Protein Information

General Information of the Protein

Protein ID	PT01508
Protein Name	C-C chemokine receptor type 4
Secondarily Protein Name	K5-5
Gene Name	CCR4
Secondarily Gene Name	CMKBR4
Sequence	MNPTDIADTTLDESIYSNYYLYESIPKPCTKEGIKAFGELFLPPLYSLVFVFGLLGNSVVVLVLFKYKRLRSMTDVYLLNLAISDLLFVFSLPFWGYYAADQWVFGLGLCKMISWMYLVGFYSGIFFVMLMSIDRYLAIVHAVFSLRARTLTYGVITSLATWSVAVFASLPGFLFSTCYTERNHTYCKTKYSLNSTTWKVLSSLEINILGLVIPLGIMLFCYSMIIRTLQHCKNEKKNKAVKMIFAVVVLFLGFWTPYNIVLFLETLVELEVLQDCTFERYLDYAIQATETLAFVHCCLNPIIYFFLGEKFRKYILQLFKTCRGLFVLCQYCGLLQIYSADTPSSSYTQSTMDHDLHDAL Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Membrane receptor > Family A G protein-coupled receptor > Peptide receptor (family A GPCR) > Chemokine receptor > CC chemokine receptor
Function	High affinity receptor for the C-C type chemokines CCL17/TARC, CCL22/MDC and CKLF isoform 1/CKLF1. The activity of this receptor is mediated by G(i) proteins which activate a phosphatidylinositol-calcium second messenger system. Can function as a chemoattractant homing receptor on circulating memory lymphocytes and as a coreceptor for some primary HIV-2 isolates. In the CNS, could mediate hippocampal-neuron survival. Show/Hide
Uniprot ID	Primary ID: P51679 Secondarily ID: Q9ULY6 Q9ULY7 Show/Hide
Ensembl ID	ENSG00000183813
HGNC ID	HGNC:1605
Subcellular Location	Cell 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: CL000795 , 300-19

