Protein Information

General Information of the Protein

Protein ID	PT04881
Protein Name	Folate receptor alpha
Secondarily Protein Name	Adult folate-binding protein Folate receptor 1 Folate receptor adult KB cells FBP Ovarian tumor-associated antigen MOv18
Gene Name	FOLR1
Secondarily Gene Name	FOLR
Sequence	MAQRMTTQLLLLLVWVAVVGEAQTRIAWARTELLNVCMNAKHHKEKPGPEDKLHEQCRPWRKNACCSTNTSQEAHKDVSYLYRFNWNHCGEMAPACKRHFIQDTCLYECSPNLGPWIQQVDQSWRKERVLNVPLCKEDCEQWWEDCRTSYTCKSNWHKGWNWTSGFNKCAVGAACQPFHFYFPTPTVLCNEIWTHSYKVSNYSRGSGRCIQMWFDPAQGNPNEEVARFYAAAMSGAGPWAAWPFLLSLALMLLWLLS Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Membrane receptor
Function	Binds to folate and reduced folic acid derivatives and mediates delivery of 5-methyltetrahydrofolate and folate analogs into the interior of cells (PubMed:23851396, PubMed:23934049, PubMed:2527252, PubMed:8033114, PubMed:8567728, PubMed:19074442). Has high affinity for folate and folic acid analogs at neutral pH (PubMed:23851396, PubMed:23934049, PubMed:2527252, PubMed:8033114, PubMed:8567728). Exposure to slightly acidic pH after receptor endocytosis triggers a conformation change that strongly reduces its affinity for folates and mediates their release (PubMed:8567728). Required for normal embryonic development and normal cell proliferation (By similarity). Show/Hide
Uniprot ID	Primary ID: P15328 Secondarily ID: Q53EW2 Q6FGT8 Q6LC90 Q9UCT2 Show/Hide
HGNC ID	HGNC:3791
Subcellular Location	Cell membrane Apical cell membrane Basolateral cell membrane Secreted Cytoplasmic vesicle Cytoplasmic vesicle Clathrin-coated vesicle Endosome

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: CL000938 , Chinese hamster RT16

