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Xpress Knock-Out

Full Knock-out  lines to validate MoA and to understand  biology  of targets.

α2-Adrenergic Receptor

Key Phenotype

Hypersensitivity to Anxiety Stimulants

Clonidine

EC50 in WT (ug)

0.02

EC50 in  KO = None

AT1

Key Phenotype

Elevated Blood Pressure and Hyperactivity

Losartan

EC50 in WT (ug)

5

EC50 in  KO = None

CHRNB3

Key Phenotype

Latency to Induced Anxiety

Cisatracurium

EC50 in WT (ug)

0.003

EC50 in  KO = None

Catechol-O-methyltransferase

Key Phenotype

Latency to depression

Entacapone

EC50 in WT (ug)

20

EC50 in  KO = None

Cytochrome P450 2D6

Key Phenotype

Latency to depression

Fluoxetine

EC50 in WT (ug)

2

EC50 in  KO = None

Dopamine D1R

Key Phenotype

Lack of reward motivation

apomorphine

EC50 in WT (ug)

1.875

EC50 in  KO = None

eIF2B

Key Phenotype

Latency to MPTP toxicity

curcumin

EC50 in WT (ug)

100

EC50 in  KO = None

GCase

Key Phenotype

Restricted Locomotion

Ambroxol

EC50 in WT (ug)

6.5

EC50 in  KO = None

GLP2R

Key Phenotype

Accelerated gastric emoting, High food consumption

glepaglutide

EC50 in WT (ug)

0.5

EC50 in  KO = None

GRIN1

Key Phenotype

Marked Learning Deficits

Lorazepam

EC50 in WT (ug)

0.3125

EC50 in  KO = None

HRH1

Key Phenotype

Severe Hyperactivity

Fexofenadine

EC50 in WT (ug)

18

EC50 in  KO = None

JAK1

Key Phenotype

Delayed Hypersensitivity to immunogens

Ruxolitinib

EC50 in WT (ug)

3

EC50 in  KO = None

KV1.1

Key Phenotype

Spontaneous Seizures

Niflumic acid

EC50 in WT (ug)

30

EC50 in  KO = None

M4 muscarinic

Key Phenotype

Latency to Pain response

Emraclidine

EC50 in WT (ug)

3.75

EC50 in  KO = None

MT1

Key Phenotype

Abnormal circadian pattern

Melatonin

EC50 in WT (ug)

0.3125

EC50 in  KO = None

Muscarine M1

Key Phenotype

Delayed inflammatory response

telenzepine

EC50 in WT (ug)

0.3

EC50 in  KO = None

NaV1.6

Key Phenotype

Hypokinesia Behaviour

​

EC50 in WT (ug)

-

EC50 in  KO = None

NMDA NR2B

Key Phenotype

Socially Isolated

ifenprodil

EC50 in WT (ug)

6

EC50 in  KO = None

P2X3

Key Phenotype

Latency to Pain Stimuli

Camlipixant

EC50 in WT (ug)

10

EC50 in  KO = None

PINK1

Key Phenotype

Fatigue, High ROS

Regorafenib

EC50 in WT (ug)

16

EC50 in  KO = None

SV2A

Key Phenotype

Resistant to hyperactivity

Levetiracetam

EC50 in WT (ug)

125

EC50 in  KO = None

TRPV1

Key Phenotype

Latency to temperature stimulation

Capsazepine

EC50 in WT (ug)

0.4

EC50 in  KO = None

V1aR

Key Phenotype

Latency to saline induced hypertension

Tolvaptan

EC50 in WT (ug)

1.5

EC50 in  KO = None

ADORA1

Key Phenotype

Latency to Pain

Naxifylline

EC50 in WT (ug)

150

EC50 in  KO = None

BCHE

Key Phenotype

Early obesity on high fat diet

Fenoverine

EC50 in WT (ug)

37.5

EC50 in  KO = None

CACNA1C

Key Phenotype

Severe Aggression and hypotensive

Amlodipine

EC50 in WT (ug)

0.5

EC50 in  KO = None

CCR1

Key Phenotype

Latency to induced inflammation

CCX-354

EC50 in WT (ug)

15

EC50 in  KO = None

D5/DRD5

Key Phenotype

Preference for high stimuli environment

Cabergoline

EC50 in WT (ug)

0.05

EC50 in  KO = None

Dopamine D2R

Key Phenotype

Highly receptive to reward

haloperidol

EC50 in WT (ug)

0.625

EC50 in  KO = None

Eotaxin

Key Phenotype

Latency to intestinal inflammation

Cetirizine

EC50 in WT (ug)

1

EC50 in  KO = None

Ghrelin

Key Phenotype

Latency to feed search under minimal feed regime

L-cysteine

EC50 in WT (ug)

50

EC50 in  KO = None

GPR6

Key Phenotype

Hypersensitivity to inflammation

SR144528

EC50 in WT (ug)

0

EC50 in  KO = None

GRIN2A

Key Phenotype

Marked Learning Deficits

Memantine

EC50 in WT (ug)

0.625

EC50 in  KO = None

HTR1A

Key Phenotype

Episodic Anxiety

Flesinoxan

EC50 in WT (ug)

1.25

EC50 in  KO = None

KCNK13

Key Phenotype

Delayed response to immunogens

Nicorandil

EC50 in WT (ug)

2.5

EC50 in  KO = None

Kv7

Key Phenotype

Resistance to epileptic medicines

retigabine

EC50 in WT (ug)

30

EC50 in  KO = None

MAPK

Key Phenotype

Latency to immunogen hypersensitivity

Cobimetinib

EC50 in WT (ug)

6

EC50 in  KO = None

mTOR

Key Phenotype

Latency to inflammation

Everolimus

EC50 in WT (ug)

1

EC50 in  KO = None

MuSK

Key Phenotype

Latency to immune response

Imatinib

EC50 in WT (ug)

40

EC50 in  KO = None

NF-κB

Key Phenotype

Slow Growth rate, Susceptible to swim bladder infections.

