Show/Hide	C20H23N3O3S	1
1	Ki = 220 nM
CP0536108 Compound Info	N-ethyl-3-(3-methyl-4-oxo-4,5,6,7-tetrahydro-2H-isoindol-1-yl)-4-phenoxybenzamide Show/Hide	C24H24N2O3	1
1	Ki = 250 nM
CP0249897 Compound Info	1-[4-[2-[4-[1-[3-(trifluoromethyl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazin-1-yl]ethanone Show/Hide	C25H30F3N7O2	3
1	Ki = 251.19 nM
2	Ki = 630.96 nM
3	Ki = 3162.28 nM
CP0359971 Compound Info	2-methyl-5-(2-phenoxyphenyl)-1H-pyrrole-3-carboxamide Show/Hide	C18H16N2O2	1
1	Ki = 270 nM
CP0224571 Compound Info	5-[5-(methanesulfonamido)-2-phenoxyphenyl]-2-methyl-1H-pyrrole-3-carboxamide Show/Hide	C19H19N3O4S	1
1	Ki = 280 nM
CP0356978 Compound Info	3-methyl-1-(2-phenoxyphenyl)-2,5,6,7-tetrahydropyrrolo[3,4-c]pyridin-4-one Show/Hide	C20H18N2O2	1
1	Ki = 340 nM
CP0475376 Compound Info	5-[2-(2,4-difluorophenoxy)-5-(methanesulfonamido)phenyl]-2-methyl-1H-pyrrole-3-carboxamide Show/Hide	C19H17F2N3O4S	1
1	Ki = 370 nM
CP0364436 Compound Info	4-methyl-1-[2-[4-[1-[3-(trifluoromethyl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazin-2-one Show/Hide	C24H28F3N7O2	3
1	Ki = 398.11 nM
2	Ki = 2511.89 nM
3	Ki = 7943.28 nM
CP0558974 Compound Info	5-[2-(4-chlorophenoxy)phenyl]-2-methyl-1H-pyrrole-3-carboxamide Show/Hide	C18H15ClN2O2	1
1	Ki = 410 nM
CP0308318 Compound Info	5-(5-amino-2-phenoxyphenyl)-2-methyl-1H-pyrrole-3-carboxamide Show/Hide	C18H17N3O2	1
1	Ki = 420 nM
CP0548979 Compound Info	N-[3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(1-methylpiperidin-4-yl)oxyphenyl]ethanesulfonamide Show/Hide	C22H28N4O4S	1
1	Ki = 430 nM
CP0072566 Compound Info	3-methyl-1-(2-phenoxyphenyl)-2,5,6,7-tetrahydro-4H-isoindol-4-one Show/Hide	C21H19NO2	1
1	Ki = 440 nM
CP0308317 Compound Info	3-methyl-1-(2-phenoxyphenyl)-2,5-dihydropyrrolo[3,4-c]pyridin-4-one Show/Hide	C20H16N2O2	1
1	Ki = 450 nM
CP0308319 Compound Info	5-(2-anilinophenyl)-2-methyl-1H-pyrrole-3-carboxamide Show/Hide	C18H17N3O	1
1	Ki = 450 nM
CP0566098 Compound Info	1-[2-(2,4-difluorophenoxy)-5-methylsulfonylphenyl]-3-methyl-2,5,6,7-tetrahydroisoindol-4-one Show/Hide	C22H19F2NO4S	1
1	Ki = 460 nM
CP0097771 Compound Info	US9296741, 352 Show/Hide	C18H19N3O	1
1	Ki = 680 nM
CP0198216 Compound Info	1-methyl-5-(2-phenoxyphenyl)pyridin-2-one Show/Hide	C18H15NO2	1
1	Ki = 890 nM
CP0261379 Compound Info	5-methyl-7-(2-phenoxyphenyl)-3,6-dihydropyrrolo[3,4-d]pyrimidin-4-one Show/Hide	C19H15N3O2	1
1	Ki = 1100 nM
CP0219126 Compound Info	3-[2-(cyclopropylmethylamino)phenyl]-1-methyl-6H-pyrrolo[2,3-c]pyridin-7-one Show/Hide	C18H19N3O	1
1	Ki = 1500 nM
CP0536106 Compound Info	5-(2-amino-6-phenoxyphenyl)-2-methyl-1H-pyrrole-3-carboxamide Show/Hide	C18H17N3O2	1
1	Ki = 1600 nM
CP0563514 Compound Info	3-methyl-5-(2-phenoxyphenyl)-1H-pyridin-2-one Show/Hide	C18H15NO2	1
1	Ki = 1700 nM
CP0356979 Compound Info	5-[2-(2,4-difluorophenoxy)-5-methylsulfonylphenyl]-2-methyl-1H-pyrrole-3-carboxamide Show/Hide	C19H16F2N2O4S	1
1	Ki = 2200 nM
CP0180784 Compound Info	(3R)-1,3-dimethyl-4-[2-[4-[1-([1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl]phenoxy]ethyl]piperazin-2-one Show/Hide	C24H31N7O2	3
1	Ki = 2511.89 nM
2	Ki = 6309.57 nM
3	Ki > 1000 nM
CP0244065 Compound Info	3-amino-1-methyl-5-(2-phenoxyphenyl)pyridin-2-one Show/Hide	C18H16N2O2	1
1	Ki = 3000 nM
CP0072567 Compound Info	1-(2-aminophenyl)-3-methyl-2,5,6,7-tetrahydro-4H-isoindol-4-one Show/Hide	C15H16N2O	1
1	Ki = 9500 nM
CP0261380 Compound Info	5-(2-aminophenyl)-2-methyl-1H-pyrrole-3-carboxamide Show/Hide	C12H13N3O	1
1	Ki = 22000 nM

Clinical Information about the Protein

Target 1 ( Bromodomain-containing protein 4 (BRD4) )

Target Type	Clinical trial Target
Disease	5 Target-related Diseases				5
1	Myelofibrosis [ICD-11: 2A20.2]
2	Testicular cancer [ICD-11: 2C80]
3	Prostate cancer [ICD-11: 2C82.0]
4	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
5	Acute myeloid leukaemia [ICD-11: 2A60]
Clinical Trial Drug(s)	6 Clinical Trial Drugs				6
1	CPI-0610	Drug Info	Phase 3	Myelofibrosis
2	(+)-JQ1	Drug Info	Phase 1	Testicular cancer
3	ABBV-744	Drug Info	Phase 1	Prostate cancer
4	AZD5153	Drug Info	Phase 1	Solid tumour/cancer
5	GSK525762	Drug Info	Phase 1	Solid tumour/cancer
6	OTX-015	Drug Info	Phase 1/2	Acute myeloid leukaemia

Target 2 ( HUMAN bromodomain-containing protein 4 (BRD4) )

Target Type	Unknown Type Target

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han