General Information of the Protein
Protein ID
PT01008
Protein Name
Macrophage colony-stimulating factor 1 receptor
Secondarily
Protein Name
CSF-1 receptor
Proto-oncogene c-Fms
Gene Name
CSF1R
Secondarily
Gene Name
FMS
Sequence
MGPGVLLLLLVATAWHGQGIPVIEPSVPELVVKPGATVTLRCVGNGSVEWDGPPSPHWTLYSDGSSSILSTNNATFQNTGTYRCTEPGDPLGGSAAIHLYVKDPARPWNVLAQEVVVFEDQDALLPCLLTDPVLEAGVSLVRVRGRPLMRHTNYSFSPWHGFTIHRAKFIQSQDYQCSALMGGRKVMSISIRLKVQKVIPGPPALTLVPAELVRIRGEAAQIVCSASSVDVNFDVFLQHNNTKLAIPQQSDFHNNRYQKVLTLNLDQVDFQHAGNYSCVASNVQGKHSTSMFFRVVESAYLNLSSEQNLIQEVTVGEGLNLKVMVEAYPGLQGFNWTYLGPFSDHQPEPKLANATTKDTYRHTFTLSLPRLKPSEAGRYSFLARNPGGWRALTFELTLRYPPEVSVIWTFINGSGTLLCAASGYPQPNVTWLQCSGHTDRCDEAQVLQVWDDPYPEVLSQEPFHKVTVQSLLTVETLEHNQTYECRAHNSVGSGSWAFIPISAGAHTHPPDEFLFTPVVVACMSIMALLLLLLLLLLYKYKQKPKYQVRWKIIESYEGNSYTFIDPTQLPYNEKWEFPRNNLQFGKTLGAGAFGKVVEATAFGLGKEDAVLKVAVKMLKSTAHADEKEALMSELKIMSHLGQHENIVNLLGACTHGGPVLVITEYCCYGDLLNFLRRKAEAMLGPSLSPGQDPEGGVDYKNIHLEKKYVRRDSGFSSQGVDTYVEMRPVSTSSNDSFSEQDLDKEDGRPLELRDLLHFSSQVAQGMAFLASKNCIHRDVAARNVLLTNGHVAKIGDFGLARDIMNDSNYIVKGNARLPVKWMAPESIFDCVYTVQSDVWSYGILLWEIFSLGLNPYPGILVNSKFYKLVKDGYQMAQPAFAPKNIYSIMQACWALEPTHRPTFQQICSFLQEQAQEDRRERDYTNLPSSSRSGGSGSSSSELEEESSSEHLTCCEQGDIAQPLLQPNNYQFC
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase PDGFR family
Function
Tyrosine-protein kinase that acts as a cell-surface receptor for CSF1 and IL34 and plays an essential role in the regulation of survival, proliferation and differentiation of hematopoietic precursor cells, especially mononuclear phagocytes, such as macrophages and monocytes. Promotes the release of pro-inflammatory chemokines in response to IL34 and CSF1, and thereby plays an important role in innate immunity and in inflammatory processes. Plays an important role in the regulation of osteoclast proliferation and differentiation, the regulation of bone resorption, and is required for normal bone and tooth development. Required for normal male and female fertility, and for normal development of milk ducts and acinar structures in the mammary gland during pregnancy. Promotes reorganization of the actin cytoskeleton, regulates formation of membrane ruffles, cell adhesion and cell migration, and promotes cancer cell invasion. Activates several signaling pathways in response to ligand binding, including the ERK1/2 and the JNK pathway (PubMed:20504948, PubMed:30982609). Phosphorylates PIK3R1, PLCG2, GRB2, SLA2 and CBL. Activation of PLCG2 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate, that then lead to the activation of protein kinase C family members, especially PRKCD. Phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leads to activation of the AKT1 signaling pathway. Activated CSF1R also mediates activation of the MAP kinases MAPK1/ERK2 and/or MAPK3/ERK1, and of the SRC family kinases SRC, FYN and YES1. Activated CSF1R transmits signals both via proteins that directly interact with phosphorylated tyrosine residues in its intracellular domain, or via adapter proteins, such as GRB2. Promotes activation of STAT family members STAT3, STAT5A and/or STAT5B. Promotes tyrosine phosphorylation of SHC1 and INPP5D/SHIP-1. Receptor signaling is down-regulated by protein phosphatases, such as INPP5D/SHIP-1, that dephosphorylate the receptor and its downstream effectors, and by rapid internalization of the activated receptor. In the central nervous system, may play a role in the development of microglia macrophages (PubMed:30982608).
