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Investigational drugs are compounds that have been approved for testing in clinical trials. They have verified structure, manufacturing process, and quality control protocols as well as passed preliminary animal studies. Clinical trials will check if potential drugs work effectively and safely on humans. Compounds, successively passed all phases of clinical trials, can be submitted for FDA (or other pharmaceutical regulatory agency) approval to become a new drug.
The library of Investigational Drugs consists of 874 compounds that entered the first phase of clinical trials. All information about national clinical trial (NCT) numbers and annotated biological activity is also available.
Related terms: epidermal growth factor receptor, MET proto-oncogene, receptor tyrosine kinase, AKT serine/threonine kinase, aurora kinase A, mitogen-activated protein kinase
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NoteAll the compounds with solubility below 10 mM are shipped as 2 mM solutions.
epidermal growth factor receptor
20
20
Number of compounds
20
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta
16
16
Number of compounds
16
MET proto-oncogene, receptor tyrosine kinase
16
16
Number of compounds
16
kinase insert domain receptor
15
15
Number of compounds
15
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta
12
12
Number of compounds
12
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma
12
12
Number of compounds
12
AKT serine/threonine kinase 1
11
11
Number of compounds
11
aurora kinase A
11
11
Number of compounds
11
mitogen-activated protein kinase 14
9
9
Number of compounds
9
colony stimulating factor 1 receptor
9
9
Number of compounds
9
fms related receptor tyrosine kinase 1
9
9
Number of compounds
9
platelet derived growth factor receptor alpha
9
9
Number of compounds
9
platelet derived growth factor receptor beta
9
9
Number of compounds
9
phosphoinositide-3-kinase regulatory subunit 1
9
9
Number of compounds
9
mitogen-activated protein kinase 1
9
9
Number of compounds
9
aurora kinase B
9
9
Number of compounds
9
Janus kinase 2
8
8
Number of compounds
8
phosphatidylinositol 3-kinase catalytic subunit type 3
8
8
Number of compounds
8
D2 receptor
8
8
Number of compounds
8
fms related receptor tyrosine kinase 3
8
8
Number of compounds
8
mitogen-activated protein kinase kinase 1
8
8
Number of compounds
8
fms related receptor tyrosine kinase 4
8
8
Number of compounds
8
Janus kinase 1
7
7
Number of compounds
7
Janus kinase 3
7
7
Number of compounds
7
B-Raf proto-oncogene, serine/threonine kinase
7
7
Number of compounds
7
Raf-1 proto-oncogene, serine/threonine kinase
7
7
Number of compounds
7
fibroblast growth factor receptor 1
7
7
Number of compounds
7
histone deacetylase 2
6
6
Number of compounds
6
histone deacetylase 3
6
6
Number of compounds
6
histone deacetylase 1
6
6
Number of compounds
6
ret proto-oncogene
6
6
Number of compounds
6
Bruton tyrosine kinase
6
6
Number of compounds
6
erb-b2 receptor tyrosine kinase 2
6
6
Number of compounds
6
AXL receptor tyrosine kinase
6
6
Number of compounds
6
mitogen-activated protein kinase kinase 2
6
6
Number of compounds
6
D3 receptor
5
5
Number of compounds
5
LCK proto-oncogene, Src family tyrosine kinase
5
5
Number of compounds
5
