General Information of the Protein
Protein ID
PT03805
Protein Name
Sodium/hydrogen exchanger 1
Secondarily
Protein Name
APNH
Na(+)/H(+) antiporter
amiloride-sensitive
Na(+)/H(+) exchanger 1
Solute carrier family 9 member 1
Gene Name
SLC9A1
Secondarily
Gene Name
APNH1
NHE1
Sequence
MVLRSGICGLSPHRIFPSLLVVVALVGLLPVLRSHGLQLSPTASTIRSSEPPRERSIGDVTTAPPEVTPESRPVNHSVTDHGMKPRKAFPVLGIDYTHVRTPFEISLWILLACLMKIGFHVIPTISSIVPESCLLIVVGLLVGGLIKGVGETPPFLQSDVFFLFLLPPIILDAGYFLPLRQFTENLGTILIFAVVGTLWNAFFLGGLMYAVCLVGGEQINNIGLLDNLLFGSIISAVDPVAVLAVFEEIHINELLHILVFGESLLNDAVTVVLYHLFEEFANYEHVGIVDIFLGFLSFFVVALGGVLVGVVYGVIAAFTSRFTSHIRVIEPLFVFLYSYMAYLSAELFHLSGIMALIASGVVMRPYVEANISHKSHTTIKYFLKMWSSVSETLIFIFLGVSTVAGSHHWNWTFVISTLLFCLIARVLGVLGLTWFINKFRIVKLTPKDQFIIAYGGLRGAIAFSLGYLLDKKHFPMCDLFLTAIITVIFFTVFVQGMTIRPLVDLLAVKKKQETKRSINEEIHTQFLDHLLTGIEDICGHYGHHHWKDKLNRFNKKYVKKCLIAGERSKEPQLIAFYHKMEMKQAIELVESGGMGKIPSAVSTVSMQNIHPKSLPSERILPALSKDKEEEIRKILRNNLQKTRQRLRSYNRHTLVADPYEEAWNQMLLRRQKARQLEQKINNYLTVPAHKLDSPTMSRARIGSDPLAYEPKEDLPVITIDPASPQSPESVDLVNEELKGKVLGLSRDPAKVAEEDEDDDGGIMMRSKETSSPGTDDVFTPAPSDSPSSQRIQRCLSDPGPHPEPGEGEPFFPKGQ
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Organism
Homo sapiens, Human
Protein Classification
Transporter
>
Electrochemical transporter
>
SLC superfamily of solute carriers
>
SLC09 family of sodium/hydrogen exchangers
Function
Electroneutral Na(+) /H(+) antiporter that extrudes Na(+) in exchange for external protons driven by the inward sodium ion chemical gradient, protecting cells from acidification that occurs from metabolism (PubMed:7110335, PubMed:7603840, PubMed:11532004, PubMed:11350981, PubMed:15035633, PubMed:14680478, PubMed:17073455, PubMed:22020933, PubMed:27650500, PubMed:15677483, PubMed:32130622, PubMed:17493937). Exchanges intracellular H(+) ions for extracellular Na(+) in 1:1 stoichiometry (By similarity). Plays a key role in maintening intracellular pH neutral and cell volume, and thus is important for cell growth, proliferation, migration and survival (PubMed:8901634, PubMed:12947095, PubMed:15096511, PubMed:22020933). In addition, can transport lithium Li(+) and functions also as a Na(+)/Li(+) antiporter (PubMed:7603840). SLC9A1 also functions in membrane anchoring and organization of scaffolding complexes that coordinate signaling inputs (PubMed:15096511).