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Uniprot ID
Primary ID:
P07333

Secondarily ID:
B5A955
D3DQG2
Q6LDW5
Q6LDY4
Q86VW7
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Ensembl ID
ENSG00000182578
HGNC ID
HGNC:2433
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: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0441015
N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]propanamide
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C30H31F3N6OS
 1
1
GI50 < 1 nM
   TI
   LI
   LO
   TS
CP0137907
2-(4-methylpiperazin-1-yl)-N-[4-methyl-5-[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]-1,3-thiazol-2-yl]acetamide
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C25H27N7OS
 1
1
GI50 = 4 nM
   TI
   LI
   LO
   TS
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
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C29H31N7O
 1
1
GI50 = 110 nM
   TI
   LI
   LO
   TS
CP0421231
N-[[1-[4-[[3-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]carbamoylamino]-2-(trifluoromethyl)phenyl]piperidin-4-yl]methyl]propanamide
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C34H36F3N5O5
 1
1
GI50 = 110 nM
   TI
   LI
   LO
   TS
CP0190068
N-[4-methyl-3-[1-(6-methylpyridine-3-carbonyl)piperidin-4-yl]oxyphenyl]-4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)benzamide
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C33H38F3N5O3
 1
1
GI50 = 162 nM
   TI
   LI
   LO
   TS
CP0388620
methyl N-[4-[7-amino-3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxypyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
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C28H32N6O5
 1
1
IC50 = 82 nM
   TI
   LI
   LO
   TS
CP0388616
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine
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C26H29N5O3
 1
1
IC50 = 400 nM
   TI
   LI
   LO
   TS
CP0061016
3-(4-Amino-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-phenol
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C17H18N4O
 1
1
IC50 = 480 nM
   TI
   LI
   LO
   TS
CP0418567
3-[4-amino-7-[3-(hydroxymethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-5-yl]phenol
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C17H18N4O2
 1
1
IC50 = 960 nM
   TI
   LI
   LO
   TS
CP0385508
2-[4-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetic acid
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C27H28FN7O2
 1
1
IC50 = 2500 nM
   TI
   LI
   LO
   TS
CP0388864
4-[6-(benzylamino)imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C20H15N5
 1
1
IC50 = 3400 nM
   TI
   LI
   LO
   TS
CP0388615
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-(1,3-thiazol-2-yl)pyrazolo[1,5-a]pyrimidin-7-amine
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C23H26N6O3S
 1
1
IC50 = 4300 nM
   TI
   LI
   LO
   TS
CP0385511
1-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-ol
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C26H27FN6O
 1
1
IC50 = 5300 nM
   TI
   LI
   LO
   TS
CP0395047
6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]-3-pyridin-2-ylimidazo[1,2-b]pyridazine
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C21H18FN5
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0138866
1-[4-[3-[4-amino-5-(2-fluoro-5-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone
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C22H25FN6O2
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0005166
BMS-354825
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C22H26ClN7O2S
 3
1 IC50 = 0.57 nM
2 IC50 = 5.012 nM
3 Kd = 0.58 nM
CP0161333
4-cyano-N-[4-(4-methylpiperazin-1-yl)-2-(4-methylpiperidin-1-yl)phenyl]-1H-pyrrole-2-carboxamide
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C23H30N6O
 1
1 IC50 = 0.8 nM
CP0120760
5-cyano-N-(4-(4-methylpiperazin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C22H27N5O2
 1
1 IC50 = 0.8 nM
CP0344654
5-cyano-N-(4-(4-methylpiperazin-1-yl)-2-(4-methylpiperidin-1-yl)phenyl)furan-2-carboxamide
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C23H29N5O2