Aryl hydrocarbon receptor
5
5
Number of compounds
5
macrophage stimulating 1 receptor
5
5
Number of compounds
5
fibroblast growth factor receptor 2
5
5
Number of compounds
5
tyrosine kinase 2
4
4
Number of compounds
4
histone deacetylase 6
4
4
Number of compounds
4
polo like kinase 1
4
4
Number of compounds
4
5-HT2A receptor
4
4
Number of compounds
4
mitogen-activated protein kinase 3
4
4
Number of compounds
4
sigma non-opioid intracellular receptor 1
4
4
Number of compounds
4
neurotrophic receptor tyrosine kinase 1
4
4
Number of compounds
4
discoidin domain receptor tyrosine kinase 1
4
4
Number of compounds
4
CYP1A2
4
4
Number of compounds
4
fibroblast growth factor receptor 4
4
4
Number of compounds
4
mitogen-activated protein kinase 11
4
4
Number of compounds
4
protein tyrosine kinase 2
4
4
Number of compounds
4
CYP1A1
4
4
Number of compounds
4
aurora kinase C
4
4
Number of compounds
4
fibroblast growth factor receptor 3
4
4
Number of compounds
4
AKT serine/threonine kinase 3
4
4
Number of compounds
4
AKT serine/threonine kinase 2
4
4
Number of compounds
4
carbonic anhydrase 2
4
4
Number of compounds
4
neurotrophic receptor tyrosine kinase 2
4
4
Number of compounds
4
neurotrophic receptor tyrosine kinase 3
4
4
Number of compounds
4
cyclin dependent kinase 2
4
4
Number of compounds
4
σ2
3
3
Number of compounds
3
Pim-1 proto-oncogene, serine/threonine kinase
3
3
Number of compounds
3
H1 receptor
3
3
Number of compounds
3
histone deacetylase 10
3
3
Number of compounds
3
Estrogen receptor-β
3
3
Number of compounds
3
EPH receptor B6
3
3
Number of compounds
3
YES proto-oncogene 1, Src family tyrosine kinase
3
3
Number of compounds
3
α1A-adrenoceptor
3
3
Number of compounds
3
α1D-adrenoceptor
3
3
Number of compounds
3
fyn related Src family tyrosine kinase
3
3
Number of compounds
3
BMX non-receptor tyrosine kinase
3
3
Number of compounds
3
TXK tyrosine kinase
3
3
Number of compounds
3
CB1 receptor
3
3
Number of compounds
3
heat shock protein 90 beta family member 1
3
3
Number of compounds
3
MER proto-oncogene, tyrosine kinase
3
3
Number of compounds
3
TEK receptor tyrosine kinase
3
3
Number of compounds
3
GluN2D
3
3
Number of compounds
3
CYP2E1
3
3
Number of compounds
3
BLK proto-oncogene, Src family tyrosine kinase
3
3
Number of compounds
3
IL2 inducible T cell kinase
3
3
Number of compounds
3
Insulin receptor
3
3
Number of compounds
3
Insulin-like growth factor I receptor
3
3
Number of compounds
3
Mineralocorticoid receptor
3
3
Number of compounds
3
casein kinase 2, alpha 1 polypeptide subunit
3
3
Number of compounds
3
carbonic anhydrase 9
3
3
Number of compounds
3
checkpoint kinase 1
3
3
Number of compounds
3
ABCG2
3
3
Number of compounds
3
glycogen synthase kinase 3 beta
3
3
Number of compounds
3
phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta
3
3
Number of compounds
3
amine oxidase copper containing 3
3
3
Number of compounds
3
LYN proto-oncogene, Src family tyrosine kinase
3
3
Number of compounds
3
CDC like kinase 2
3
3
Number of compounds
3
cyclin dependent kinase 4
3
3
Number of compounds
3
cyclin dependent kinase 6
3
3
Number of compounds
3
carbonic anhydrase 1
3
3
Number of compounds
3
NET
3
3
Number of compounds
3
MMP3
2
2
Number of compounds
2
MMP13
2
2
Number of compounds
2
histone deacetylase 8
2
2
Number of compounds
2