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Uniprot ID
Primary ID:
P19634

Secondarily ID:
B1ALD6
D3DPL4
Q96EM2
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Ensembl ID
ENSG00000090020
HGNC ID
HGNC:11071
Subcellular Location
Cell membrane
Basolateral 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: CL000429 , AP-1
Compound ID Compound Name Compound Formula
CP0478335
(1R,3R)-3-(3-bromo-4-fluorophenyl)-N-(diaminomethylidene)-2,2-dimethylcyclopropane-1-carboxamide
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C13H15BrFN3O
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0526608
2-(5-(4-fluoro-3-methylphenyl)-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidin-2-yl)acetonitrile
   Show/Hide
C22H23FN6
 1
1
IC50 = 4.6 nM
   TI
   LI
   LO
   TS
CP0402747
(1R,3R)-N-(diaminomethylidene)-3-(3-ethyl-4-fluorophenyl)-2,2-dimethylcyclopropane-1-carboxamide
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C15H20FN3O
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0410748
(1R,3R)-N-(diaminomethylidene)-3-(2,5-dichlorophenyl)-2,2-dimethylcyclopropane-1-carboxamide
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C13H15Cl2N3O
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0047122
N-(diaminomethylidene)-2-methyl-5-methylsulfonyl-4-pyrrol-1-ylbenzamide
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C14H16N4O3S
 3
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
2
IC50 = 380 nM
   TI
   LI
   LO
   TS
3
IC50 = 400 nM
   TI
   LI
   LO
   TS
CP0501109
5-(1-(5-(3-chloro-4-fluorophenyl)pyrimidin-4-yl)piperidin-4-yl)-4-methyl-1H-imidazol-2-amine
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C19H20ClFN6
 1
1
IC50 = 5.4 nM
   TI
   LI
   LO
   TS
CP0524133
(1R,3R)-N-(diaminomethylidene)-3-(3,5-dichlorophenyl)-2,2-dimethylcyclopropane-1-carboxamide
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C13H15Cl2N3O
 1
1
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0505661
5-(4-fluoro-3-methylphenyl)-2-methoxy-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C21H24FN5O
 1
1
IC50 = 6.5 nM
   TI
   LI
   LO
   TS
CP0456449
5-(4-fluoro-3-methylphenyl)-2-isopropoxy-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C23H28FN5O
 1
1
IC50 = 7.4 nM
   TI
   LI
   LO
   TS
CP0528970
5-[(1R,3S)-3-(3,5-Dichloro-phenyl)-2,2-dimethyl-cyclopropyl]-4-methyl-1H-imidazol-2-ylamine
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C15H17Cl2N3
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0101915
BMS-284640
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C15H19N3O2
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0531746
(1R,3R)-N-(diaminomethylidene)-3-(3-methoxyphenyl)-2,2-dimethylcyclopropane-1-carboxamide
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C14H19N3O2
 1
1
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0448431
(1R,3R)-3-(3-chlorophenyl)-N-(diaminomethylidene)-2,2-dimethylcyclopropane-1-carboxamide
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C13H16ClN3O
 2
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
2
IC50 = 21 nM
   TI
   LI
   LO
   TS
CP0523765
5-(3-chloro-4-fluorophenyl)-2-methoxy-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C20H21ClFN5O
 1
1
IC50 = 15 nM
   TI
   LI
   LO
   TS
CP0497973
(1R,3R)-N-(diaminomethylidene)-3-(4-fluoro-3-propan-2-ylphenyl)-2,2-dimethylcyclopropane-1-carboxamide
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C16H22FN3O
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0503384
5-(4-fluoro-3-methylphenyl)-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C20H22FN5
 1
1
IC50 = 21 nM
   TI
   LI
   LO
   TS
CP0461468
4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)-5-m-tolylpyrimidine