 1
1 IC50 = 1 nM
CP0137907
2-(4-methylpiperazin-1-yl)-N-[4-methyl-5-[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]-1,3-thiazol-2-yl]acetamide
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C25H27N7OS
 1
1 IC50 = 1.2 nM
CP0579995
5-[6-methyl-5-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxypyridin-2-yl]-2-(propan-2-ylamino)-1H-pyrimidin-6-one
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C22H23N7O2
 1
1 IC50 = 1.6 nM
CP0133124
5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine
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C20H15ClF3N5
 4
1 IC50 = 1.7 nM
2 IC50 = 12 nM
3 IC50 = 13 nM
4 IC50 = 20 nM
CP0161570
4-cyano-N-(4-(4-methylpiperazin-1-yl)-2-(piperidin-1-yl)phenyl)-1H-pyrrole-2-carboxamide
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C22H28N6O
 1
1 IC50 = 2 nM
CP0568954
2-(cyclopropylamino)-3-methyl-5-[6-methyl-5-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxypyridin-2-yl]pyrimidin-4-one
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C23H23N7O2
 1
1 IC50 = 2 nM
CP0545184
2-(cyclopropylamino)-5-[6-methyl-5-[2-(1-methylpyrazol-4-yl)pyridin-4-yl]oxypyridin-2-yl]-1H-pyrimidin-6-one
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C22H21N7O2
 1
1 IC50 = 3.6 nM
CP0540361
DCC-3014
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C23H25N7O2
 1
1 IC50 = 3.7 nM
CP0315539
5-cyano-N-(5-hydroxy-2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C17H17N3O3
 1
1 IC50 = 17 nM
CP0321403
5-cyano-N-(2,5-di(piperidin-1-yl)phenyl)furan-2-carboxamide
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C22H26N4O2
 1
1 IC50 = 17 nM
CP0336739
5-cyano-N-(5-((2,3-dihydroxypropoxy)methyl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C21H25N3O5
 1
1 IC50 = 19 nM
CP0086098
5-cyano-N-[5-(hydroxymethyl)-2-(4-methylpiperidin-1-yl)phenyl]furan-2-carboxamide
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C19H21N3O3
 1
1 IC50 = 24 nM
CP0513780
5-cyano-N-(5-(hydroxymethyl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C18H19N3O3
 1
1 IC50 = 25 nM
CP0015521
5-[[3-methoxy-4-[(4-methoxyphenyl)methoxy]phenyl]methyl]pyrimidine-2,4-diamine
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C20H22N4O3
 5
1 IC50 = 30 nM
2 IC50 = 60 nM
3 IC50 = 470 nM
4 Kd = 1.6 nM
5 Kd = 2.2 nM
CP0370310
5-cyano-furan-2-carboxylic acid (5-guanidinomethyl-2-piperidin-1-yl-phenyl)-amide
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C19H22N6O2
 1
1 IC50 = 34 nM
CP0002211
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
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C22H27FN4O2
 4
1 IC50 = 35 nM
2 IC50 = 82.5 nM
3 Kd = 2 nM
4 Kd = 2.5 nM
CP0370313
5-cyano-N-(2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C17H17N3O2
 1
1 IC50 = 36 nM
CP0354096
5-cyano-N-(5-(methylsulfonamidomethyl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C19H22N4O4S
 1
1 IC50 = 37 nM
CP0369265
5-cyano-N-(5-formyl-2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C18H17N3O3
 1
1 IC50 = 37 nM
CP0370316
N-[2-[4-(2-hydroxyethyl)piperidin-1-yl]phenyl]-5-nitrofuran-2-carboxamide
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C18H21N3O5
 1
1 IC50 = 43 nM
CP0109216
4-nitro-N-(2-(piperidin-1-yl)phenyl)-1H-pyrrole-2-carboxamide
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C16H18N4O3
 1
1 IC50 = 47 nM
CP0302228
4-cyano-N-(2-(piperidin-1-yl)phenyl)-1H-pyrrole-2-carboxamide
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C17H18N4O
 1
1 IC50 = 47 nM
CP0368685
5-nitro-N-(2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C16H17N3O4
 2
1 IC50 = 47 nM
2 IC50 = 53 nM
CP0238677
(8E)-14-(2-pyrrolidin-1-ylethoxy)-6,11,25-trioxa-18,20,23-triazatetracyclo[17.3.1.12,5.113,17]pentacosa-1(23),2,4,8,13,15,17(24),19,21-nonaene
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C25H28N4O4
 1
1 IC50 = 69 nM
CP0526494
N-[2-(4-methylpiperidin-1-yl)phenyl]-5-nitrofuran-2-carboxamide
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C17H19N3O4
 1
1 IC50 = 78 nM
CP0177258