nemo like kinase
2
2
Number of compounds
2
phosphoinositide-3-kinase regulatory subunit 3
2
2
Number of compounds
2
Kv11.1
2
2
Number of compounds
2
WEE2 oocyte meiosis inhibiting kinase
2
2
Number of compounds
2
histone deacetylase 5
2
2
Number of compounds
2
α1B-adrenoceptor
2
2
Number of compounds
2
topoisomerase (DNA) I mitochondrial
2
2
Number of compounds
2
5-HT2C receptor
2
2
Number of compounds
2
signal transducer and activator of transcription 3
2
2
Number of compounds
2
S1P1 receptor
2
2
Number of compounds
2
TRPV1
2
2
Number of compounds
2
Angiotensin-converting enzyme 2
2
2
Number of compounds
2
EPH receptor A8
2
2
Number of compounds
2
TYRO3 protein tyrosine kinase
2
2
Number of compounds
2
ALK receptor tyrosine kinase
2
2
Number of compounds
2
STE20 like kinase
2
2
Number of compounds
2
serine/threonine kinase 10
2
2
Number of compounds
2
mitogen-activated protein kinase kinase kinase 1
2
2
Number of compounds
2
ribosomal protein S6 kinase A5
2
2
Number of compounds
2
GluN2C
2
2
Number of compounds
2
CDC like kinase 3
2
2
Number of compounds
2
CYP1B1
2
2
Number of compounds
2
serine/threonine kinase 35
2
2
Number of compounds
2
pancreatic lipase
2
2
Number of compounds
2
mitogen-activated protein kinase kinase kinase 3
2
2
Number of compounds
2
FER tyrosine kinase
2
2
Number of compounds
2
NRAS
2
2
Number of compounds
2
CB2 receptor
2
2
Number of compounds
2
Organic cation transporter 2
2
2
Number of compounds
2
MDM2 proto-oncogene
2
2
Number of compounds
2
EPH receptor A2
2
2
Number of compounds
2
c-ros oncogene 1, receptor tyrosine kinase
2
2
Number of compounds
2
discoidin domain receptor tyrosine kinase 2
2
2
Number of compounds
2
FYN proto-oncogene, Src family tyrosine kinase
2
2
Number of compounds
2
ZAK sterile alpha motif and leucine zipper containing kinase AZK
2
2
Number of compounds
2
A1 receptor
2
2
Number of compounds
2
Pregnane X receptor
2
2
Number of compounds
2
protein kinase C alpha
2
2
Number of compounds
2
protein kinase C delta
2
2
Number of compounds
2
protein kinase C epsilon
2
2
Number of compounds
2
protein kinase C eta
2
2
Number of compounds
2
protein kinase C theta
2
2
Number of compounds
2
DAT
2
2
Number of compounds
2
SERT
2
2
Number of compounds
2
activin A receptor type 1B
2
2
Number of compounds
2
transforming growth factor beta receptor 1
2
2
Number of compounds
2
cyclin dependent kinase 9
2
2
Number of compounds
2
casein kinase 1 alpha 1
2
2
Number of compounds
2
casein kinase 1 epsilon
2
2
Number of compounds
2
mitogen-activated protein kinase kinase kinase kinase 4
2
2
Number of compounds
2
ABCB1
2
2
Number of compounds
2
receptor interacting serine/threonine kinase 2
2
2
Number of compounds
2
Organic anion transporter 1
1
1
Number of compounds
1
MMP1
1
1
Number of compounds
1
MMP9
1
1
Number of compounds
1
ADAM9
1
1
Number of compounds
1
ADAM10
1
1
Number of compounds
1
ADAM17
1
1
Number of compounds
1
histone deacetylase 11
1
1
Number of compounds
1
mitogen-activated protein kinase 10
1
1
Number of compounds
1
phosphodiesterase 4A
1
1
Number of compounds
1
phosphodiesterase 4B
1
1
Number of compounds
1
phosphodiesterase 4C
1
1
Number of compounds
1
phosphodiesterase 4D
1
1
Number of compounds
1
phosphodiesterase 10A
1
1
Number of compounds
1
cyclin G associated kinase
1
1
Number of compounds
