6_RFQ_attachment.pdf
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- Attached to
- TRND Malaria Williamson Profiling from lead optimization and safety profiling panels Federal contract opportunity
- Solicitation number
- NIHDA201800287
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List of safety targets
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44 Safety Targets
GPCR
ADENOSINE A(2A)
ADRENERGIC alpha(1A) alpha(2A) beta(1) beta(2)
CANNABINOID CB(1)
CB(2)
CHOLECYSTOKININ CCK(1) [CCK(A)]
DOPAMINE D(1)
D(2S)
ENDOTHELIN ET(A)
HISTAMINE H(1)
H(2)
MUSCARINIC M(1)
M(2) M(3)
OPIOD & OPIOD-LIKE delta(2) [DOP] kappa [KOP] mu [MOP]
SEROTONIN 5-HT (1A)
5-HT (1B)
5-HT (2A)
5-HT (2B)
VASOPRESSIN V(1A)
TRANSPORTERS
DOPAMINE dopamine transporter NOREPINEPHRINE norepinephrine transporter SEROTONIN 5-HT transporter
ION CHANNELS
GABA CHANNELS BZD [central]
GLUTAMATE CHANNELS NMDA
NICOTINIC CHANNELS N neuronal α4β2
SEROTONIN CHANNELS 5-HT(3)
Ca(2+) CHANNELS Ca(2+) channel [L, dihydropyridine site] K+ CHANNELS hERG [membrane preparation]
K(V) channel Na(+) CHANNELS Na(+) channel [site 2]
NUCLEAR RECEPTORS
STEROID NUCLEAR RECEPTORS AR
GR
KINASES
CTK Lck kinase
OTHER NON-KINASE ENZYMES
AA METABOLISM COX(1)
COX(2)
MONOAMINE & NEUROTRANSMITTER acetylcholinesterase
MAO-A
PHOSPHODIESTERASES PDE3A
PDE4D2
87 Safety Targets
GPCR
ADENOSINE A(1)
A(2A) ADRENERGIC alpha(1A) alpha(1B) alpha(1D) alpha(2A) alpha(2B) beta(1) beta(2)
ANGIOTENSIN II AT(1)
BRADYKININ B(2)
CANNABINOID CB(1)
CB(2)
CHEMOKINES CCR1
CXCR2 (IL-8B)
CHOLECYSTOKININ CCK(1) [CCK(A)]
CCK(2) [CCK(B)]
DOPAMINE D(1)
D(2L) D(2S)
ENDOTHELIN ET(A)
GABA GABA(B[1a]) GLUTAMATE mGlu5
HISTAMINE H(1)
H(2) LEUKOTRIENES CysLT(1) [LTD(4)]
MELANOCORTIN MC(1)
MC(4)
MUSCARINIC M(1)
M(2) M(3) M(4)
NEUROKININ NK(1)
NEUROPEPTIDE Y Y(1)
OPIOD & OPIOD-LIKE delta(1) [OP1,DOP] kappa [OP2, KOP] mu [OP3, MOP]
PLATELET ACTIVATING FACTOR PAF
SEROTONIN 5-HT (1A)
5-HT (1B)
5-HT (2A)
5-HT (2B)
5-HT (2C)
VASOPRESSIN V(1a)
TRANSPORTERS
ADENOSINE adenosine transporter DOPAMINE dopamine transporter GABA GABA transporter NOREPINEPHRINE norepinephrine transporter SEROTONIN 5-HT transporter
ION CHANNELS
GABA CHANNELS GABA(A) [flunitrazepam, central]
GABA(A) [Ro-15-1788] Cl(-) channel [GABA-gated]
GLUTAMATE CHANNELS AMPA
kainate NMDA [agonism] NMDA [glycine] NMDA [phencyclidine] NMDA [polyamine]
GLYCINE CHANNELS glycine [strychnine-sensitive] NICOTINIC CHANNELS N neuronal acetylcholine
N neuronal acetylcholine α(1) [bungarotoxin]
SEROTONIN CHANNELS 5-HT(3)
Ca(2+) CHANNELS Ca(2+) channel [L, dihydropyridine site]
Ca(2+) channel [L, diltiazem site] Ca(2+) channel [L, verapamil site] Ca(2+) channel [N]
K+ CHANNELS hERG K(ATP) channel
Na(+) CHANNELS Na(+) channel [site 2]
NUCLEAR RECEPTORS
NON-STEROID NUCLEAR RECEPTORS PPAR(γ)
STEROID NUCLEAR RECEPTORS AR
ERα
GR
PR-B
KINASES
RTK IRK [InsR] CTK Lck kinase AGC PKC [non-selective]
OTHER NON-KINASE ENZYMES
AA METABOLISM COX(1)
COX(2)
ATP(ASE) ATPase [Na(+)/K(+)]
MONOAMINE & NEUROTRANSMITTER MAO-A
MAO-A
PHOSPHODIESTERASES PDE3
PDE4
SERINE PROTEASES cathepsin G
METALLOPROTEASES ACE
MISCELLANEOUS ENZYMES acetylcholinesterase [ACES]
Sheet1
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