5-cyano-N-(5-((4-methylpiperazin-1-yl)methyl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C23H29N5O2
 1
1 IC50 = 80 nM
CP0370312
5-cyano-N-(5-methoxy-2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C18H19N3O3
 1
1 IC50 = 90 nM
CP0275670
4-[[[2-[3-(morpholin-4-ylmethyl)anilino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
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C22H26N6O3S
 1
1 IC50 = 91 nM
CP0177260
5-cyano-N-(5-cyano-2-(piperidin-1-yl)phenyl)furan-2-carboxamide
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C18H16N4O2
 1
1 IC50 = 120 nM
CP0302229
N-[2-[4-(hydroxymethyl)piperidin-1-yl]phenyl]-5-nitrofuran-2-carboxamide
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C17H19N3O5
 1
1 IC50 = 130 nM
CP0109217
N-[2-(4-hydroxypiperidin-1-yl)phenyl]-5-nitrofuran-2-carboxamide
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C16H17N3O5
 1
1 IC50 = 140 nM
CP0177261
N-[5-(aminomethyl)-2-piperidin-1-ylphenyl]-5-cyanofuran-2-carboxamide
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C18H20N4O2
 1
1 IC50 = 200 nM
CP0496364
4-[[[2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
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C17H18F3N7O2S
 1
1 IC50 = 233 nM
CP0541657
N-[2-(azepin-1-yl)phenyl]-5-nitrofuran-2-carboxamide
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C17H13N3O4
 1
1 IC50 = 260 nM
CP0169053
4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
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C17H17BrF3N7O2S
 1
1 IC50 = 264 nM
CP0551444
N-[3-[[4-[(4-sulfamoylphenyl)methylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
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C22H25N7O3S
 1
1 IC50 = 305 nM
CP0109220
N-[2-(3-methylpiperidin-1-yl)phenyl]-5-nitrofuran-2-carboxamide
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C17H19N3O4
 1
1 IC50 = 380 nM
CP0109218
N-[2-(4-methylpiperazin-1-yl)phenyl]-5-nitrofuran-2-carboxamide
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C16H18N4O4
 1
1 IC50 = 390 nM
CP0192173
N-(2-piperidin-1-ylphenyl)-1,2-oxazole-5-carboxamide
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C15H17N3O2
 1
1 IC50 = 400 nM
CP0340908
3-(2-cyanofuran-5-carboxamido)-4-(piperidin-1-yl)benzoic acid
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C18H17N3O4
 1
1 IC50 > 2000 nM
CP0041597
1-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-3-[1-(1,3-thiazol-2-yl)ethyl]urea
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C24H24N4O5S
 1
1 Kd = 0.83 nM
CP0034949
4-[6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl]-N-(4-propan-2-yloxyphenyl)piperazine-1-carboxamide
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C31H42N6O4
 1
1 Kd = 4.9 nM
CP0127888
AB-460
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C24H23N5O3
 1
1 Kd = 8.5 nM
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
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C29H31N7O
 3
1 Kd = 10 nM
2 Kd = 11 nM
3 Kd = 19 nM
CP0002230
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide
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C28H22F3N7O
 1
1 Kd = 45 nM
CP0034962
16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8(13),9,11,20(25),21,23-nonaen-3-one
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C26H21N3O4
 1
1 Kd = 110 nM
CP0016677
N-[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-N-methylbenzamide
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C35H30N4O4
 1
1 Kd = 330 nM
Clinical Information about the Protein
Target 1 ( Macrophage colony-stimulating factor 1 receptor (CSF1R) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Tenosynovial giant cell tumour [ICD-11: 2F7B]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3 Amyotrophic lateral sclerosis [ICD-11: 8B60.0]
Approved Drug(s) 1 Approved Drug  1
1 Pexidartinib Approved
Tenosynovial giant cell tumour
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 DCC-3014 Phase 1/2
Solid tumour/cancer
2 BLZ-945 Phase 2
Amyotrophic lateral sclerosis
Target 2 ( CSF1R messenger RNA (CSF1R mRNA) )
Target Type Literature-reported Target