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0374519 Compound Info	N-cycloheptyl-7-methoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine Show/Hide	C25H37N5O	1
1	IC50 = 13 nM Bioactivity Info	TI LI LO TS
CP0417402 Compound Info	C-014C Show/Hide	C22H32N4O2	1
1	IC50 = 13 nM Bioactivity Info	TI LI LO TS
CP0399036 Compound Info	2-(1,4'-Bipiperidine-1'-yl)-N-cycloheptyl-6,7-dimethoxyquinazolin-4-amine Show/Hide	C27H41N5O2	3
1	IC50 = 18 nM Bioactivity Info	TI LI LO TS
2	IC50 = 73 nM Bioactivity Info	TI LI LO TS
3	IC50 = 140 nM Bioactivity Info	TI LI LO TS
CP0460669 Compound Info	N-cycloheptyl-2-[4-[cyclopentyl(methyl)amino]piperidin-1-yl]-6,7-dimethoxyquinazolin-4-amine Show/Hide	C28H43N5O2	1
1	IC50 = 18 nM Bioactivity Info	TI LI LO TS
CP0311718 Compound Info	N-cycloheptyl-6,7-dimethoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine Show/Hide	C26H39N5O2	3
1	IC50 = 19 nM Bioactivity Info	TI LI LO TS
2	IC50 = 70 nM Bioactivity Info	TI LI LO TS
3	IC50 = 200 nM Bioactivity Info	TI LI LO TS
CP0399358 Compound Info	(1'-{4-[(4-Chlorophenyl)amino]-6,7-dimethoxyquinazolin-2-yl}-1,4'-bipiperidin-3-yl)methanol Show/Hide	C27H34ClN5O3	2
1	IC50 = 19 nM Bioactivity Info	TI LI LO TS
2	IC50 = 23 nM Bioactivity Info	TI LI LO TS
CP0179371 Compound Info	N-(4-chlorophenyl)-6,7-dimethoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine Show/Hide	C25H30ClN5O2	2
1	IC50 = 24 nM Bioactivity Info	TI LI LO TS
2	IC50 = 110 nM Bioactivity Info	TI LI LO TS
CP0462299 Compound Info	[1-[1-[4-(cycloheptylamino)-6,7-dimethoxyquinazolin-2-yl]piperidin-4-yl]piperidin-3-yl]methanol Show/Hide	C28H43N5O3	2
1	IC50 = 30 nM Bioactivity Info	TI LI LO TS
2	IC50 = 100 nM Bioactivity Info	TI LI LO TS
CP0480246 Compound Info	N-cycloheptyl-6-methoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine Show/Hide	C25H37N5O	1
1	IC50 = 31 nM Bioactivity Info	TI LI LO TS
CP0384581 Compound Info	N-cycloheptyl-2-[4-(4-fluoropiperidin-1-yl)piperidin-1-yl]-6,7-dimethoxyquinazolin-4-amine Show/Hide	C27H40FN5O2	1
1	IC50 = 32 nM Bioactivity Info	TI LI LO TS
CP0490272 Compound Info	1'-{4-[(4-Chlorophenyl)amino]-6,7-dimethoxyquinazolin-2-yl}-1,4'-bipiperidin-3-ol Show/Hide	C26H32ClN5O3	2
1	IC50 = 48 nM Bioactivity Info	TI LI LO TS
2	IC50 = 85 nM Bioactivity Info	TI LI LO TS
CP0467631 Compound Info	N-(4-chlorophenyl)-6,7-dimethoxy-2-[4-[3-(methoxymethyl)piperidin-1-yl]piperidin-1-yl]quinazolin-4-amine Show/Hide	C28H36ClN5O3	2
1	IC50 = 52 nM Bioactivity Info	TI LI LO TS
2	IC50 = 64 nM Bioactivity Info	TI LI LO TS
CP0459609 Compound Info	1'-(4-{[2-(4-Chlorophenyl)ethyl]amino}-6,7-dimethoxyquinazolin-2-yl)-1,40-bipiperidin-3-yl]methanol Show/Hide	C29H38ClN5O3	1