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C20H23N5
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0110088
N-(diaminomethylidene)-3-methylsulfonyl-4-propan-2-ylbenzamide
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C12H17N3O3S
 3
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
2
IC50 = 3400 nM
   TI
   LI
   LO
   TS
3
IC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0440455
(1R,3R)-N-(diaminomethylidene)-3-(4-fluoro-3-methylphenyl)-2,2-dimethylcyclopropane-1-carboxamide
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C14H18FN3O
 1
1
IC50 = 32 nM
   TI
   LI
   LO
   TS
CP0495438
5-[(1R,3S)-3-(3-Chloro-phenyl)-2,2-dimethyl-cyclopropyl]-4-methyl-1H-imidazol-2-ylamine
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C15H18ClN3
 1
1
IC50 = 39 nM
   TI
   LI
   LO
   TS
CP0554892
(1S,2S)-N-(diaminomethylidene)-2-(2,5-dichlorophenyl)cyclopropane-1-carboxamide
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C11H11Cl2N3O
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0408382
5-(3-chloro-4-fluorophenyl)-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C19H19ClFN5
 1
1
IC50 = 41 nM
   TI
   LI
   LO
   TS
CP0101916
5-cyclopropyl-N-(diaminomethylidene)-1-quinolin-5-ylpyrazole-4-carboxamide
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C17H16N6O
 1
1
IC50 = 59 nM
   TI
   LI
   LO
   TS
CP0391008
5-(2-chlorophenyl)-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C19H20ClN5
 1
1
IC50 = 61 nM
   TI
   LI
   LO
   TS
CP0542813
5-(3-chlorophenyl)-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C19H20ClN5
 1
1
IC50 = 61 nM
   TI
   LI
   LO
   TS
CP0530055
(1R,3R)-N-(diaminomethylidene)-2,2-dimethyl-3-phenylcyclopropane-1-carboxamide
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C13H17N3O
 1
1
IC50 = 69 nM
   TI
   LI
   LO
   TS
CP0542812
2-(5-(4-fluoro-3-methylphenyl)-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidin-2-yl)-N-isopropylacetamide
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C25H31FN6O
 1
1
IC50 = 87 nM
   TI
   LI
   LO
   TS
CP0541557
(1S,2S)-2-(3-bromo-4-fluorophenyl)-N-(diaminomethylidene)cyclopropane-1-carboxamide
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C11H11BrFN3O
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0458931
(1S,2S)-N-(diaminomethylidene)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropane-1-carboxamide
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C13H15N3O2
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0565841
5-[(1R,3S)-3-(3,5-Dichloro-phenyl)-2,2-dimethyl-cyclopropyl]-1H-imidazol-2-ylamine
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C14H15Cl2N3
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0522889
4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)-5-o-tolylpyrimidine
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C20H23N5
 1
1
IC50 = 250 nM
   TI
   LI
   LO
   TS
CP0500527
(1S,2S)-2-(3-chlorophenyl)-N-(diaminomethylidene)cyclopropane-1-carboxamide
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C11H12ClN3O
 1
1
IC50 = 280 nM
   TI
   LI
   LO
   TS
CP0449456
5-(3-methoxyphenyl)-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C20H23N5O
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0503387
5-(4-chlorophenyl)-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C19H20ClN5
 1
1
IC50 = 350 nM
   TI
   LI
   LO
   TS
CP0522899
4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)-5-phenylpyrimidine
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C19H21N5
 1
1
IC50 = 520 nM
   TI
   LI
   LO
   TS
CP0448434
(1S,2S)-N-(diaminomethylidene)-2-(3-methoxyphenyl)cyclopropane-1-carboxamide
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C12H15N3O2