Sodium salicylate

EC50 in WT (ug)

150

EC50 in  KO = None

Nrf2

Key Phenotype

Resistant to oxidative damage

Omaveloxolone

EC50 in WT (ug)

15

EC50 in  KO = None

PDE4D

Key Phenotype

Latency to skin inflammation

Apremilast

EC50 in WT (ug)

1

EC50 in  KO = None

PTAFR

Key Phenotype

Latency to aversive temperature

Donepezil

EC50 in WT (ug)

0.5

EC50 in  KO = None

Transthyretin

Key Phenotype

Delayed a-syn toxicity

Diflunisal

EC50 in WT (ug)

100

EC50 in  KO = None

TYK2

Key Phenotype

Delayed innate immune response

Deucravacitinib

EC50 in WT (ug)

0.6

EC50 in  KO = None

V1B

Key Phenotype

Latency to anxiety

Terlipressin

EC50 in WT (ug)

0.34

EC50 in  KO = None

AMPA

Key Phenotype

Latency to hyperactivity

Talampanel

EC50 in WT (ug)

0.25

EC50 in  KO = None

CHRNA1

Key Phenotype

Delayed muscle contraction

Memantine

EC50 in WT (ug)

0.625

EC50 in  KO = None

Casein kinase 1δ

Key Phenotype

Latency to a-syn aggregation toxicity

Trapidil

EC50 in WT (ug)

20

EC50 in  KO = None

CNR1/CB1

Key Phenotype

Latency to hyperactivity

Rimonabant

EC50 in WT (ug)

2

EC50 in  KO = None

Delta Opioid

Key Phenotype

Increased perception of pain

naltrindole

EC50 in WT (ug)

0.3

EC50 in  KO = None

DPPI

Key Phenotype

Latency to allergic inflammatory response

Sitagliptin

EC50 in WT (ug)

10

EC50 in  KO = None

GABAAR

Key Phenotype

Sensitive to Anxiety

Taurine

EC50 in WT (ug)

300

EC50 in  KO = None

GLP-1R

Key Phenotype

Protected from High Fat diet induced pathology

Semaglutide

EC50 in WT (ug)

0.3

EC50 in  KO = None

GRIK4

Key Phenotype

Anhedonia with social withdrawal

Citalopram

EC50 in WT (ug)

2

EC50 in  KO = None

5HT2C

Key Phenotype

High impulsivity

Vabicaserin

EC50 in WT (ug)

1

EC50 in  KO = None

HTR2B

Key Phenotype

Socially Isolated with reduced Memory

Cariprazine

EC50 in WT (ug)

0.1875

EC50 in  KO = None

KOR

Key Phenotype

Latency to depression

Levorphanol:

EC50 in WT (ug)

0.15

EC50 in  KO = None

LRRK2

Key Phenotype

Delayed inflammatory response

Crizotinib

EC50 in WT (ug)

50

EC50 in  KO = None

MET

Key Phenotype

Early Neuronal degeneration

Crizotinib

EC50 in WT (ug)

50

EC50 in  KO = None

Mu Opioid

Key Phenotype

Latency to GI dysfunction

Morphine

EC50 in WT (ug)

3.75

EC50 in  KO = None

Nav1.2

Key Phenotype

Spontaneous Psychosis like behaviour

lidocaine

EC50 in WT (ug)

7

EC50 in  KO = None

NLRP3

Key Phenotype

Latency to eczema

Entrectinib

EC50 in WT (ug)

60

EC50 in  KO = None

Orexin 1

Key Phenotype

Increased sleep bouts

Lemborexant

EC50 in WT (ug)

0.625

EC50 in  KO = None

PDE5

Key Phenotype

Hypertension

Avanafil

EC50 in WT (ug)

10

EC50 in  KO = None

RIPKI

Key Phenotype

Resistance to inflammatory cell death

Quizartinib

EC50 in WT (ug)

3.54

EC50 in  KO = None

TREM2

Key Phenotype

Low Microglia activation in Multiple Sclerosis, slow to develop Ulcerative Colitis

Nilotinib

EC50 in WT (ug)

60

EC50 in  KO = None

USP30

Key Phenotype

Latency to MPTP Toxicity, Reduced ROS

CMPD-39

EC50 in WT (ug)

0.12

EC50 in  KO = None

VMAT2

Key Phenotype

Resistance to hyperkinesia, Dystonia

Tetrabenazine

EC50 in WT (ug)

1.25

EC50 in  KO = None

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