1	IC50 = 61 nM Bioactivity Info	TI LI LO TS
CP0399034 Compound Info	(1'-{4-[(4-Chlorobenzyl)amino]-6,7-dimethoxyquinazolin-2-yl}-1,4'-bipiperidin-3-yl)methanol Show/Hide	C28H36ClN5O3	2
1	IC50 = 87 nM Bioactivity Info	TI LI LO TS
2	IC50 = 450 nM Bioactivity Info	TI LI LO TS
CP0459485 Compound Info	N-(4-chlorophenyl)-6,7-dimethoxy-2-[4-(3-methoxypiperidin-1-yl)piperidin-1-yl]quinazolin-4-amine Show/Hide	C27H34ClN5O3	2
1	IC50 = 100 nM Bioactivity Info	TI LI LO TS
2	IC50 = 510 nM Bioactivity Info	TI LI LO TS
CP0468430 Compound Info	[4-[1-[4-(4-chloroanilino)-6,7-dimethoxyquinazolin-2-yl]piperidin-4-yl]morpholin-2-yl]methanol Show/Hide	C26H32ClN5O4	2
1	IC50 = 100 nM Bioactivity Info	TI LI LO TS
2	IC50 = 620 nM Bioactivity Info	TI LI LO TS
CP0459608 Compound Info	[1-[1-[4-[3-(4-chlorophenyl)propylamino]-6,7-dimethoxyquinazolin-2-yl]piperidin-4-yl]piperidin-3-yl]methanol Show/Hide	C30H40ClN5O3	1
1	IC50 = 180 nM Bioactivity Info	TI LI LO TS
CP0384582 Compound Info	N-cyclooctyl-6,7-dimethoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine Show/Hide	C27H41N5O2	2
1	IC50 = 200 nM Bioactivity Info	TI LI LO TS
2	IC50 = 1200 nM Bioactivity Info	TI LI LO TS
CP0417413 Compound Info	N-cycloheptyl-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine Show/Hide	C24H35N5	1
1	IC50 = 200 nM Bioactivity Info	TI LI LO TS
CP0438817 Compound Info	N-cycloheptyl-6,7-dimethoxy-2-(4-propan-2-ylpiperazin-1-yl)quinazolin-4-amine Show/Hide	C24H37N5O2	2
1	IC50 = 220 nM Bioactivity Info	TI LI LO TS
2	IC50 = 660 nM Bioactivity Info	TI LI LO TS
CP0374428 Compound Info	N-cycloheptyl-2-[4-(dimethylamino)piperidin-1-yl]-6,7-dimethoxyquinazolin-4-amine Show/Hide	C24H37N5O2	2
1	IC50 = 260 nM Bioactivity Info	TI LI LO TS
2	IC50 = 730 nM Bioactivity Info	TI LI LO TS
CP0384584 Compound Info	N-cyclohexyl-6,7-dimethoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine Show/Hide	C25H37N5O2	2
1	IC50 = 480 nM Bioactivity Info	TI LI LO TS
2	IC50 = 1900 nM Bioactivity Info	TI LI LO TS
CP0374427 Compound Info	N-cycloheptyl-2-(1-cyclohexylpiperidin-4-yl)-6,7-dimethoxyquinazolin-4-amine Show/Hide	C28H42N4O2	1
1	IC50 = 510 nM Bioactivity Info	TI LI LO TS
CP0374450 Compound Info	N-cycloheptyl-2-(4-cyclohexylpiperazin-1-yl)-6,7-dimethoxyquinazolin-4-amine Show/Hide	C27H41N5O2	1
1	IC50 = 550 nM Bioactivity Info	TI LI LO TS
CP0399037 Compound Info	[1-[1-[4-(4-chlorophenyl)-6,7-dimethoxyquinazolin-2-yl]piperidin-4-yl]piperidin-3-yl]methanol Show/Hide	C27H33ClN4O3	1
1	IC50 > 1000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000108 , CCRF-CEM