 1
1
IC50 = 540 nM
   TI
   LI
   LO
   TS
CP0528210
4-chloro-6-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)-5-phenylpyrimidine
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C19H20ClN5
 1
1
IC50 = 580 nM
   TI
   LI
   LO
   TS
CP0421386
5-[(1R,3S)-3-(3-Chloro-phenyl)-2,2-dimethyl-cyclopropyl]-1H-imidazol-2-ylamine
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C14H16ClN3
 1
1
IC50 = 750 nM
   TI
   LI
   LO
   TS
CP0526304
4-ethoxy-6-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)-5-phenylpyrimidine
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C21H25N5O
 1
1
IC50 = 820 nM
   TI
   LI
   LO
   TS
CP0449455
5-(2-methoxyphenyl)-4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C20H23N5O
 1
1
IC50 = 940 nM
   TI
   LI
   LO
   TS
CP0554847
5-[(1R,3S)-3-(3,5-Dichloro-phenyl)-2,2-dimethyl-cyclopropyl]-4-methyl-1H-imidazole
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C15H16Cl2N2
 1
1
IC50 = 950 nM
   TI
   LI
   LO
   TS
CP0449169
(1S,2S)-2-(2-chlorophenyl)-N-(diaminomethylidene)cyclopropane-1-carboxamide
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C11H12ClN3O
 1
1
IC50 = 980 nM
   TI
   LI
   LO
   TS
CP0408269
4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)-5-p-tolylpyrimidine
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C20H23N5
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0373156
(1S,2S)-N-(diaminomethylidene)-2-(3-nitrophenyl)cyclopropane-1-carboxamide
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C11H12N4O3
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0442995
(1S,2S)-N-(diaminomethylidene)-2-(4-fluorophenyl)cyclopropane-1-carboxamide
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C11H12FN3O
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0542437
N-[4-[1-[5-(3-chloro-4-fluorophenyl)pyrimidin-4-yl]piperidin-4-yl]-5-methyl-1H-imidazol-2-yl]acetamide
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C21H22ClFN6O
 1
1
IC50 = 1900 nM
   TI
   LI
   LO
   TS
CP0466376
5-[(1R,3R)-3-(2,3-Dihydro-benzofuran-4-yl)-2,2-dimethyl-cyclopropyl]-4-methyl-1H-imidazol-2-ylamine
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C17H21N3O
 1
1
IC50 = 2600 nM
   TI
   LI
   LO
   TS
CP0451518
(1S,2S)-2-(4-chlorophenyl)-N-(diaminomethylidene)cyclopropane-1-carboxamide
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C11H12ClN3O
 1
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
CP0454856
(1S,2S)-N-(diaminomethylidene)-2-phenylcyclopropane-1-carboxamide
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C11H13N3O
 1
1
IC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0422168
6-[(1R,3S)-3-(3,5-Dichloro-phenyl)-2,2-dimethyl-cyclopropyl]-pyrimidine-2,4-diamine
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C15H16Cl2N4
 1
1
IC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0511468
5-[(1R,3R)-3-(2,3-Dihydro-benzofuran-4-yl)-2,2-dimethyl-cyclopropyl]-1H-imidazol-2-ylamine
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C16H19N3O
 1
1
IC50 = 3800 nM
   TI
   LI
   LO
   TS
CP0453368
5-[(1R,3S)-3-(3,5-Dichloro-phenyl)-2,2-dimethyl-cyclopropyl]-1H-imidazole
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C14H14Cl2N2
 1
1
IC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0508673
1-[(1R,3S)-3-(3-Chloro-phenyl)-2,2-dimethyl-cyclopropyl]-2-methylsulfanyl-1H-imidazole
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C15H17ClN2S
 1
1
IC50 = 4850 nM
   TI
   LI
   LO
   TS
CP0528899
5-[(1R,3S)-3-(3-Chloro-phenyl)-2,2-dimethyl-cyclopropyl]-thiazol-2-ylamine
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C14H15ClN2S
 1
1
IC50 = 8000 nM
   TI
   LI
   LO
   TS
CP0542778