1
mitogen-activated protein kinase kinase kinase 19
1
1
Number of compounds
1
mitogen-activated protein kinase kinase kinase 4
1
1
Number of compounds
1
NIMA related kinase 3
1
1
Number of compounds
1
polo like kinase 2
1
1
Number of compounds
1
polo like kinase 3
1
1
Number of compounds
1
WEE1 G2 checkpoint kinase
1
1
Number of compounds
1
NADPH oxidase 1
1
1
Number of compounds
1
M1 receptor
1
1
Number of compounds
1
V1A receptor
1
1
Number of compounds
1
V2 receptor
1
1
Number of compounds
1
Nav1.2
1
1
Number of compounds
1
CFTR
1
1
Number of compounds
1
CYP51A1
1
1
Number of compounds
1
μ receptor
1
1
Number of compounds
1
ribosomal protein S6 kinase A1
1
1
Number of compounds
1
5-HT1A receptor
1
1
Number of compounds
1
5-HT1B receptor
1
1
Number of compounds
1
5-HT2B receptor
1
1
Number of compounds
1
Kv1.1
1
1
Number of compounds
1
Kv1.3
1
1
Number of compounds
1
Kv1.4
1
1
Number of compounds
1
Kv1.5
1
1
Number of compounds
1
Kv1.6
1
1
Number of compounds
1
UDP-glucose ceramide glucosyltransferase
1
1
Number of compounds
1
carbonic anhydrase 13
1
1
Number of compounds
1
LPA1 receptor
1
1
Number of compounds
1
α2B-adrenoceptor
1
1
Number of compounds
1
RyR1
1
1
Number of compounds
1
kelch like ECH-associated protein 1
1
1
Number of compounds
1
EPH receptor A3
1
1
Number of compounds
1
EPH receptor A6
1
1
Number of compounds
1
EPH receptor A7
1
1
Number of compounds
1
tyrosine kinase with immunoglobulin like and EGF like domains 1
1
1
Number of compounds
1
homeodomain interacting protein kinase 4
1
1
Number of compounds
1
mitogen-activated protein kinase kinase 5
1
1
Number of compounds
1
CCK1 receptor
1
1
Number of compounds
1
activin A receptor type 1
1
1
Number of compounds
1
bone morphogenetic protein receptor type IB
1
1
Number of compounds
1
phosphatidylinositol 4-kinase beta
1
1
Number of compounds
1
ribosomal protein S6 kinase B1
1
1
Number of compounds
1
Cav2.2
1
1
Number of compounds
1
mGlu5 receptor
1
1
Number of compounds
1
Ecto-5'-Nucleotidase
1
1
Number of compounds
1
CYP2A7
1
1
Number of compounds
1
tubulin alpha 1a
1
1
Number of compounds
1
PMCA4
1
1
Number of compounds
1
tec protein tyrosine kinase
1
1
Number of compounds
1
kallikrein related peptidase 7
1
1
Number of compounds
1
MAPK activated protein kinase 2
1
1
Number of compounds
1
serine/threonine kinase 17b
1
1
Number of compounds
1
GPR119
1
1
Number of compounds
1
TRPA1
1
1
Number of compounds
1
CXCR1
1
1
Number of compounds
1
CXCR2
1
1
Number of compounds
1
proteasome 20S subunit beta 5
1
1
Number of compounds
1
Monoacylglycerol lipase
1
1
Number of compounds
1
GABAA receptor α1 subunit
1
1
Number of compounds
1
GABAA receptor β2 subunit
1
1
Number of compounds
1
GABAA receptor δ subunit
1
1
Number of compounds
1
erb-b2 receptor tyrosine kinase 3
1
1
Number of compounds
1
Farnesoid X receptor
1
1
Number of compounds
1
nuclear receptor coactivator 1
1
1
Number of compounds
1
carbonic anhydrase 7
1
1
Number of compounds
1
beta-secretase 1
1
1
Number of compounds
1
acetylcholinesterase (Cartwright blood group)
1
1
Number of compounds
1
megakaryocyte-associated tyrosine kinase
1
1
Number of compounds
1
Endothelin-converting enzyme 1
1
1
Number of compounds
1
nicotinic acetylcholine receptor α4 subunit
1
1
Number of compounds
1
ATR serine/threonine kinase