Cell Line Info

Cell Line ID: CL000064 , Chem-1

Cell Line Info

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL000026 , CHO-K1

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000131 , HEK293-F

Cell Line Info

Cell Line ID: CL000059 , HuT 78

Cell Line Info

Cell Line ID: CL000233 , L1.2

Cell Line Info

Cell Line ID: CL000040 , THP-1

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0311718 Compound Info	N-cycloheptyl-6,7-dimethoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine Show/Hide	C26H39N5O2	1
1	IC50 = 70 nM
CP0179371 Compound Info	N-(4-chlorophenyl)-6,7-dimethoxy-2-(4-pyrrolidin-1-ylpiperidin-1-yl)quinazolin-4-amine Show/Hide	C25H30ClN5O2	1
1	IC50 = 150 nM
CP0051868 Compound Info	4-N-[(2,4-dichlorophenyl)methyl]-2-N-[5-(diethylamino)pentan-2-yl]pyrimidine-2,4-diamine Show/Hide	C20H29Cl2N5	1
1	IC50 = 270 nM
CP0300639 Compound Info	[4-[4-[(2,4-dichlorophenyl)methylamino]pyrido[2,3-d]pyrimidin-2-yl]piperazin-1-yl]-[(2R)-piperidin-2-yl]methanone Show/Hide	C24H27Cl2N7O	1
1	Kd = 50.12 nM
CP0156159 Compound Info	(3S)-N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]morpholine-3-carboxamide Show/Hide	C25H26ClN5O5S2	1
1	Kd = 79.43 nM
CP0278336 Compound Info	(2S)-N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]piperidine-2-carboxamide Show/Hide	C26H28ClN5O4S2	1
1	Kd = 125.89 nM
CP0077036 Compound Info	2-amino-N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-2-methylpropanamide Show/Hide	C24H26ClN5O4S2	1
1	Kd = 141.25 nM
CP0234241 Compound Info	(R)-(4-(4-(2,4-dichlorobenzylamino)pyrimidin-2-yl)piperazin-1-yl)(piperidin-2-yl)methanone Show/Hide	C21H26Cl2N6O	1
1	Kd = 173.78 nM
CP0278337 Compound Info	(2R)-N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-2-(methylamino)propanamide Show/Hide	C24H26ClN5O4S2	1
1	Kd = 199.53 nM
CP0279147 Compound Info	N-[(2,4-dichlorophenyl)methyl]-2-[2-(pyrrolidin-2-ylmethyl)-2,8-diazaspiro[4.5]decan-8-yl]pyrimidin-4-amine Show/Hide	C24H32Cl2N6	1
1	Kd = 199.53 nM
CP0130918 Compound Info	N-[5-bromo-3-[[3-[2-(dimethylamino)ethoxy]-4-methoxyphenyl]methoxy]pyrazin-2-yl]-4-methylbenzenesulfonamide Show/Hide	C23H27BrN4O5S	1
1	Kd = 251.19 nM
CP0191660 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-4-methylmorpholine-3-carboxamide Show/Hide	C26H28ClN5O5S2	1
1	Kd = 251.19 nM
CP0077037 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]oxane-4-carboxamide Show/Hide	C26H27ClN4O5S2	1
1	Kd = 501.19 nM
CP0309251 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-(1-hydroxyethyl)indazol-1-yl]methyl]phenyl]methyl]acetamide Show/Hide	C23H23ClN4O4S2	1
1	Kd = 501.19 nM
CP0156161 Compound Info	(3R)-N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]morpholine-3-carboxamide Show/Hide	C25H26ClN5O5S2	1
1	Kd = 562.34 nM
CP0108525 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-2-hydroxy-2-methylpropanamide Show/Hide	C24H25ClN4O5S2	1
1	Kd = 630.96 nM
CP0130854 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-5-fluoro-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-2-hydroxy-2-methylpropanamide Show/Hide	C24H24ClFN4O5S2	1
1	Kd = 630.96 nM
CP0247370 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-6-fluoro-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-2-hydroxy-2-methylpropanamide Show/Hide	C24H24ClFN4O5S2	1
1	Kd = 630.96 nM
CP0191661 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]oxolane-2-carboxamide Show/Hide	C25H25ClN4O5S2	1
1	Kd = 794.33 nM
CP0304249 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-hydroxyindazol-1-yl]methyl]phenyl]methyl]acetamide Show/Hide	C21H19ClN4O4S2	1
1	Kd = 794.33 nM
CP0130917 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]acetamide Show/Hide	C22H21ClN4O4S2	1
1	Kd = 1000 nM
CP0156162 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]oxetane-3-carboxamide Show/Hide	C24H23ClN4O5S2	1
1	Kd = 1000 nM
CP0174383 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-6-fluoro-4-methoxyindazol-1-yl]methyl]phenyl]methyl]acetamide Show/Hide	C22H20ClFN4O4S2	1
1	Kd = 1000 nM
CP0191663 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-(hydroxymethyl)indazol-1-yl]methyl]phenyl]methyl]acetamide Show/Hide	C22H21ClN4O4S2	1
1	Kd = 1000 nM
CP0234242 Compound Info	N-[(2,4-dichlorophenyl)methyl]-N-methyl-2-[2-(pyrrolidin-2-ylmethyl)-2,8-diazaspiro[4.5]decan-8-yl]pyrimidin-4-amine Show/Hide	C25H34Cl2N6	1
1	Kd = 1000 nM
CP0156152 Compound Info	N-[[3-[[3-[(3-fluoro-4-methylphenyl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-2-hydroxy-2-methylpropanamide Show/Hide	C27H29FN4O5S	1
1	Kd = 1258.93 nM
CP0278335 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-5-fluoro-4-methoxyindazol-1-yl]methyl]phenyl]methyl]acetamide Show/Hide	C22H20ClFN4O4S2	1
1	Kd = 3162.28 nM
CP0130855 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-fluoroindazol-1-yl]methyl]phenyl]methyl]acetamide Show/Hide	C21H18ClFN4O3S2	1
1	Kd = 5011.87 nM
CP0077039 Compound Info	N-[[3-[[4-chloro-3-[(5-chlorothiophen-2-yl)sulfonylamino]indazol-1-yl]methyl]phenyl]methyl]acetamide Show/Hide	C21H18Cl2N4O3S2	1
1	Kd = 6309.57 nM
CP0278338 Compound Info	N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-(difluoromethyl)indazol-1-yl]methyl]phenyl]methyl]acetamide Show/Hide	C22H19ClF2N4O3S2	1
1	Kd = 7943.28 nM
CP0197772 Compound Info	2,3-dichloro-N-(3-methoxy-1-methylpyrazolo[3,4-d]pyrimidin-4-yl)benzenesulfonamide Show/Hide	C13H11Cl2N5O3S	1
1	Kd > 6309.57 nM
CP0356743 Compound Info	5-chloro-N-(3-methoxy-1-methylpyrazolo[3,4-d]pyrimidin-4-yl)thiophene-2-sulfonamide Show/Hide	C11H10ClN5O3S2	1
1	Kd > 6309.57 nM
CP0174384 Compound Info	N-[[2-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]pyridin-4-yl]methyl]acetamide Show/Hide	C21H20ClN5O4S2	1
1	Kd > 10000 nM

Clinical Information about the Protein

Target 1 ( C-C chemokine receptor type 4 (CCR4) )

Target Type	Successful Target
Disease	1 Target-related Disease				1
1	Asthma [ICD-11: CA23]
Clinical Trial Drug(s)	1 Clinical Trial Drug				1
1	GSK-2239633	Drug Info	Phase 1	Asthma
Preclinical Drug(s)	1 Preclinical Drug				1
1	AZD-1678	Drug Info	Preclinical	Asthma

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT06393	C-C chemokine receptor type 4	Mus musculus, Mouse	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han