Linker Information
General Information of This Linker
| Linker ID |
LIN0KXXOP
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| Linker Name |
H1H21234N-N297Q- LP4 lINKER
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C79H126N16O24S
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| Isosmiles |
CC([C@H](NC([C@H](NC(CCOCCOCCOCCOCCNC(CCC(N(CC1=C2C=CC=C1)C3=C(C4=C2N=NN4CCCCCOCCOCCN)C=CC=C3)=O)=O)=O)CCCCNC(COC5CCCCCC6=C5N=NN6CCOCCOCCOCCOCCC(NCCS(O)(=O)=O)=O)=O)=O)C(N[C@@H](CCCNC(N)=O)C(O)=O)=O)C
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| InChI |
InChI=1S/C79H126N16O24S/c1-58(2)72(77(102)87-63(78(103)104)20-15-30-85-79(81)105)88-76(101)62(19-11-12-29-82-70(99)57-119-66-23-6-3-5-22-65-74(66)90-91-94(65)34-40-114-46-50-118-54-52-115-47-42-110-36-26-68(97)84-32-55-120(106,107)108)86-69(98)27-37-111-43-48-116-51-53-117-49-45-113-39-31-83-67(96)24-25-71(100)93-56-59-16-7-8-17-60(59)73-75(61-18-9-10-21-64(61)93)95(92-89-73)33-13-4-14-35-109-41-44-112-38-28-80/h7-10,16-18,21,58,62-63,66,72H,3-6,11-15,19-20,22-57,80H2,1-2H3,(H,82,99)(H,83,96)(H,84,97)(H,86,98)(H,87,102)(H,88,101)(H,103,104)(H3,81,85,105)(H,106,107,108)/t62-,63+,66?,72+/m1/s1
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| InChIKey |
CNUVRYUDXTVDFN-BKBCWDEQSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1716.032
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Polar area
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530.67
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Complexity
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3662.846966
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xlogp Value
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1.8302
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Heavy Count
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120
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Rot Bonds
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66
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Hbond acc
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29
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Hbond Donor
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11
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
H1H21234N-N297Q-LP4 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.923 nM
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Positive MSR1 expression (MSR1+++/++) | ||
| Method Description |
Anti-MSR1-LXR Agonist Conjugate Activity in Differentiated THP-2/LXR-Luc cells
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| In Vitro Model | Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia | THP-1/LXR-Luc cells | CVCL_5115 | ||
References