4-(4-(4-methyl-1H-imidazol-5-yl)piperidin-1-yl)-6-morpholino-5-phenylpyrimidine
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C23H28N6O
 1
1
IC50 = 8600 nM
   TI
   LI
   LO
   TS
CP0538913
1-[(1R,3S)-3-(2,3-Dihydro-benzofuran-4-yl)-2,2-dimethyl-cyclopropyl]-2-methylsulfanyl-1H-imidazole
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C17H20N2OS
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0467844
5-[(1R,3R)-3-(2,3-Dihydro-benzofuran-4-yl)-2,2-dimethyl-cyclopropyl]-4-methyl-1H-imidazole
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C17H20N2O
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0408268
5-(3-chloro-4-fluorophenyl)-4-(4-(1,4-dimethyl-1H-imidazol-5-yl)piperidin-1-yl)pyrimidine
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C20H21ClFN5
 1
1
IC50 = 11000 nM
   TI
   LI
   LO
   TS
CP0395299
(1S,2S)-N-(diaminomethylidene)-2-(4-propan-2-ylphenyl)cyclopropane-1-carboxamide
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C14H19N3O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0397805
(1S,2S)-N-(diaminomethylidene)-2-(4-nitrophenyl)cyclopropane-1-carboxamide
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C11H12N4O3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0438757
1-[(1R,3S)-3-(3,5-Dichloro-phenyl)-2,2-dimethyl-cyclopropyl]-1H-pyrazol-3-ylamine
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C14H15Cl2N3
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0465806
5-[(1R,3R)-3-(2,3-Dihydro-benzofuran-4-yl)-2,2-dimethyl-cyclopropyl]-[1,2,4]oxadiazol-3-ylamine
   Show/Hide
C15H17N3O2
 1
1
IC50 = 30000 nM
   TI
   LI
   LO
   TS
CP0467975
5-[(1R,3S)-3-(3,5-Dichloro-phenyl)-2,2-dimethyl-cyclopropyl]-thiazol-2-ylamine
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C14H14Cl2N2S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0477079
5-[(1R,3R)-3-(2,3-Dihydro-benzofuran-4-yl)-2,2-dimethyl-cyclopropyl]-thiazol-2-ylamine
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C16H18N2OS
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0528871
5-[(1R,3R)-3-(2,3-Dihydro-benzofuran-4-yl)-2,2-dimethyl-cyclopropyl]-1H-imidazole
   Show/Hide
C16H18N2O
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0731184
N-carbamimidoyl-3-(3-((E)-3-(diaminomethyleneamino)-2-methyl-3-oxoprop-1-enyl)phenyl)-2-methylacrylamide
   Show/Hide
C16H20N6O2
 1
1 IC50 = 2 nM
CP0047122
N-(diaminomethylidene)-2-methyl-5-methylsulfonyl-4-pyrrol-1-ylbenzamide
   Show/Hide
C14H16N4O3S
 1
1 IC50 = 5 nM
CP0024264
4-(1-acetylpiperidin-4-yl)-N-(diaminomethylidene)-3-(trifluoromethyl)benzamide
   Show/Hide
C16H19F3N4O2
 2
1 IC50 = 6 nM
2 IC50 ~ 6 nM
CP0101915
BMS-284640
   Show/Hide
C15H19N3O2
 1
1 IC50 = 9 nM
CP0110088
N-(diaminomethylidene)-3-methylsulfonyl-4-propan-2-ylbenzamide
   Show/Hide
C12H17N3O3S
 1
1 IC50 = 30 nM
CP0101916
5-cyclopropyl-N-(diaminomethylidene)-1-quinolin-5-ylpyrazole-4-carboxamide
   Show/Hide
C17H16N6O
 1
1 IC50 = 59 nM
CP0667979
N-carbamimidoyl-3-(2-((E)-3-(diaminomethyleneamino)-2-methyl-3-oxoprop-1-enyl)-4-methylphenyl)-2-methylacrylamide
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C17H22N6O2
 1
1 IC50 = 3600 nM
Clinical Information about the Protein
Target 1 ( Sodium/hydrogen exchanger 1 (SLC9A1) )
Target Type Clinical trial Target
Disease 3 Target-related Diseases  3
1 Angina pectoris [ICD-11: BA40]
2 Cardiac arrhythmias [ICD-11: BC9Z]
3 Heart arrhythmia [ICD-11: BC65]
Discontinued Drug(s) 3 Discontinued Drugs  3
1 CARIPORIDE Discontinued in Phase 2
Angina pectoris
2 ENIPORIDE Discontinued in Phase 2
Cardiac arrhythmias
3 HOE-694 Terminated
Heart arrhythmia
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT04400 Sodium/hydrogen exchanger 1 Rattus norvegicus, Rat