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0055020 Compound Info	AGF94 Show/Hide	C19H21N5O6S	4
1	IC50 = 0.31 nM Bioactivity Info	TI LI LO TS
2	IC50 = 0.38 nM Bioactivity Info	TI LI LO TS
3	IC50 = 173 nM Bioactivity Info	TI LI LO TS
4	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0374708 Compound Info	(2S)-2-[[4-[3-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acid Show/Hide	C19H21N5O6S	2
1	IC50 = 0.33 nM Bioactivity Info	TI LI LO TS
2	IC50 = 494 nM Bioactivity Info	TI LI LO TS
CP0776522 Compound Info	(4-{[2-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)ethyl]thio}benzoyl)-L-glutamic Acid Show/Hide	C20H21N5O6S	1
1	IC50 = 0.51 nM Bioactivity Info	TI LI LO TS
CP0206826 Compound Info	(2S)-2-[[5-[3-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-3-carbonyl]amino]pentanedioic acid Show/Hide	C19H21N5O6S	2
1	IC50 = 0.61 nM Bioactivity Info	TI LI LO TS
2	IC50 = 506 nM Bioactivity Info	TI LI LO TS
CP0705783 Compound Info	(4-{N-[2-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)ethyl]-2,2,2-trifluoroacetamido}benzoyl)-L-glutamic Acid Show/Hide	C22H21F3N6O7	1
1	IC50 = 1.08 nM Bioactivity Info	TI LI LO TS
CP0383884 Compound Info	(2S)-2-[[5-[4-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-2-carbonyl]amino]pentanedioic acid Show/Hide	C21H24N6O6	2
1	IC50 = 1.27 nM Bioactivity Info	TI LI LO TS
2	IC50 = 687 nM Bioactivity Info	TI LI LO TS
CP0946262 Compound Info	(S)-2-(4-{[N-Methyl-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methylamino]-carbonyl}phenylcarbonyl)aminopentanedioic acid Show/Hide	C21H22N6O7	1
1	IC50 = 1.4 nM Bioactivity Info	TI LI LO TS
CP0946260 Compound Info	(S)-2-(3-{[N-methyl-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methylamino]-carbonyl}phenylcarbonyl)aminopentanedioic acid Show/Hide	C21H22N6O7	1
1	IC50 = 1.78 nM Bioactivity Info	TI LI LO TS
CP0330758 Compound Info	(S)-2-({5-[4-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)-butyl]-thiophene-2-carbonyl}-amino)-pentanedioicAcid Show/Hide	C20H23N5O6S	1
1	IC50 = 1.82 nM Bioactivity Info	TI LI LO TS
CP0874529 Compound Info	{4-[2-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)ethoxy]benzoyl}-L-glutamic Acid Show/Hide	C20H21N5O7	1
1	IC50 = 1.89 nM Bioactivity Info	TI LI LO TS
CP0705782 Compound Info	(4-{N-[2-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)ethyl]formamido}benzoyl)-L-L-glutamic Acid Show/Hide	C21H22N6O7	1
1	IC50 = 3.01 nM Bioactivity Info	TI LI LO TS
CP0838078 Compound Info	(4-{[2-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)ethyl]amino}benzoyl)-L-glutamic Acid Show/Hide	C20H22N6O6	1
1	IC50 = 3.04 nM Bioactivity Info	TI LI LO TS
CP0429653 Compound Info	(2S)-2-[[5-[4-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)but-1-ynyl]pyridine-2-carbonyl]amino]pentanedioic acid Show/Hide	C21H20N6O6	2
1	IC50 = 4.43 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0740290 Compound Info	(4-{N-[2-(2-Amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-6-yl)ethyl]acetamido}benzoyl)-L-glutamic Acid Show/Hide	C22H24N6O7	1
1	IC50 = 4.87 nM Bioactivity Info	TI LI LO TS
CP0050307 Compound Info	(S)-2-(4-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl)benzamido)pentanedioic acid Show/Hide	C22H25N5O6	2
1	IC50 = 6.3 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0419800 Compound Info	(2S)-2-[[5-[3-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]butanedioic acid Show/Hide	C18H19N5O6S	2
1	IC50 = 6.6 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0931090 Compound Info	(S)-2-(5-{[N-methyl-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methylamino]carbonyl}thiophene-2-carbonyl)aminopentanedioic acid Show/Hide	C19H20N6O7S	1
1	IC50 = 7.78 nM Bioactivity Info	TI LI LO TS
CP0386884 Compound Info	(2S)-2-[[5-[3-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]hexanedioic acid Show/Hide	C20H23N5O6S	2
1	IC50 = 9.5 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0041026 Compound Info	(2S)-2-[(5-{methyl[(2-methyl-4-oxo-1,4-dihydroquinazolin-6-yl)methyl]amino}thiophen-2-yl)formamido]pentanedioic acid Show/Hide	C21H22N4O6S	2
1	IC50 = 15 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0383883 Compound Info	(2S)-2-[[6-[4-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-3-carbonyl]amino]pentanedioic acid Show/Hide	C21H24N6O6	2
1	IC50 = 15.02 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0386883 Compound Info	4-[[5-[3-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]butanoic acid Show/Hide	C18H21N5O4S	2
1	IC50 = 27.4 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0036368 Compound Info	(2S)-2-{[4-(2-{2-amino-4-oxo-1H,4H,7H-pyrrolo[2,3-d]pyrimidin-5-yl}ethyl)phenyl]formamido}pentanedioic acid Show/Hide	C20H21N5O6	3