1
1
Number of compounds
1
A2B receptor
1
1
Number of compounds
1
bromodomain containing 2
1
1
Number of compounds
1
bromodomain testis associated
1
1
Number of compounds
1
tyrosinase
1
1
Number of compounds
1
p21 (RAC1) activated kinase 1
1
1
Number of compounds
1
protein kinase, DNA-activated, catalytic subunit
1
1
Number of compounds
1
histone deacetylase 4
1
1
Number of compounds
1
histone H3 associated protein kinase
1
1
Number of compounds
1
Pim-3 proto-oncogene, serine/threonine kinase
1
1
Number of compounds
1
αβ-Hydrolase 2
1
1
Number of compounds
1
GlyT1
1
1
Number of compounds
1
PROT
1
1
Number of compounds
1
KNa1.1
1
1
Number of compounds
1
Nav1.8
1
1
Number of compounds
1
Neutral endopeptidase
1
1
Number of compounds
1
EPH receptor A1
1
1
Number of compounds
1
doublecortin like kinase 1
1
1
Number of compounds
1
doublecortin like kinase 2
1
1
Number of compounds
1
FES proto-oncogene, tyrosine kinase
1
1
Number of compounds
1
protein tyrosine kinase 2 beta
1
1
Number of compounds
1
serine/threonine kinase 4
1
1
Number of compounds
1
protein kinase AMP-activated catalytic subunit alpha 1
1
1
Number of compounds
1
protein kinase AMP-activated catalytic subunit alpha 2
1
1
Number of compounds
1
protein kinase AMP-activated non-catalytic subunit beta 1
1
1
Number of compounds
1
protein kinase AMP-activated non-catalytic subunit gamma 1
1
1
Number of compounds
1
Acetyl-CoA carboxylase 1
1
1
Number of compounds
1
Acetyl-CoA carboxylase 2
1
1
Number of compounds
1
EPH receptor A5
1
1
Number of compounds
1
EPH receptor B1
1
1
Number of compounds
1
Inducible NOS
1
1
Number of compounds
1
HPGD
1
1
Number of compounds
1
5-HT3A
1
1
Number of compounds
1
GPR84
1
1
Number of compounds
1
D1 receptor
1
1
Number of compounds
1
phosphoinositide-3-kinase regulatory subunit 2
1
1
Number of compounds
1
poly(ADP-ribose) polymerase 1
1
1
Number of compounds
1
TAAR3
1
1
Number of compounds
1
src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites
1
1
Number of compounds
1
Neuron-derived orphan receptor 1
1
1
Number of compounds
1
erb-b2 receptor tyrosine kinase 4
1
1
Number of compounds
1
muscle associated receptor tyrosine kinase
1
1
Number of compounds
1
interleukin 1 receptor associated kinase 1
1
1
Number of compounds
1
glycine receptor α1 subunit
1
1
Number of compounds
1
A2A receptor
1
1
Number of compounds
1
mitogen-activated protein kinase kinase kinase kinase 2
1
1
Number of compounds
1
NIMA related kinase 2
1
1
Number of compounds
1
polo like kinase 4
1
1
Number of compounds
1
serine/threonine kinase 3
1
1
Number of compounds
1
tyrosine kinase non receptor 2
1
1
Number of compounds
1
mitogen-activated protein kinase kinase kinase 5
1
1
Number of compounds
1
Peroxisome proliferator-activated receptor-α
1
1
Number of compounds
1
coagulation factor II, thrombin
1
1
Number of compounds
1
kallikrein B1
1
1
Number of compounds
1
plasminogen activator, tissue type
1
1
Number of compounds
1
P2X7
1
1
Number of compounds
1
Cav1.2
1
1
Number of compounds
1
TRPM6
1
1
Number of compounds
1
receptor interacting serine/threonine kinase 4
1
1
Number of compounds
1
COX-1
1
1
Number of compounds
1
COX-2
1
1
Number of compounds
1
mitogen-activated protein kinase kinase kinase 8
1
1
Number of compounds
1
citron rho-interacting serine/threonine kinase
1
1