1	IC50 = 42 nM Bioactivity Info	TI LI LO TS
2	IC50 = 388 nM Bioactivity Info	TI LI LO TS
3	IC50 = 894 nM Bioactivity Info	TI LI LO TS
CP0399631 Compound Info	(2S)-2-[[5-[5-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)pentyl]thiophene-2-carbonyl]amino]pentanedioic acid Show/Hide	C21H25N5O6S	1
1	IC50 = 45.5 nM Bioactivity Info	TI LI LO TS
CP0381988 Compound Info	(2S)-2-[[5-[4-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)butyl]thiophene-2-carbonyl]amino]pentanedioic acid Show/Hide	C20H23N5O6S	1
1	IC50 = 49.3 nM Bioactivity Info	TI LI LO TS
CP0379858 Compound Info	(2S)-2-[[5-[3-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carbonyl]amino]pentanoic acid Show/Hide	C19H23N5O4S	2
1	IC50 = 55.7 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0461015 Compound Info	(2S)-2-[[5-[3-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acid Show/Hide	C19H21N5O6S	1
1	IC50 = 109 nM Bioactivity Info	TI LI LO TS
CP0036197 Compound Info	2-[(4-{[(2,4-diaminopteridin-6-yl)methyl](methyl)amino}phenyl)formamido]pentanedioic acid Show/Hide	C20H22N8O5	3
1	IC50 = 114 nM Bioactivity Info	TI LI LO TS
2	IC50 = 216 nM Bioactivity Info	TI LI LO TS
3	IC50 = 461 nM Bioactivity Info	TI LI LO TS
CP0374710 Compound Info	(2S)-2-[[5-[3-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl)propyl]thiophene-3-carbonyl]amino]pentanedioic acid Show/Hide	C19H21N5O6S	2
1	IC50 = 148 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0374709 Compound Info	(2S)-2-[[4-[3-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl)propyl]thiophene-2-carbonyl]amino]pentanedioic acid Show/Hide	C19H21N5O6S	2
1	IC50 = 154 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0383886 Compound Info	CHEBI:71223 Show/Hide	C23H23N7O5	2
1	IC50 = 168 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0383887 Compound Info	(2S)-2-[[6-[4-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)butyl]pyridine-2-carbonyl]amino]pentanedioic acid Show/Hide	C21H24N6O6	2
1	IC50 = 186 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0383885 Compound Info	(2S)-2-[[6-[4-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)but-1-ynyl]pyridine-3-carbonyl]amino]pentanedioic acid Show/Hide	C21H20N6O6	2
1	IC50 = 449 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0468983 Compound Info	(2S)-2-[[5-[2-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)ethyl]thiophene-2-carbonyl]amino]pentanedioic acid Show/Hide	C18H19N5O6S	1
1	IC50 = 550 nM Bioactivity Info	TI LI LO TS
CP0411313 Compound Info	5-[3-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophene-2-carboxylic acid Show/Hide	C14H14N4O3S	2
1	IC50 = 661 nM Bioactivity Info	TI LI LO TS
2	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0876574 Compound Info	(S)-2-(5-{[N-methyl-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methylamino]carbonyl}thiophene-3-carbonyl)aminopentanedioic acid Show/Hide	C19H20N6O7S	1
1	IC50 = 867 nM Bioactivity Info	TI LI LO TS
CP0200251 Compound Info	(2S)-2-[[5-[(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)methyl]thiophene-2-carbonyl]amino]pentanedioic acid Show/Hide	C17H17N5O6S	1
1	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0399627 Compound Info	(2S)-2-[[5-[6-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)hexyl]thiophene-2-carbonyl]amino]pentanedioic acid Show/Hide	C22H27N5O6S	1
1	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0416461 Compound Info	(2S)-2-[[6-[4-(2-amino-4-oxo-3,7-dihydropyrrolo[2,3-d]pyrimidin-6-yl)but-1-ynyl]pyridine-2-carbonyl]amino]pentanedioic acid Show/Hide	C21H20N6O6	1
1	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0935714 Compound Info	(S)-2-(4-{[N-methyl-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methylamino]carbonyl}thiophene-2-carbonyl)aminopentanedioic acid Show/Hide	C19H20N6O7S	1
1	IC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0946261 Compound Info	(S)-2-(4-{[N-methyl-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)methylamino]-sulfonyl}phenylcarbonyl)aminopentanedioic acid Show/Hide	C20H22N6O8S	1
1	IC50 > 1000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000330 , CHO Pro-4 MtxRII OuaR-2-4

Cell Line Info

Clinical Information about the Protein

Target 1 ( Folate receptor alpha (FOLR1) )

Target Type	Successful Target
Disease	2 Target-related Diseases				2
1	Malaria [ICD-11: 1F40-1F45]
2	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Approved Drug(s)	1 Approved Drug				1
1	Pyrimethamine	Drug Info	Approved	Malaria
Clinical Trial Drug(s)	1 Clinical Trial Drug				1
1	Talotrexin	Drug Info	Phase 1/2	Solid tumour/cancer

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han