Number of compounds
1
receptor activator of NF-kappa B
1
1
Number of compounds
1
carbonic anhydrase 4
1
1
Number of compounds
1
carbonic anhydrase 12
1
1
Number of compounds
1
activin A receptor type 2B
1
1
Number of compounds
1
protein kinase A
1
1
Number of compounds
1
TLR7
1
1
Number of compounds
1
dual specificity tyrosine phosphorylation regulated kinase 1A
1
1
Number of compounds
1
mitogen-activated protein kinase 15
1
1
Number of compounds
1
protein kinase C beta
1
1
Number of compounds
1
Protein kinase G (PKG) 2
1
1
Number of compounds
1
ribosomal protein S6 kinase A3
1
1
Number of compounds
1
ribosomal protein S6 kinase A6
1
1
Number of compounds
1
α2A-adrenoceptor
1
1
Number of compounds
1
α2C-adrenoceptor
1
1
Number of compounds
1
D4 receptor
1
1
Number of compounds
1
Y5 receptor
1
1
Number of compounds
1
5-HT4 receptor
1
1
Number of compounds
1
FFA1 receptor
1
1
Number of compounds
1
κ receptor
1
1
Number of compounds
1
casein kinase 1 delta
1
1
Number of compounds
1
misshapen like kinase 1
1
1
Number of compounds
1
mitogen-activated protein kinase 9
1
1
Number of compounds
1
mitogen-activated protein kinase kinase kinase 2
1
1
Number of compounds
1
glycogen synthase kinase 3 alpha
1
1
Number of compounds
1
NLRP3
1
1
Number of compounds
1
GlyT2
1
1
Number of compounds
1
TAO kinase 3
1
1
Number of compounds
1
Alanine/serine/cysteine transporter 2
1
1
Number of compounds
1
Casein kinase 2
1
1
Number of compounds
1
casein kinase 2, beta polypeptide subunit
1
1
Number of compounds
1
KCa1.1
1
1
Number of compounds
1
Monoamine oxidase A
1
1
Number of compounds
1
Monoamine oxidase B
1
1
Number of compounds
1
NK1 receptor
1
1
Number of compounds
1
epoxide hydrolase 2
1
1
Number of compounds
1
serine/threonine-protein kinase MST4
1
1
Number of compounds
1
glutathione-disulfide reductase
1
1
Number of compounds
1
protein kinase, cAMP-dependent, catalytic, alpha subunit
1
1
Number of compounds
1
mitogen-activated protein kinase 4
1
1
Number of compounds
1
MAPK interacting serine/threonine kinase 1
1
1
Number of compounds
1
MAPK interacting serine/threonine kinase 2
1
1
Number of compounds
1
Sodium/bile acid and sulphated solute cotransporter 2
1
1
Number of compounds
1
β1-adrenoceptor
1
1
Number of compounds
1
Aminopeptidase N
1
1
Number of compounds
1
Arginyl aminopeptidase
1
1
Number of compounds
1
Leucine aminopeptidase 3
1
1
Number of compounds
1
CXCR4
1
1
Number of compounds
1
B1 receptor
1
1
Number of compounds
1
B2 receptor
1
1
Number of compounds
1
TLR2
1
1
Number of compounds
1
TLR4
1
1
Number of compounds
1
Transforming growth factor β receptor
1
1
Number of compounds
1
Rho associated coiled-coil containing protein kinase 2
1
1
Number of compounds
1
lysine demethylase 1A
1
1
Number of compounds
1
cyclin dependent kinase 1
1
1
Number of compounds
1
cyclin dependent kinase 16
1
1
Number of compounds
1
cyclin dependent kinase 17
1
1
Number of compounds
1
cyclin dependent kinase 5
1
1
Number of compounds
1
cyclin dependent kinase 7
1
1
Number of compounds
1
C-terminal Src kinase
1
1
Number of compounds
1
protein tyrosine kinase 6
1
1
Number of compounds
1
SRC proto-oncogene, non-receptor tyrosine kinase
1
1
Number of compounds
1
tribbles pseudokinase 3
1
1
Number of compounds
1
Guanylyl cyclase-G
1
1
Number of compounds
1
EBCL-0026